|
Binding affinity for Cannabinoid receptor 2 by the ability to displace radiolabeled CP-55940 from mouse spleen synaptosomes
|
Mus musculus
|
230.0
nM
|
|
Journal : Bioorg. Med. Chem. Lett.
Title : Novel 1',1'-chain substituted Delta(8)-tetrahydrocannabinols.
Year : 2002
Volume : 12
Issue : 24
First Page : 3583
Last Page : 3586
Authors : Papahatjis DP, Nikas SP, Andreou T, Makriyannis A.
Abstract : 1',1'-Cyclopropyl side chain substituents enhance the affinities of Delta(8)-tetrahydrocannabinol and respective cannabidiol analogues for the CB1 and CB2 cannabinoid receptors. The results support the hypothesis for a subsite within CB1 and CB2 binding domain at the level of the benzylic side chain carbon in the tetrahydrocannabinol and cannabidiol series. Efficient procedures for the synthesis of 1',1'-cyclopropyl analogues are described.
|
Inhibitory potency against fatty acid amide hydrolase activity in mouse brain microsomes in presence of 58 uM anandamide at 160 uM
|
Mus musculus
|
66.0
%
|
|
Journal : J. Med. Chem.
Title : The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
Year : 2005
Volume : 48
Issue : 16
First Page : 5059
Last Page : 5087
Authors : Lambert DM, Fowler CJ.
|
Agonist activity at rat TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx
|
Rattus norvegicus
|
96.0
nM
|
|
Journal : J. Med. Chem.
Title : Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Year : 2010
Volume : 53
Issue : 14
First Page : 5085
Last Page : 5107
Authors : Baraldi PG, Preti D, Materazzi S, Geppetti P.
|
Binding affinity to GPR55
|
None
|
445.0
nM
|
|
Journal : J. Med. Chem.
Title : Emerging targets in osteoporosis disease modification.
Year : 2010
Volume : 53
Issue : 11
First Page : 4332
Last Page : 4353
Authors : Allen JG, Fotsch C, Babij P.
|
Antiosteoporotic activity in mouse assessed as decrease in bone resorption-associated serum CTX-1 level at 10 mg/kg administered 3 times a week for 8 weeks
|
Mus musculus
|
18.0
%
|
|
Journal : J. Med. Chem.
Title : Emerging targets in osteoporosis disease modification.
Year : 2010
Volume : 53
Issue : 11
First Page : 4332
Last Page : 4353
Authors : Allen JG, Fotsch C, Babij P.
|
Inhibition of human neutrophil migration incubated for 30 mins prior to fMLP challenge by boyden chamber assay
|
Homo sapiens
|
0.45
nM
|
|
Journal : Bioorg. Med. Chem.
Title : Cannabidiol (CBD) and its analogs: a review of their effects on inflammation.
Year : 2015
Volume : 23
Issue : 7
First Page : 1377
Last Page : 1385
Authors : Burstein S.
Abstract : First isolated from Cannabis in 1940 by Roger Adams, the structure of CBD was not completely elucidated until 1963. Subsequent studies resulted in the pronouncement that THC was the 'active' principle of Cannabis and research then focused primarily on it to the virtual exclusion of CBD. This was no doubt due to the belief that activity meant psychoactivity that was shown by THC and not by CBD. In retrospect this must be seen as unfortunate since a number of actions of CBD with potential therapeutic benefit were downplayed for many years. In this review, attention will be focused on the effects of CBD in the broad area of inflammation where such benefits seem likely to be developed. Topics covered in this review are; the medicinal chemistry of CBD, CBD receptor binding involved in controlling Inflammation, signaling events generated by CBD, downstream events affected by CBD (gene expression and transcription), functional effects reported for CBD and combined THC plus CBD treatment.
|
Inhibition of Cav1.2 calcium current measured using whole cell patch clamp in rat ventricular myocytes
|
Rattus norvegicus
|
100.0
nM
|
|
Title : IC50 data for the L-type calcium channel extracted from a set of literature articles
|
Competitive inhibition of human liver microsomes CYP1A1 expressed in supersomes coexpressing NADPH-CYP reductase using 7-Ethoxyresorufin as substrate measured every 5 mins for 30 mins in presence of NADPH by fluorescence assay
|
Homo sapiens
|
150.0
nM
|
|
Journal : Eur J Med Chem
Title : Inhibitors of cytochrome P450 (CYP) 1B1.
