MORPHINE

/static/temp/default.svg Search structure
Synonyms
Status
Molecule Category Free-form
ATC N02AA01
UNII 76I7G6D29C
EPA CompTox DTXSID9023336

Structure

InChI Key BQJCRHHNABKAKU-KBQPJGBKSA-N
Smiles CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5
InChI
InChI=1S/C17H19NO3/c1-18-7-6-17-10-3-5-13(20)16(17)21-15-12(19)4-2-9(14(15)17)8-11(10)18/h2-5,10-11,13,16,19-20H,6-8H2,1H3/t10-,11+,13-,16-,17-/m0/s1

Physicochemical Descriptors

Property Name Value
Molecular Formula C17H19NO3
Molecular Weight 285.34
AlogP 1.2
Hydrogen Bond Acceptor 4.0
Hydrogen Bond Donor 2.0
Number of Rotational Bond 0.0
Polar Surface Area 52.93
Molecular species BASE
Aromatic Rings 1.0
Heavy Atoms 21.0
Assay Description Organism Bioactivity Reference
Binding to delta opioid receptor by using [3H]DPDPE as radioligand in guinea pig brain minus cerebellum Cavia porcellus 430.0 nM
Inhibition of twitches in guinea pig ileum Cavia porcellus 75.0 nM
Inhibition of opioid activity in electricaly stimulated myenteric plexus longitudinal muscle of guinea pig ileum(GPI) preparation Cavia porcellus 33.1 nM
Inhibitory activity of compound in guinea pig ileum tissue Cavia porcellus 0.13 nM
Inhibitory concentration evaluated in electrically stimulated guinea pig myenteric plexus longitudinal muscle Cavia porcellus 69.7 nM
Irreversible antagonistic potency in guinea pig ileal longitudinal muscle (GPI) Cavia porcellus 292.0 nM
Opioid agonist activity was measured by Anti-Straub tail (AST) test after subcutaneous administration in guinea pig ilium Cavia porcellus 79.0 nM
Opioid agonistic activity was measured in guinea pig ileum Cavia porcellus 68.2 nM
Tested for potent reversible agonist activity on electrically stimulated guinea pig ileal longitudinal muscle preparation Cavia porcellus 24.0 nM
Concentration inhibiting electrically induced contraction of guinea pig ileum(GPI) at an ED50 of 5.6(ug/kg). Cavia porcellus 58.6 nM
Evaluated for the inhibition concentration in the guinea pig ileal longitudinal muscle preparation (GPI) Cavia porcellus 2.92 nM
In vitro inhibition of contractions in the electrically stimulated guinea pig ileum. Cavia porcellus 58.6 nM
Inhibition of the electrically induced muscle contractions was determined using the guinea pig ileum Cavia porcellus 51.0 nM
Agonist activity in guinea pig ileum preparation Cavia porcellus 79.8 nM
Inhibitory effect was measured on guinea pig ileum for maximal contraction Cavia porcellus 140.0 nM
Mu opioid receptor agonist activity as inhibition of electrically stimulated mysenteric plexus in guinea pig ileum Cavia porcellus 57.3 nM
Opioid antagonist activity in guinea pig ileum assay Cavia porcellus 6.31 nM
Binding to kappa opioid receptor by using [3H]U-69593 as radioligand in guinea pig cerebellum Cavia porcellus 130.0 nM
Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with 0.2 mg/kg Naloxone Cavia porcellus 0.13 nM
Compound was evaluated for the inhibition of twitches in mouse vas deferens Mus musculus 500.0 nM
Concentration inhibiting electrically induced contraction of mouse vas deferens(MVD) at an ED50 of 5.6(ug/kg). Mus musculus 644.0 nM
Inhibition of opioid activity in electricaly stimulated myenteric plexus longitudinal muscle of mouse vas deferens(MVD) preparation Mus musculus 194.0 nM
Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus;longitudinal muscle)[agonist action at mu 1 opioid receptors) and inhibition of electrically evoked contraction of mouse vas deferens (agonist action at delta 1 opioid receptor) None 309.0 nM
Opioid agonistic activity was measured in mouse vas deferens Mus musculus 492.0 nM
Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with saline Mus musculus 1.0 nM
Binding to mu opioid receptor by using [3H]DAMGO as radioligand in guinea pig brain minus cerebellum Cavia porcellus 8.5 nM
Antagonist activity in mouse vas deferens preparation. Mus musculus 244.0 nM
Binding affinity against mu opioid receptor was determined in brain membrane preparations from male Hartley guinea-pigs Cavia porcellus 38.0 nM
In vivo binding affinity against mu opioid receptor was measured by using labeled ligand [3H]naloxone (0.5 nM) Cavia porcellus 38.0 nM
Compound was evaluated for binding affinity towards mu-specific opiate receptor from combinatorial peptoid library None 2.0 nM
Inhibition of [3H]dihydromorphine (1 nM) binding to mu opioid receptor of rat brain homogenate Rattus norvegicus 3.0 nM
50% Inhibition of stereospecific [3H]-naltrexone (10e-9 M) binding towards opiate receptor in rat brain homogenate None 0.027 nM
Concentration required to inhibit opiate receptor using radioligand [3H]- Etorphine None 160.0 nM
Inhibitory activity against opiate receptor in rat using [3H]naloxone as radioligand None 8.6 nM
Inhibition of [3H]dihydromorphine binding to opiate receptor from rat neural membranes after incubation at 20 nM concentration at 37 degree C None 1.0 %
Binding affinities against Opioid receptor mu 1 of guinea pig brain membrane using [3H]DAGO as the radioligand using competition binding assays. Cavia porcellus 7.71 nM
Binding affinity for the Opioid receptor mu 1 Cavia porcellus 1.8 nM
Binding affinity of compound was determined against Opioid receptor mu 1 from native receptor in guinea pig Cavia porcellus 3.0 nM
Inhibition of [3H]naltrindole binding to opioid receptor delta 1 of Chinese hamster ovary membrane Cricetulus griseus 140.0 nM
Displacement of [3H]-BRL 52537 from opioid receptor kappa site in guinea pig Cavia porcellus 301.0 nM
Displacement of [3H]U-69593 from kappa opioid receptors in guine pig brain (minus cerebellum). Cavia porcellus 151.0 nM