Year : 2017
Volume : 135
First Page : 296
Last Page : 306
Authors : Dutour R, Poirier D.
Abstract : Human cytochrome P450 1B1 (CYP1B1) is involved in the metabolism of various drugs. This enzyme catalyzes the hydroxylation of aryl compounds, thus generating more polar metabolites that can be easily excreted. CYP1B1 is also known for its ability to activate procarcinogens into carcinogens. For example, it can hydroxylate 17β-estradiol (E2) into 4-hydroxy-E2, which can promote tumorigenesis as a potent estrogen, or after being transformed into E2-3,4-quinone. Since elevated expression levels of CYP1B1 have been reported in various cancers, but not in normal tissues, this enzyme represents an interesting therapeutic target. This review put emphasis on different families of inhibitors, especially those reported since 2003.
|
Displacement of [3H]-CP55940 from recombinant human CB2 receptor expressed in Sf9 cell membranes co-expressing Galphai3beta1gamma2 measured after 90 mins by scintillation counting method
|
Homo sapiens
|
372.0
nM
|
|
Journal : J Nat Prod
Title : Plant-Based Modulators of Endocannabinoid Signaling.
Year : 2019
Volume : 82
Issue : 3
First Page : 636
Last Page : 646
Authors : Cunningham CW.
Abstract : Extracts from Cannabis species have aided the discovery of the endocannabinoid signaling system (ECSS) and phytocannabinoids that possess broad therapeutic potential. Whereas the reinforcing effects of C. sativa are largely attributed to CB1 receptor agonism by Δ9-tetrahydrocannabinol (Δ9-THC), the observed medicinal effects of Cannabis arise from the combined actions of various compounds. In addition to compounds bearing a classical cannabinoid structure, naturally occurring fatty acid amides and esters resembling anandamide and 2-arachidonoyl glycerol isolated from non- Cannabis species are also valuable tools for studying ECSS function. This review highlights the potential of plant-based secondary metabolites from Cannabis and unrelated species as ECSS modulators.
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
25.7
%
|
|
Title : Identification of inhibitors of SARS-Cov2 M-Pro enzymatic activity using a small molecule repurposing screen
Year : 2020
Authors : Maria Kuzikov, Elisa Costanzi, Jeanette Reinshagen, Francesca Esposito, Laura Vangeel, Markus Wolf, Bernhard Ellinger, Carsten Claussen, Gerd Geisslinger, Angela Corona, Daniela Iaconis, Carmine Talarico, Candida Manelfi, Rolando Cannalire, Giulia Rossetti, Jonas Gossen, Simone Albani, Francesco Musiani, Katja Herzog, Yang Ye, Barbara Giabbai, Nicola Demitri, Dirk Jochmans, Steven De Jonghe, Jasper Rymenants, Vincenzo Summa, Enzo Tramontano, Andrea R. Beccari, Pieter Leyssen, Paola Storici, Johan Neyts, Philip Gribbon, and Andrea Zaliani
Abstract : Compound repurposing is an important strategy being pursued in the identification of effective treatment against the SARS-CoV-2 infection and COVID-19 disease. In this regard, SARS-CoV-2 main protease (M-Pro), also termed 3CL-Pro, is an attractive drug target as it plays a central role in viral replication by processing the viral polyprotein into 11 non-structural proteins. We report the results of a screening campaign involving ca 8.7 K compounds containing marketed drugs, clinical and preclinical candidates, and chemicals regarded as safe in humans. We confirmed previously reported inhibitors of 3CL-Pro, but we have also identified 68 compounds with IC50 lower than 1 uM and 127 compounds with IC50 lower than 5 uM. Profiling showed 67% of confirmed hits were selective (> 5 fold) against other Cys- and Ser- proteases (Chymotrypsin and Cathepsin-L) and MERS 3CL-Pro. Selected compounds were also analysed in their binding characteristics.
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.03
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.03
%
|
|
Title : Cytopathic SARS-Cov2 screening on VERO-E6 cells in a large repurposing effort
Year : 2020
Authors : Andrea Zaliani, Laura Vangeel, Jeanette Reinshagen, Daniela Iaconis, Maria Kuzikov, Oliver Keminer, Markus Wolf, Bernhard Ellinger, Francesca Esposito, Angela Corona, Enzo Tramontano, Candida Manelfi, Katja Herzog, Dirk Jochmans, Steven De Jonghe, Winston Chiu, Thibault Francken, Joost Schepers, Caroline Collard, Kayvan Abbasi, Carsten Claussen , Vincenzo Summa, Andrea R. Beccari, Johan Neyts, Philip Gribbon and Pieter Leyssen
Abstract : Worldwide, there are intensive efforts to identify repurposed drugs as potential therapies against SARS-CoV-2 infection and the associated COVID-19 disease. To date, the anti-inflammatory drug dexamethasone and (to a lesser extent) the RNA-polymerase inhibitor remdesivir have been shown to be effective in reducing mortality and patient time to recovery, respectively, in patients. Here, we report the results of a phenotypic screening campaign within an EU-funded project (H2020-EXSCALATE4COV) aimed at extending the repertoire of anti-COVID therapeutics through repurposing of available compounds and highlighting compounds with new mechanisms of action against viral infection. We screened 8702 molecules from different repurposing libraries, to reveal 110 compounds with an anti-cytopathic IC50 < 20 µM. From this group, 18 with a safety index greater than 2 are also marketed drugs, making them suitable for further study as potential therapies against COVID-19. Our result supports the idea that a systematic approach to repurposing is a valid strategy to accelerate the necessary drug discovery process.
|
Inhibition of NLRP3 inflammasome activation in LPS-stimulated human THP1 cells assessed as reduction in IL-1beta secretion at 0.1 uM incubated for 1 hr followed by nigericin addition and measured after 1 hr by ELISA relative to control
|
Homo sapiens
|
63.9
%
|
|
Journal : J Nat Prod
Title : Inhibitory Effect of Cannabidiol on the Activation of NLRP3 Inflammasome Is Associated with Its Modulation of the P2X7 Receptor in Human Monocytes.
Year : 2020
Volume : 83
Issue : 6
First Page : 2025
Last Page : 2029
Authors : Liu C, Ma H, Slitt AL, Seeram NP.
Abstract : Cannabidiol (CBD), a phytocannabinoid, has been reported to have anti-inflammatory effects associated with NLRP3 inflammasome activation, but its mechanism of anti-inflammasome action remains unclear. Herein, we report CBD's effect on NLRP3 inflammasome activation and its modulation of P2X7, an inflammasome activation-related receptor, in human THP-1 monocytes. CBD (0.1, 1, and 10 μM) exerted anti-inflammasome activity in LPS-nigericin-stimulated THP-1 monocytes by reducing media IL-1β concentration (by 63.9%, 64.1%, and 83.1%, respectively), which was similar to the known NLRP3 inflammasome inhibitors oridonin and MCC950 (16.9% vs 20.8% and 17.4%, respectively; at 10 μM). CBD (10 μM) decreased nigericin-alone- and nigericin-lipopolysaccharide-induced potassium efflux by 13.7% and 13.0%, respectively, in THP-1 monocytes, strongly suggesting P2X7 receptor modulation. Computational docking data supported the potential for CBD binding to the P2X7 receptor via interaction with GLU 172 and VAL 173 residues. Overall, the observed CBD suppressive effect on NLRP3 inflammasome activation in THP-1 monocytes was associated with decreased potassium efflux, as well as in silico prediction of P2X7 receptor binding. CBD inhibitory effects on the NLRP3 inflammasome may contribute to the overall anti-inflammatory effects reported for this phytocannabinoid.
|
Inhibition of NLRP3 inflammasome activation in LPS-stimulated human THP1 cells assessed as reduction in IL-1beta secretion at 1 uM incubated for 1 hr followed by nigericin addition and measured after 1 hr by ELISA relative to control
|
Homo sapiens
|
64.1
%
|
|
Journal : J Nat Prod
Title : Inhibitory Effect of Cannabidiol on the Activation of NLRP3 Inflammasome Is Associated with Its Modulation of the P2X7 Receptor in Human Monocytes.