Receptor binding affinity towards opioid receptor kappa Cavia porcellus 301.0 nM
Binding affinity against opioid receptor kappa 1 from human cloned receptor None 64.0 nM
In vitro binding affinity at opioid receptor kappa 1 was determined in human CHO cells using [3H]U-69593 None 113.0 nM
In vitro potency was measured against human Opioid receptor kappa 1 None 260.0 nM
Binding affinity to displace radioligand [3H]DAMGO on Opioid receptor mu 1 in guinea pig membranes. Cavia porcellus 0.88 nM
Binding affinity towards Opioid receptor mu 1 of guinea pig brain membranes using radioligand 0.25 nM [3H]DAMGO Cavia porcellus 0.88 nM
In vitro binding affinity against cloned human Opioid receptor delta 1 expressed in HEK 293S cells None 150.0 nM
Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor kappa 1 expressed in CHO cell membrane None 260.0 nM
Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor mu 1 using [3H]- DAMGO as radioligand Cavia porcellus 3.467 nM
Binding affinity determined against Opioid receptor delta 1 from human cloned receptor None 299.0 nM
In vitro potency was measured against human Opioid receptor delta 1 None 150.0 nM
Activity was evaluated by inhibition of the binding of 1 nM [3H]U-69593 at Opioid receptor kappa 1 binding site Cavia porcellus 330.0 nM
Evaluated for the binding affinity at kappa receptor None 301.0 nM
Inhibition of [3H]-DAMGO binding to Opioid receptor mu 1 of Chinese hamster ovary membrane Cricetulus griseus 0.88 nM
Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor delta 1 expressed in CHO cell membrane;Range is between (63-360) None 150.0 nM
Evaluated for inhibitory activity against Opioid receptor delta 1 of mouse vas deferens (MVD). None 736.0 nM
Binding affinity against Opioid receptor kappa 1 isolated from rat brain membrane was determined using [3H]U-69593 as radioligand None 113.0 nM
Inhibition of [3H]naloxone binding to opiate receptor from rat neural membranes after incubation at 20 nM concentration at 37 degree C None 2.0 %
Opioid receptor activity was evaluated using guinea pig ileum (GPI) assay Cavia porcellus 54.7 nM
Compound was tested for irreversible antagonistic activity against opioid receptor in electrically stimulated longitudinal muscle of guinea pig ileum Cavia porcellus 29.0 nM
In vitro opioid inhibitory activity against in guinea pig ileum Cavia porcellus 65.0 nM
Inhibition of [3H]- U69,593 binding to Guinea pig Opioid receptor kappa 1 Cavia porcellus 271.0 nM
Inhibition of 9 (2 nM) binding to Opioid receptor kappa 1 of rat brain homogenate Rattus norvegicus 27.0 nM
Evaluated the ability to protect against the irreversible antagonism of morphines effects by beta-FNA in guinea pig ileal longitudinal muscle. Cavia porcellus 24.0 nM
In vitro inhibitory activity against opioid receptor in Guinea pig ileum Cavia porcellus 28.0 nM
Inhibitory potency against delta Opioid receptor delta 1 in longitudinal muscle preparation of mouse vas deferens Mus musculus 390.0 nM
Evaluated for the inhibition of [3H]EKC binding to Opioid receptor kappa 1 of guinea pig brain Cavia porcellus 530.0 nM
Inhibition of [3H]U-69593 radioligand binding to Guinea pig opioid receptor kappa 1. Cavia porcellus 1.82 nM
Binding affinity towards Opioid receptor kappa 1 was determined None 86.0 nM
Binding affinity for Opioid receptor kappa 1 was determined. None 52.14 nM
Binding affinity towards opioid receptor kappa 2 Bos taurus 33.0 nM
Opioid receptor activity was evaluated using mouse vas deferens (MVD) assay Mus musculus 258.0 nM
Inhibition of opioid receptor mu in guinea pig ileum (GPI) Cavia porcellus 38.0 nM
Affinity for opioid receptor mu sites Cavia porcellus 3.3 nM
Displacement of [3H]DAGO from mu opioid receptors in guinea pig brain (minus cerebellum). Cavia porcellus 3.3 nM
Receptor binding affinity towards opioid receptor mu Cavia porcellus 3.3 nM
Binding affinity against Opioid receptor kappa 1 in guinea pig brain membranes Cavia porcellus 110.0 nM
Binding affinity at Opioid receptor kappa 1 by displacement of [3H]U-69593 in guinea pig brain membranes Cavia porcellus 188.0 nM
Binding affinity for the Opioid receptor kappa 1 Cavia porcellus 86.0 nM
Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig Cavia porcellus 151.0 nM
Opioid receptor activity in terms of inhibition of [3H]dihydromorphine binding in rat brain membrane None 1.6 nM
Affinity for opioid receptor delta sites Cavia porcellus 456.0 nM
Compound was evaluated for its binding affinity against opioid receptor delta subtype in guinea pig brain (minus cerebellum) using [3H]-DADLE as radioligand. Cavia porcellus 460.0 nM
Receptor binding affinity towards opioid receptor delta Cavia porcellus 456.0 nM
Binding affinity to displace radioligand [3H]U-69593 on Opioid receptor kappa 1 in guinea pig membranes. Cavia porcellus 24.0 nM
Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand. Cavia porcellus 69.1 nM
Binding affinity towards guinea pig Opioid receptor kappa 1 using radioligand [3H]U-69593 Cavia porcellus 24.0 nM
Binding affinity towards opioid receptor kappa 1 Cavia porcellus 49.0 nM
Binding affinity to Opioid receptor kappa 1 in guinea pig cortex using [3H]EKC as radioligand Cavia porcellus 167.0 nM
Displacement of [3H]- DAGO from opioid receptor mu in rat brain membrane Rattus norvegicus 3.9 nM
Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane Rattus norvegicus 205.0 nM
Activity was evaluated by inhibition of the binding of 0.8 nM [3H]- DAMGO at Opioid receptor mu 1 binding site None 0.9 nM
Binding affinity towards opioid receptor mu 1 None 0.5 nM
Activity was evaluated by inhibition of the binding of 1 nM [3H]DPDPE at Opioid receptor delta 1 binding site Cavia porcellus 132.0 nM
Binding affinity towards Opioid receptor delta 1 Bos taurus 280.0 nM
Inhibition of [3H]- DADLE binding to Rat brain Opioid receptor delta 1 Rattus norvegicus 684.0 nM
Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1. None 7.37 nM Inhibition of [3H]DADLE radioligand binding to rat brain opioid receptor delta 1. None 684.0 nM
Evaluated for the inhibition of [3H]DADLE binding to Opioid receptor delta 1 of guinea pig brain Cavia porcellus 185.0 nM
Inhibition of [3H]DSLET binding to delta 1 opioid receptors in rat brain membranes None 280.0 nM
Binding affinity at opioid receptor delta 1 by displacement of [3H]DADLE in rat brain membrane None 157.0 nM
Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain None 90.0 nM
Binding affinity against Opioid receptor delta 1 isolated from rat brain membrane was determined using [3H][Ile]-deltorphin as radioligand None 217.0 nM
Ability to induce 50% of maximal effect in guinea pig ileum expressing Opioid receptor mu 1 Cavia porcellus 77.0 nM
Evaluated for inhibitory activity against Opioid receptor mu 1 of guinea pig ileum (GPI) Cavia porcellus 71.6 nM
Binding affinities against Opioid receptor delta 1 of guinea pig brain membrane using [3H]DPDPE as the radioligand using competition binding assays. Cavia porcellus 629.51 nM
Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes Cavia porcellus 710.0 nM
Binding affinity of compound was determined against Opioid receptor delta 1 from a native receptor in guinea pig Cavia porcellus 456.0 nM
Binding affinity towards Opioid receptor delta 1 using [3H]DADLE as radioligand. None 684.0 nM
Inhibition of [3H]DPDPE radioligand binding to rat opioid receptor delta 1 site from rat brain membranes None 90.0 nM
In vitro binding affinity at opioid receptor delta 1 was determined in C6 rat glioma cells using [3H]Ile5,6 deltorphin II None 217.0 nM
Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor kappa 1 using [3H]- U-69,593 as radioligand Cavia porcellus 467.74 nM
Inhibitory potency against Opioid receptor mu 1 in longitudinal muscle preparation of guinea pig ileum Cavia porcellus 70.0 nM
Inhibition of electrically evoked contraction of guinea pig ileum (myenteric plexus:longitudinal muscle preparation) by antagonist action at mu 1 opioid receptors Cavia porcellus 70.0 nM
Binding affinity against Opioid receptor delta 1 was determined in brain membrane preparations from male Hartley guinea-pigs Cavia porcellus 510.0 nM
Binding affinity to displace radioligand [3H]naltrindole on Opioid receptor delta 1 in guinea pig membranes. Cavia porcellus 140.0 nM
Binding affinity towards Opioid receptor delta 1 of guinea pig brain membranes using radioligand 0.2 nM [3H]Naltrindole Cavia porcellus 140.0 nM
Inhibition of binding of [3H]-DPDPE to opioid receptor delta 1 from rat brain membrane. None 90.0 nM
Inhibition of [3H]-[D-Pen2, D-Pen5]-enkephalin (2 nM) to Opioid receptor delta 1 of male Sprague-Dawley rat brain homogenate Rattus norvegicus 15.0 nM
Inhibition of [3H]U-69593 binding to Opioid receptor kappa 1 of Chinese hamster ovary membrane Cricetulus griseus 24.0 nM
In vivo binding affinity against delta Opioid receptor was measured by using labeled ligand [3H]DADLE (1 nM) with 4 nM sufentanil Cavia porcellus 375.0 nM
Binding affinity using guinea pig brain membrane preparations, towards Opioid receptor delta 1 using [3H]DPDPE as radioligand Cavia porcellus 416.87 nM
Binding affinity for Opioid receptor delta 1 was determined None 113.3 nM
Inhibition of Opioid receptors with [3H]naloxone binding in the absence of NaCl Cavia porcellus 10.0 nM
Inhibition of Opioid receptors binding by inhibiting specific [3H]naloxone binding by 50% in the presence of 100 mM NaCl Cavia porcellus 250.0 nM
Concentration required to inhibit [3H]naltrexone binding to Opioid receptors None 27.0 nM
Displacement of [3H]naloxone from rat brain Opioid receptors Rattus norvegicus 22.0 nM
Tested for In vitro binding constant for Opioid receptors by measuring the inhibition of stereospecific binding of [3H]naloxone in rat brain homogenates None 11.0 nM
Displacement of [3H]nalotrexone from rat-brain Opioid receptors Rattus norvegicus 27.0 nM
Displacement [3H]naloxone from rat-brain Opioid receptors Rattus norvegicus 4.2 nM
Compound was tested for its binding affinity towards Opioid receptors using [3H]naloxone from rat whole brain None 32.5 nM
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells None 2.0 %
In vitro binding affinity against cloned human Opioid receptor mu 1 expressed in HEK 293S cells None 0.57 nM
Binding affinity determined against Opioid receptor mu 1 from human cloned receptor None 3.0 nM
In vitro potency was measured against human Opioid receptor mu 1 None 17.0 nM
Inhibition of binding of [3H]diprenorphine to cloned human Opioid receptor mu 1 expressed in CHO cell membrane;Range is in between (6.8-43) None 17.0 nM
Inhibition of [3H]- DAMGO binding to Rat brain Opioid receptor mu 1 Rattus norvegicus 1.94 nM
Inhibition of [3H]DAMGO radioligand binding to rat brain opioid receptor mu 1. None 0.14 nM Inhibition of [3H]DAMGO radioligand binding to rat brain opioid receptor mu 1. None 1.94 nM
Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. None 2.1 nM
Inhibition of [3H]DAGO binding to mu 1 opioid receptor in rat brain membranes None 2.15 nM
Binding affinity at Opioid receptor mu 1 by displacement of [3H]DAMGO in rat brain membrane None 11.0 nM
Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes None 1.0 nM
Binding affinity against Opioid receptor mu 1 isolated from rat brain membrane was determined using [3H]DAMGO as radioligand None 6.55 nM
Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand. None 8.14 nM
Binding affinity by inhibition of [3H]DAMGO binding to Opioid receptor mu 1 from rat brain membranes None 1.8 nM
Binding affinity to Opioid receptor mu 1 in rat brain using [3H]-NAL as radioligand None 5.7 nM
Inhibition of [3H]DAMGO binding to rat brain homogenat Opioid receptor mu 1 Rattus norvegicus 2.8 nM
In vitro binding affinity at opioid receptor mu 1 was determined in C6 rat glioma cells using [3H]DAMGO None 6.55 nM
Inhibition of binding of [3H]DAMGO to opioid receptor mu 1 from rat brain membrane. None 1.8 nM
mu-1 receptor binding affinity in rat brain by 3H [d-Ala2, d-Leu5] enkephalin displacement. None 0.78 nM
Binding affinity for Opioid receptor mu 1 Homo sapiens 3.96 nM
Binding affinity towards mu opioid receptor was determined None 1.8 nM
Binding affinity towards opioid receptor mu 2 Bos taurus 2.5 nM
mu-2 receptor binding affinity in rat brain by 3H [d-Ala2, (N-Me)Phe4, Gly5-ol] enkephalin displacement. Rattus norvegicus 4.8 nM
Ability to displace 50% of (-)-naloxone (1.0) in mouse brain homogenate Rattus norvegicus 200.0 nM
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM Cavia porcellus 5.3 %
Compound was evaluated for the binding affinity to delta opioid receptor None 51.0 nM
Antinociceptive activity determined in vivo in tail flick assay in male Swiss mice with 2.0 mg/kg Naloxone Mus musculus 0.09 nM
% maximum inhibition is elicited when the response reaches plateau, calculated regarding electrically induced contraction in guinea pig ileum as 100% Cavia porcellus 87.2 %
Relative inhibitory activity expressed as the percentage of the maximum inhibition by the compound against that of morphine Cavia porcellus 100.0 %
Binding affinity against mu opioid receptor in guinea pig brain membranes Cavia porcellus 6.51 nM
Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor None 21.3 nM
Binding affinity for mu opioid receptor was evaluated by displacing [3H]- diprenorphine Rattus norvegicus 36.0 nM
Compound was evaluated for the binding affinity to mu opioid receptor None 38.0 nM
Evaluated for the inhibition of [3H]DAGO binding to mu-receptor of guinea pig brain Cavia porcellus 4.0 nM
Inhibition of [3H]naloxone binding to rat brain membrane with 100 mM NaCl. None 73.0 nM
Inhibition of [3H]-Naloxone binding to rat brain membrane without NaCl None 4.5 nM
Ability to inhibit electrically evoked contractions of isolated muscle preparations of mouse vas deference (MVD, delta receptor) None 644.0 nM
Ability to inhibit electrically evoked contractions of isolated muscle preparations of guinea pig ileum (GPI, mu receptor) Cavia porcellus 58.8 nM
Binding affinity for rat brain opioid receptor mu 1 Rattus norvegicus 6.55 nM
Binding affinity for rat brain opioid receptor delta 1 Rattus norvegicus 217.0 nM
Binding affinity against mu opioid receptor in mouse hot plate test Mus musculus 1.8 nM
Binding affinity against delta opioid receptor in mouse hot plate test Mus musculus 90.0 nM
Displacement of [3H]DAMGO from mu opioid receptor of rat brain membranes Rattus norvegicus 6.55 nM
Displacement of [3H]U-69593 from kappa opioid receptor of rat brain membranes Rattus norvegicus 113.0 nM
Inhibition of [3H]DAMGO binding to opioid receptor mu from rat brain membranes Rattus norvegicus 6.55 nM
Inhibition of [3H]U-69593 binding to opioid receptor kappa from guinea pig brain membranes Cavia porcellus 113.0 nM
Displacement of [3H[Ile5,6]-deltorphin II from delta opioid receptor of rat brain membranes Rattus norvegicus 217.0 nM
Inhibition of [3H][Ile5,6]deltorphin II binding to opioid receptor delta from rat brain membranes Rattus norvegicus 217.0 nM
Stimulation of [35S]GTP-gamma-S, binding at Opioid receptor mu 1 None 15.6
In vitro agonistic activity against opioid receptor mu of guinea pig ileum Cavia porcellus 311.0 nM
Inhibition of isolated guinea pig ileum contraction induced by electrical stimulation Cavia porcellus 127.4 nM
Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells Homo sapiens 0.88 nM
Displacement of [3H]naltrindole from human delta opioid receptor expressed in CHO cells Homo sapiens 140.0 nM
Displacement of [3H]U69593 from human kappa opioid receptor expressed in CHO cells Homo sapiens 24.0 nM
Displacement of radiolabeled DAMGO from mu opioid receptor in Hartley guinea pig brain Cavia porcellus 2.5 nM
Displacement of radiolabeled DPDPE-Cl from delta opioid receptor in Hartley guinea pig brain Cavia porcellus 58.0 nM
Displacement of radiolabeled U69593 from kappa1 opioid receptor in Hartley guinea pig brain Cavia porcellus 33.9 nM
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain Cavia porcellus 13.9 nM
Displacement of [3H]DAMGO from human recombinant MOR expressed in CHO cells Homo sapiens 1.1 nM
Displacement of [3H]Cl-DPDPE from human recombinant DOR expressed in CHO cells Homo sapiens 140.0 nM
Displacement of [3H]U-69593 from human recombinant KOR expressed in CHO cells Homo sapiens 46.9 nM
Stimulation of [35S]GTPgammaS binding to human recombinant MOR Homo sapiens 15.6 nM
Stimulation of [35S]GTP-gamma-S binding to human recombinant DOR Homo sapiens 316.0 nM
Stimulation of [35S]GTP-gamma-S binding to human recombinant KOR Homo sapiens 484.0 nM
Displacement of [3H]DAMGO from human cloned mu opioid receptor Homo sapiens 1.1 nM