Year : 2020
Volume : 83
Issue : 6
First Page : 2025
Last Page : 2029
Authors : Liu C, Ma H, Slitt AL, Seeram NP.
Abstract : Cannabidiol (CBD), a phytocannabinoid, has been reported to have anti-inflammatory effects associated with NLRP3 inflammasome activation, but its mechanism of anti-inflammasome action remains unclear. Herein, we report CBD's effect on NLRP3 inflammasome activation and its modulation of P2X7, an inflammasome activation-related receptor, in human THP-1 monocytes. CBD (0.1, 1, and 10 μM) exerted anti-inflammasome activity in LPS-nigericin-stimulated THP-1 monocytes by reducing media IL-1β concentration (by 63.9%, 64.1%, and 83.1%, respectively), which was similar to the known NLRP3 inflammasome inhibitors oridonin and MCC950 (16.9% vs 20.8% and 17.4%, respectively; at 10 μM). CBD (10 μM) decreased nigericin-alone- and nigericin-lipopolysaccharide-induced potassium efflux by 13.7% and 13.0%, respectively, in THP-1 monocytes, strongly suggesting P2X7 receptor modulation. Computational docking data supported the potential for CBD binding to the P2X7 receptor via interaction with GLU 172 and VAL 173 residues. Overall, the observed CBD suppressive effect on NLRP3 inflammasome activation in THP-1 monocytes was associated with decreased potassium efflux, as well as in silico prediction of P2X7 receptor binding. CBD inhibitory effects on the NLRP3 inflammasome may contribute to the overall anti-inflammatory effects reported for this phytocannabinoid.
|
Inhibition of NLRP3 inflammasome activation in LPS-stimulated human THP1 cells assessed as reduction in IL-1beta secretion at 10 uM incubated for 1 hr followed by nigericin addition and measured after 1 hr by ELISA relative to control
|
Homo sapiens
|
83.1
%
|
|
Journal : J Nat Prod
Title : Inhibitory Effect of Cannabidiol on the Activation of NLRP3 Inflammasome Is Associated with Its Modulation of the P2X7 Receptor in Human Monocytes.
Year : 2020
Volume : 83
Issue : 6
First Page : 2025
Last Page : 2029
Authors : Liu C, Ma H, Slitt AL, Seeram NP.
Abstract : Cannabidiol (CBD), a phytocannabinoid, has been reported to have anti-inflammatory effects associated with NLRP3 inflammasome activation, but its mechanism of anti-inflammasome action remains unclear. Herein, we report CBD's effect on NLRP3 inflammasome activation and its modulation of P2X7, an inflammasome activation-related receptor, in human THP-1 monocytes. CBD (0.1, 1, and 10 μM) exerted anti-inflammasome activity in LPS-nigericin-stimulated THP-1 monocytes by reducing media IL-1β concentration (by 63.9%, 64.1%, and 83.1%, respectively), which was similar to the known NLRP3 inflammasome inhibitors oridonin and MCC950 (16.9% vs 20.8% and 17.4%, respectively; at 10 μM). CBD (10 μM) decreased nigericin-alone- and nigericin-lipopolysaccharide-induced potassium efflux by 13.7% and 13.0%, respectively, in THP-1 monocytes, strongly suggesting P2X7 receptor modulation. Computational docking data supported the potential for CBD binding to the P2X7 receptor via interaction with GLU 172 and VAL 173 residues. Overall, the observed CBD suppressive effect on NLRP3 inflammasome activation in THP-1 monocytes was associated with decreased potassium efflux, as well as in silico prediction of P2X7 receptor binding. CBD inhibitory effects on the NLRP3 inflammasome may contribute to the overall anti-inflammatory effects reported for this phytocannabinoid.
|
Antagonist activity at rat TRPA1 expressed in HEK293 cells assessed as inhibition of allylisothiocyanate-induced Ca2+ response preincubated for 5 mins followed by allylisothiocyanate addition by Fluo-4AM dye based fluorescence assay
|
Rattus norvegicus
|
450.0
nM
|
|
Journal : J Nat Prod
Title : Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, Cannabis sativa L., Is a Selective Thermo-TRP Modulator.