Displacement of [3H]U-69593 from human cloned kappa opioid receptor Homo sapiens 46.9 nM
Displacement of [3H]DPDPE from human cloned delta opioid receptor Homo sapiens 140.0 nM
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding Homo sapiens 15.6 nM
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding Homo sapiens 484.0 nM
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding Homo sapiens 316.0 nM
Analgesic activity in mouse assessed as inhibition of hind paw lick at 10 mg/kg, ip by hot plate test Mus musculus 50.7 %
Displacement of [3H]etorphine from opioid receptor in rat cerebrum Rattus norvegicus 23.6 nM
Displacement of 3.0 nM [3H]etorphine from opioid receptor in rat cerebrum Rattus norvegicus 142.0 nM
Agonist activity at mu opioid receptor in Swiss mouse vas deferens assessed as inhibition of electrically-stimulated twitch Mus musculus 395.0 nM
Activation of human mu opioid receptor expressed in HEK293a cells coexpressing YFP-labelled alphai1 and CFP-labelled beta-1-gamma-2 Gi subunits assessed as decrease in fluorescence resonance energy transfer signal at 10 uM Homo sapiens 6.4 nM
Activation of human mu opioid receptor expressed in HEK293a cells by [35S]GTP-gamma-S binding assay Homo sapiens 7.0 nM
Activation of human mu opioid receptor expressed in HEK293a cells co-expressing YFP-labelled alphai1 and CFP-labelled beta1gamma2 Gi subunits assessed as Gi protein activation by fluorescence resonance energy transfer Homo sapiens 6.0 nM
Displacement of [3H]naloxone from human mu poioid receptor expressed in HEK293 cells Homo sapiens 4.0 nM
Displacement of [3H]diprenorphine from recombinant mu opioid receptor expressed in C6 cells None 1.7 nM
Displacement of [3H]diprenorphine from recombinant delta opioid receptor expressed in C6 cells None 104.57 nM
Displacement of [3H]diprenorphine from recombinant kappa opioid receptor expressed in CHO cells None 65.5 nM
Antinociceptive activity in anaesthetized rat assessed as inhibition of noxious pinch-induced electromyograph response at 0.3 mg/kg, iv administered as bolus dose for 30 seconds and 0.3 mg/kg/hr, iv administered via infusion measured after 1 hr Rattus norvegicus 40.0 %
Displacement of [3H]DAMGO from mu opioid receptor in ICR mouse whole brain Mus musculus 1.27 nM
Displacement of [3H]DPDPE from delta opioid receptor in ICR mouse whole brain Mus musculus 500.0 nM
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum Cavia porcellus 500.0 nM
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy Homo sapiens 67.9 %
Agonist activity at kappa opioid receptor in ddy mouse vas deferens assessed as inhibition of electric stimulation-induced contraction Mus musculus 145.1 nM
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Homo sapiens 15.6 nM
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Homo sapiens 316.0 nM
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding Homo sapiens 484.0 nM
Displacement of [3H]naloxone from opioid receptor in Sprague-Dawley rat striatal membrane by scintillation spectrophotometry Rattus norvegicus 2.0 nM
Displacement of [3H]DAMGO form mu opioid receptor in guinea pig brain Cavia porcellus 0.88 nM
Displacement of [3H]Naltrindole form delta opioid receptor in guinea pig brain Cavia porcellus 140.0 nM
Displacement of [3H]U69593 form kappa opioid receptor in guinea pig brain Cavia porcellus 24.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in mouse whole brain without cerebellum Mus musculus 1.271 nM
Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig cerebellum Cavia porcellus 213.1 nM
Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells Homo sapiens 2.55 nM
Displacement of [3H]diprenorphine from human kappa receptor expressed in CHO cells by scintillation counting Homo sapiens 6.9 nM
Displacement of [3H]diprenorphine from rat mu receptor expressed in CHO cells by scintillation counting Rattus norvegicus 116.8 nM
Displacement of [3H]diprenorphine from rat delta receptor expressed in CHO cells by scintillation counting Rattus norvegicus 76.9 nM
Agonist activity at rat mu opioid receptor assessed as stimulation of [35]SGTPgammaS binding Rattus norvegicus 123.5 nM
Displacement of [3H]DAMGO from mu opioid receptor from Wistar rat brain by liquid scintillation counting Rattus norvegicus 5.64 nM
Displacement of [3H]deltorphin-2 from delta opioid receptor from Wistar rat brain by liquid scintillation counting Rattus norvegicus 404.0 nM
Agonist activity at mu opioid receptor in Swiss albino mouse ileum assessed as inhibition of electrically-stimulated muscle contraction Mus musculus 85.5 nM
Binding affinity to kappa opioid receptor None 33.7 nM
Binding affinity to MOR/alpha2A adrenergic receptor heterodimer expressed in HEK293 cells coexpressing Gi protein assessed as inhibition of norepinephrine-induced Gi protein FRET signal None 25.0 %
Inhibition of MOR/alpha2A adrenergic receptor heterodimer expressed in HEK293 cells assessed as stimulation of ERK1/2 phosphorylation None 3.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in Sprague-Dawley rat brain membrane by liquid scintillation counting Rattus norvegicus 6.55 nM
Displacement of [3H][Ile5,6]deltorphin 2 from delta opioid receptor in Sprague-Dawley rat brain membrane by liquid scintillation counting Rattus norvegicus 113.0 nM
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane by liquid scintillation counting Cavia porcellus 217.0 nM
Agonist activity at human delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins Homo sapiens 15.6 nM
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins Homo sapiens 316.0 nM
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins Homo sapiens 484.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes Cavia porcellus 2.2 nM
Displacement of [3H]DPDPE from delta opioid receptor in rat brain membranes Rattus norvegicus 1.8 nM
Displacement of [125I]-IBNtxA from MOR-1 expressed in CHO cells None 4.6 nM
Displacement of [125I]-IBNalA from MOR-1 expressed in CHO cells None 2.52 nM
Displacement of [125I]-IBOxyA from MOR-1 expressed in CHO cells None 1.92 nM
Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig forebrain homogenates Cavia porcellus 1.98 nM
Displacement of [3H]-NTI from delta opioid receptor in guinea pig forebrain homogenates Cavia porcellus 325.0 nM
Displacement of [3H]-U69593 from kappa opioid receptor in guinea pig cerebellum homogenates Cavia porcellus 54.3 nM
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum homogenate by scintillation counting Cavia porcellus 46.9 nM
Displacement of [3H]NTI from delta opioid receptor in guinea pig forebrain homogenate by scintillation counting Cavia porcellus 140.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig forebrain homogenate by scintillation counting Cavia porcellus 1.1 nM
Displacement of [125I]IOXY from human mu opioid receptor expressed in CHO cells coexpressing human recombinant MOR after 2 hrs by liquid scintillation counting Homo sapiens 2.55 nM
Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting Homo sapiens 2.6 nM
Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting Homo sapiens 2.6 nM
Displacement of [3H]-DADLE from human delta opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting Homo sapiens 605.0 nM
Displacement of [3H]-U69593 from human kappa opioid receptor expressed in CHO cells membrane after 2 hrs by liquid scintillation counting Homo sapiens 299.0 nM
Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK-293 cells by scintillation counting Homo sapiens 2.2 nM
Agonist activity at human mu opioid receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 1 hr by HTRF assay Homo sapiens 3.7 nM
Displacement of [3H]-DAMGO from human mu opioid receptor expressed in CHO cells after 60 mins by scintillation counting Homo sapiens 0.88 nM
Displacement of [3H]-U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting Homo sapiens 24.0 nM
Displacement of [3H]-naltrindole from human delta opioid receptor expressed in CHO cells after 3 hrs by scintillation counting Homo sapiens 140.0 nM
Displacement of [3H]DAMGO from mu-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay None 0.14 nM
Displacement of [3H]DPDPE from delta-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay None 295.0 nM
Displacement of [3H]diprenorphine from kappa-opioid receptor expressed in CHOK1 cells after overnight incubation by scintillation proximity assay None 13.3 nM
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins by cAMP EIA Homo sapiens 4.3 nM
Antinociceptive activity against formalin-induced pain in Mus musculus Swiss albino (mouse) assessed as inhibition of licking during second phase (15 to 30 min) at 10 mg/kg, ip administered 30 min before experimental session Mus musculus 100.0 %
Antinociceptive activity against formalin-induced pain in Mus musculus Swiss albino (mouse) assessed as inhibition of licking during first phase (0 to 5 min) at 10 mg/kg, ip administered 30 min before experimental session Mus musculus 100.0 %
Antinociceptive activity Swiss albino Mus musculus (mouse) assessed as inhibition of formalin-induced paw licking at 5 mg/kg, po administered 30 min prior to formalin-challenge measured from 15 to 30 min relative to control Mus musculus 100.0 %
Antinociceptive activity Swiss albino Mus musculus (mouse) assessed as inhibition of formalin-induced paw licking at 5 mg/kg, po administered 30 min prior to formalin-challenge measured up to 5 min relative to control Mus musculus 68.02 %
Displacement of [3H]diprenorphine from human KOR expressed in CHO cells after 1 hr by liquid scintillation counting analysis Homo sapiens 60.9 nM
Displacement of [3H]diprenorphine from rat MOR expressed in rat C6 cells after 1 hr by liquid scintillation counting analysis Rattus norvegicus 6.3 nM
Displacement of [3H]diprenorphine from rat DOR expressed in rat C6 cells after 1 hr by liquid scintillation counting analysis Rattus norvegicus 171.0 nM
Agonist activity at rat MOR expressed in rat C6 cells assessed as stimulation of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting analysis Rattus norvegicus 194.0 nM
Antinociceptive activity in Swiss mouse assessed as inhibition of formalin-induced paw licking at 5 mg/kg, sc administered 30 mins prior to formalin challenge measured during inflammatory phase for 20 to 25 mins Mus musculus 97.21 %
Antinociceptive activity in Swiss mouse assessed as inhibition of formalin-induced paw licking at 5 mg/kg, sc administered 30 mins prior to formalin challenge measured during neurogenic phase for 1 to 5 mins Mus musculus 94.0 %
Antinociceptive activity in Swiss mouse assessed as inhibition of acetic acid-induced abdominal writhing response at 5 mg/kg, ip administered 30 mins prior to acetic acid challenge measured for 10 to 20 mins Mus musculus 98.3 %
Displacement of [3H]U69,593 from human recombinant kappa opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis Homo sapiens 299.0 nM
Displacement of [3H]DADLE from human recombinant delta opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis Homo sapiens 605.0 nM
Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting analysis Homo sapiens 2.6 nM