Year : 2020
Volume : 83
Issue : 9
First Page : 2727
Last Page : 2736
Authors : Chianese G,Lopatriello A,Schiano-Moriello A,Caprioglio D,Mattoteia D,Benetti E,Ciceri D,Arnoldi L,De Combarieu E,Vitale RM,Amodeo P,Appendino G,De Petrocellis L,Taglialatela-Scafati O
Abstract : Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural characterization of cannabitwinol, complicated by broadening of H NMR signals and lack of expected 2D NMR correlations at room temperature, was fully carried out in methanol-d at -30 °C. All the attempts to prepare CBDD by reaction of CBD with formaldehyde or its iminium analogue (Eschenmoser salt) failed, suggesting that this sterically congested dimer is the result of enzymatic reactions on the corresponding monomeric acids. Analysis of the cannabitwinol profile of transient receptor potential (TRP) modulation evidenced the impact of dimerization, revealing a selectivity for channels activated by a decrease of temperature (TRPM8 and TRPA1) and the lack of significant affinity for those activated by an increase of temperature (e.g., TRPV1). The putative binding modes of cannabitwinol with TRPA1 and TRPM8 were investigated in detail by a molecular docking study using the homology models of both channels.
|
Agonist activity at rat TRPA1 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of allylisothiocyanate by Fluo-4-AM dye based spectrofluorimetric method
|
Rattus norvegicus
|
480.0
nM
|
|
Journal : J Nat Prod
Title : Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, Cannabis sativa L., Is a Selective Thermo-TRP Modulator.
Year : 2020
Volume : 83
Issue : 9
First Page : 2727
Last Page : 2736
Authors : Chianese G,Lopatriello A,Schiano-Moriello A,Caprioglio D,Mattoteia D,Benetti E,Ciceri D,Arnoldi L,De Combarieu E,Vitale RM,Amodeo P,Appendino G,De Petrocellis L,Taglialatela-Scafati O
Abstract : Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural characterization of cannabitwinol, complicated by broadening of H NMR signals and lack of expected 2D NMR correlations at room temperature, was fully carried out in methanol-d at -30 °C. All the attempts to prepare CBDD by reaction of CBD with formaldehyde or its iminium analogue (Eschenmoser salt) failed, suggesting that this sterically congested dimer is the result of enzymatic reactions on the corresponding monomeric acids. Analysis of the cannabitwinol profile of transient receptor potential (TRP) modulation evidenced the impact of dimerization, revealing a selectivity for channels activated by a decrease of temperature (TRPM8 and TRPA1) and the lack of significant affinity for those activated by an increase of temperature (e.g., TRPV1). The putative binding modes of cannabitwinol with TRPA1 and TRPM8 were investigated in detail by a molecular docking study using the homology models of both channels.
|
Agonist activity at rat TRPV4 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method
|
Rattus norvegicus
|
900.0
nM
|
|
Journal : J Nat Prod
Title : Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, Cannabis sativa L., Is a Selective Thermo-TRP Modulator.
Year : 2020
Volume : 83
Issue : 9
First Page : 2727
Last Page : 2736
Authors : Chianese G,Lopatriello A,Schiano-Moriello A,Caprioglio D,Mattoteia D,Benetti E,Ciceri D,Arnoldi L,De Combarieu E,Vitale RM,Amodeo P,Appendino G,De Petrocellis L,Taglialatela-Scafati O
Abstract : Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural characterization of cannabitwinol, complicated by broadening of H NMR signals and lack of expected 2D NMR correlations at room temperature, was fully carried out in methanol-d at -30 °C. All the attempts to prepare CBDD by reaction of CBD with formaldehyde or its iminium analogue (Eschenmoser salt) failed, suggesting that this sterically congested dimer is the result of enzymatic reactions on the corresponding monomeric acids. Analysis of the cannabitwinol profile of transient receptor potential (TRP) modulation evidenced the impact of dimerization, revealing a selectivity for channels activated by a decrease of temperature (TRPM8 and TRPA1) and the lack of significant affinity for those activated by an increase of temperature (e.g., TRPV1). The putative binding modes of cannabitwinol with TRPA1 and TRPM8 were investigated in detail by a molecular docking study using the homology models of both channels.
|
Antagonist activity at rat TRPV3 expressed in HEK293 cells assessed as inhibition of thymol-induced Ca2+ response preincubated for 5 mins followed by thymol addition by Fluo-4AM dye based fluorescence assay
|
Rattus norvegicus
|
750.0
nM
|
|
Journal : J Nat Prod
Title : Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, Cannabis sativa L., Is a Selective Thermo-TRP Modulator.