Inhibition of gastrointestinal transit of charcoal meal in rat at 55.2 mg/kg, po Rattus norvegicus 70.0 %
Displacement of [3H]U-69593 from kappa opoid receptor in Dunkin-Hartley guinea pig brain after 1 hr by liquid scintillation spectrometry Cavia porcellus 468.0 nM
Displacement of [3H]DPDPE from delta opoid receptor in Dunkin-Hartley guinea pig brain after 2 hrs by liquid scintillation spectrometry Cavia porcellus 417.0 nM
Displacement of [3H]DAMGO from mu opoid receptor in Dunkin-Hartley guinea pig brain after 1.5 hrs by liquid scintillation spectrometry Cavia porcellus 3.5 nM
Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting Homo sapiens 299.0 nM
Displacement of [3H]DADLE from human delta opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting Homo sapiens 605.0 nM
Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cells after 2 hrs by liquid scintillation counting Homo sapiens 2.6 nM
Activation of mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to U69593 Mus musculus 71.0 %
Activation of mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to DAMGO Mus musculus 97.0 %
Activation of human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to U69593 Homo sapiens 90.0 %
Activation of human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to DPDPE Homo sapiens 69.0 %
Activation of human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay relative to DAMGO Homo sapiens 91.0 %
Agonist activity at mouse MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay Mus musculus 30.0 nM
Agonist activity at mouse KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay Mus musculus 400.0 nM
Agonist activity at human KOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay Homo sapiens 400.0 nM
Agonist activity at human MOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay Homo sapiens 50.0 nM
Agonist activity at human DOR assessed as inhibition of forskolin-stimulated cAMP accumulation after 30 mins by cell based TR-FRET assay Homo sapiens 500.0 nM
Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as beta-arrestin recruitment by chemiluminescence assay Homo sapiens 501.19 nM
Agonist activity at human mu opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation by fluorescence assay Homo sapiens 39.81 nM
Displacement of radiolabeled DAMGO from human recombinant mu opioid receptor expressed in OPRM1 cells Homo sapiens 2.5 nM
Displacement of [3H]U-69593 from kappa opioid receptor in CHO cells at 10 uM after 120 mins relative to control Cricetulus griseus 100.0 %
Displacement of [3H]U-69593 from kappa opioid receptor in CHO cells at 1 uM after 120 mins relative to control Cricetulus griseus 95.0 %
Displacement of [3H]DADLE from delta opioid receptor in CHO cells at 1 uM after 120 mins relative to control Cricetulus griseus 72.0 %
Displacement of [3H]DADLE from delta opioid receptor in CHO cells at 10 uM after 120 mins relative to control Cricetulus griseus 95.0 %
Displacement of [3H]diprenorphine from mu opioid receptor in HEK293 cells at 10 uM after 120 mins relative to control Homo sapiens 98.0 %
Displacement of [3H]diprenorphine from mu opioid receptor in HEK293 cells at 1 uM after 120 mins relative to control Homo sapiens 81.0 %
Displacement of radiolabeled dihydromorphine from opioid receptor in rat brain homogenates Rattus norvegicus 3.0 nM
Binding affinity to rat brain opioid receptor Rattus norvegicus 3.0 nM
Displacement of [3H]-naloxone from rat opioid receptor after 30 mins by liquid scintillation counting analysis in absence of NaCl Rattus norvegicus 10.0 nM
Displacement of [3H]-naloxone from rat opioid receptor after 30 mins by liquid scintillation counting analysis in presence of NaCl Rattus norvegicus 250.0 nM
Displacement of [3H]-naloxone from human mu opioid receptor expressed in CHO-K1 cells by scintillation counting analysis Homo sapiens 5.2 nM
Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes Rattus norvegicus 1.45 nM
Displacement of [3H]DSLET from delta opioid receptor in rat brain membranes Rattus norvegicus 82.5 nM
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membranes Cavia porcellus 28.1 nM
Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction Cavia porcellus 29.3 nM
Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction Mus musculus 155.0 nM
Agonist activity at human mu opioid receptor expressed CHO-K1 cells coexpressing Galpha15 assessed as induction of intracellular calcium release by FLIPR calcium assay Homo sapiens 10.0 nM
Stimulation of mouse MOR expressed in CHO cells after 1.5 hrs by [35S]GTPgammaS binding assay Mus musculus 120.0 nM
Displacement of [3H]DAMGO from human recombinant opioid mu receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method Homo sapiens 2.6 nM
Displacement of [3H]DADLE from human recombinant opioid delta receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method Homo sapiens 605.0 nM
Displacement of [3H]U69,593 from human recombinant opioid kappa receptor expressed in CHO cell membranes after 2 hrs by liquid scintillation counting method Homo sapiens 299.0 nM
Displacement of [3H]naloxone from MOR (unknown origin) expressed in human 293T cells Homo sapiens 22.0 nM
Displacement of [3H]-diprenorphine from opioid receptor in rat brain membrane homogenates after 1 hr by liquid scintillation counting Rattus norvegicus 2.6 nM
Displacement of [3H]-diprenorphine from zebrafish mu opioid receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting Danio rerio 187.4 nM
Displacement of [3H]-U-69593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting Cavia porcellus 35.0 nM