Year : 2020
Volume : 83
Issue : 9
First Page : 2727
Last Page : 2736
Authors : Chianese G,Lopatriello A,Schiano-Moriello A,Caprioglio D,Mattoteia D,Benetti E,Ciceri D,Arnoldi L,De Combarieu E,Vitale RM,Amodeo P,Appendino G,De Petrocellis L,Taglialatela-Scafati O
Abstract : Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural characterization of cannabitwinol, complicated by broadening of H NMR signals and lack of expected 2D NMR correlations at room temperature, was fully carried out in methanol-d at -30 °C. All the attempts to prepare CBDD by reaction of CBD with formaldehyde or its iminium analogue (Eschenmoser salt) failed, suggesting that this sterically congested dimer is the result of enzymatic reactions on the corresponding monomeric acids. Analysis of the cannabitwinol profile of transient receptor potential (TRP) modulation evidenced the impact of dimerization, revealing a selectivity for channels activated by a decrease of temperature (TRPM8 and TRPA1) and the lack of significant affinity for those activated by an increase of temperature (e.g., TRPV1). The putative binding modes of cannabitwinol with TRPA1 and TRPM8 were investigated in detail by a molecular docking study using the homology models of both channels.
|
Agonist activity at rat TRPV3 stably transfected in HEK293 cells assessed as increase in calcium influx in presence of ionomycin by Fluo-4-AM dye based spectrofluorimetric method
|
Rattus norvegicus
|
510.0
nM
|
|
Journal : J Nat Prod
Title : Cannabitwinol, a Dimeric Phytocannabinoid from Hemp, Cannabis sativa L., Is a Selective Thermo-TRP Modulator.
Year : 2020
Volume : 83
Issue : 9
First Page : 2727
Last Page : 2736
Authors : Chianese G,Lopatriello A,Schiano-Moriello A,Caprioglio D,Mattoteia D,Benetti E,Ciceri D,Arnoldi L,De Combarieu E,Vitale RM,Amodeo P,Appendino G,De Petrocellis L,Taglialatela-Scafati O
Abstract : Cannabitwinol (CBDD, 3), the second member of a new class of dimeric phytocannabinoids in which two units are connected by a methylene bridge, was isolated from a hemp (Cannabis sativa L.) industrial extract. The structural characterization of cannabitwinol, complicated by broadening of H NMR signals and lack of expected 2D NMR correlations at room temperature, was fully carried out in methanol-d at -30 °C. All the attempts to prepare CBDD by reaction of CBD with formaldehyde or its iminium analogue (Eschenmoser salt) failed, suggesting that this sterically congested dimer is the result of enzymatic reactions on the corresponding monomeric acids. Analysis of the cannabitwinol profile of transient receptor potential (TRP) modulation evidenced the impact of dimerization, revealing a selectivity for channels activated by a decrease of temperature (TRPM8 and TRPA1) and the lack of significant affinity for those activated by an increase of temperature (e.g., TRPV1). The putative binding modes of cannabitwinol with TRPA1 and TRPM8 were investigated in detail by a molecular docking study using the homology models of both channels.
|
Inhibition of 5-HT7A (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT2A (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of muscarinic acetylcholine receptor M4 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of H4 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of M3 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of sigma 1 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha2A receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of D5 dopamine receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT1E receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of beta1 adrenergic receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT3 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha1A receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT1D (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of beta-3 adrenergic receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of NET receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT2B (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT6 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of DRD4 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha1B receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of muscarinic acetylcholine receptor M5 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of GABAA receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of rat brain BZP at 10 uM relative to control
|
Rattus norvegicus
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of PBR (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha1D receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of muscarinic acetylcholine receptor M2 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT1B (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of DAT (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of beta-2 adrenergic receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of D3 dopamine receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT1A (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT5A (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of muscarinic acetylcholine receptor M1 (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of D2 dopamine receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of histamine H1 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of SERT (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of histamine H2 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of 5-HT2C (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of mu-type opioid receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of kappa-type opioid receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of D1 dopamine receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of histamine H3 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha2B receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of sigma2 receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of alpha2C receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Inhibition of delta-type opioid receptor receptor (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
50.0
%
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Competitive inhibition of human recombinant CYP1A1 using 7-Ethoxyresorufin as substrate by Lineweaver-Burk plot analysis
|
Homo sapiens
|
160.0
nM
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Mixed type inhibition of human recombinant CYP2B6 expressed in baculovirus-infected insect cells using coumarin as substrate preincubated for 5 mins followed by NADPH-generating system addition by Lineweaver-Burk plot analysis
|
Homo sapiens
|
690.0
nM
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Mixed type inhibition of human recombinant CYP2C19 using (S)-mephenytoin as substrate preincubated for 5 mins followed by NADPH-generating system addition measured after 40 mins by Lineweaver-Burk plot analysis
|
Homo sapiens
|
790.0
nM
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Competitive inhibition of human recombinant CYP3A5 expressed in baculovirus-infected insect cells using diltiazem as substrate incubated for 15 mins followed by NADPH-generating system addition by Michaelis-Menten plot analysis
|
Homo sapiens
|
190.0
nM
|
|
Journal : J Med Chem
Title : The Essential Medicinal Chemistry of Cannabidiol (CBD).
Year : 2020
Volume : 63
Issue : 21
First Page : 12137
Last Page : 12155
Authors : Nelson KM,Bisson J,Singh G,Graham JG,Chen SN,Friesen JB,Dahlin JL,Niemitz M,Walters MA,Pauli GF
Abstract : This Perspective of the published essential medicinal chemistry of cannabidiol (CBD) provides evidence that the popularization of CBD-fortified or CBD-labeled health products and CBD-associated health claims lacks a rigorous scientific foundation. CBD's reputation as a cure-all puts it in the same class as other "natural" panaceas, where valid ethnobotanicals are reduced to single, purportedly active ingredients. Such reductionist approaches oversimplify useful, chemically complex mixtures in an attempt to rationalize the commercial utility of natural compounds and exploit the "natural" label. Literature evidence associates CBD with certain semiubiquitous, broadly screened, primarily plant-based substances of undocumented purity that interfere with bioassays and have a low likelihood of becoming therapeutic agents. Widespread health challenges and pandemic crises such as SARS-CoV-2 create circumstances under which scientists must be particularly vigilant about healing claims that lack solid foundational data. Herein, we offer a critical review of the published medicinal chemistry properties of CBD, as well as precise definitions of CBD-containing substances and products, distilled to reveal the essential factors that impact its development as a therapeutic agent.
|
Antioxidant activity assessed as DPPH radical scavenging activity at 100 uM incubated for 2 hrs by microplate reader method
|
None
|
66.7
%
|
|
|
Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition and measured after 20 mins by Ellman's method
|
Equus caballus
|
670.0
nM
|
|
|
Inhibition of caspase-1 activity in H2O2-stimulated human HaCaT cells assessed as reduction in enzyme activity at 10 uM using YUAD-Pna as a substrate measured after 2 hrs by colorimetric assay relative to control
|
Homo sapiens
|
15.7
%
|
|
|
Inhibition of IL-1beta expression in H2O2- stimulated human HaCaT cells at 10 uM incubated for 6 hrs followed by H2O2 stimulation measured after 24 hrs by ELISA relative to control
|
Homo sapiens
|
16.2
%
|
|
|
Binding affinity to recombinant human caspase-1 assessed as dissociation constant measured after 90 sec by SPR method
|
Homo sapiens
|
18.8
nM
|
|
|
Binding affinity to recombinant human caspase-1 assessed as dissociation constant at equilibrium measured after 30 sec by SPR method
|
Homo sapiens
|
0.078
1/s
|
|
|
Inhibition of human LDHB assessed as reduction in lactate production using pyruvate as substrate at 10 uM in presence of NADH by spectrophotometric analysis relative to control
|
Homo sapiens
|
50.0
%
|
|