Displacement of [3H]-DAMGO from mu opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting Cavia porcellus 3.9 nM
Displacement of [3H]-DPDPE from delta opioid receptor in rat brain membrane after 120 mins by scintillation counting Rattus norvegicus 2.0 nM
Agonist activity at human MOR expressed in CHO cells assessed as induction of membrane potential change measured every 3 secs for 30 secs by fluorescent membrane potential assay Homo sapiens 6.3 nM
Binding affinity to human mu opioid receptor Homo sapiens 0.53 nM
Binding affinity to human kappa opioid receptor Homo sapiens 120.0 nM
Displacement of [3H]naloxone from human mu opioid receptor expressed in CHO-K1 cells after 150 mins by liquid scintillation counting method Homo sapiens 5.2 nM
null: The Ki (binding affinity) for u opioid receptors was determined using a competitive displacement assay as previously described in Neumeyer (Journal of Med. Chem. 2012, p 3878), which is incorporated herein in its entirety. Briefly, membrane protein from CHO (Chinese Hamster Ovarian) cells that stably expressed the cloned human u opioid receptor were incubated with 12 different concentrations of the compound set forth herein in the presence of 0.25 nM [3H]DAMGO (see Tiberi et al., Can. J. Physiol. Pharmacol. 1988, Vol. 66, p 1368, which is incorporated by reference herein in its entirety) in a final volume of 1 mL of 50 mM Tris-HCl, pH 7.5 at 25° C. Incubation times of 60 min were used for [3H]DAMGO (see Gulati et al., Life Sci. 1990, Vol. 47, p 159, which is incorporated by reference herein in its entirety). Nonspecific binding was measured by inclusion of 10 uM naloxone. The binding was terminated by filtering the samples through Schleicher & Schuell No. 32 glass fiber. Homo sapiens 0.32 nM
Functional Assay (GTPgammaS Binding): The EC50 and Imax for mu opioid receptors was determined using a [I35S]GTPgammaS binding assay. This assay measures the functional properties of a compound by quantifying the level of G-protein activation following agonist binding in studies using stably transfected cells, and is considered to be a measure of the efficacy of a compound. Membranes from CHO (Chinese Hamster Ovary) cells that stably expressed the cloned human Mu opioid receptor were used in the experiments. Specifically, in a final volume of 0.5 mL, 12 different concentrations of each test compound were incubated with 7.5 ug of CHO cell membranes that stably expressed the human mu opioid receptor. The assay buffer consisted of 50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, 3 uM GDP, and 100 mM NaCl. The final concentration of [35S]GTPgammaS was 0.080 nM. Nonspecific binding was measured by inclusion of 10 uM GTPgammaS. Binding was initiated by the addition of the membranes. Homo sapiens 34.0 nM
Displacement of [3H]DPN from zebrafish mu opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method Danio rerio 187.0 nM
Displacement of [3H]DPN from zebrafish delta 1a opioid receptor expressed in HEK293 cell membranes after 1 hr by scintillation counting method Danio rerio 223.0 nM
Displacement of [3H]DAMGO from mu-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting Cavia porcellus 5.2 nM
Displacement of [3H]DPDPE from delta-type opioid receptor in guinea pig brain membranes after 120 mins by solid scintillation counting Cavia porcellus 2.0 nM
Displacement of [125I]BNtxA from mouse MOR expressed in CHO cell membranes after 90 mins by filter binding assay Mus musculus 4.6 nM
Antinociceptive activity in Kunming mouse assessed as inhibition of acetic acid-induced writhes at 0.8 mg/kg, ip pretreated for 15 mins followed by acetic acid challenge measured for 30 mins relative to control Mus musculus 86.0 %
Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method Homo sapiens 61.0 %
Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method Homo sapiens 85.0 %
Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method Homo sapiens 31.0 %
Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method Homo sapiens 63.0 %
Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 1 uM incubated for 1 hr by scintillation counting method Homo sapiens 42.0 %
Displacement of [3H]diprenorphine from human KOR expressed in African green monkey COS1 cell membranes at 10 uM incubated for 1 hr by scintillation counting method Homo sapiens 80.0 %
Displacement of [3H]diprenorphine from human MOR expressed in African green monkey COS1 cell membranes incubated for 1 hr by scintillation counting method Homo sapiens 4.0 nM
Displacement of [3H]diprenorphine from human DOR expressed in African green monkey COS1 cell membranes incubated for 1 hr by scintillation counting method Homo sapiens 340.0 nM
Displacement of [3H]U-69,593 from kappa opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis Cavia porcellus 35.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis Cavia porcellus 3.9 nM
Displacement of [3H]DPDPE from delta opioid receptor in Sprague-Dawley rat brain membranes after 120 mins by scintillation counting analysis Rattus norvegicus 2.0 nM
Agonist activity at human mu opioid receptor expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by scintillation counting method Homo sapiens 64.0 nM
Agonist activity at human mu opioid receptor expressed in human USOS-beta-arrestin-hMOR-PathHunter cells incubated for 90 mins by beta-arrestin-2 enzyme fragment complementation assay Homo sapiens 379.0 nM
Agonist activity at rat MOR expressed in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting Rattus norvegicus 123.5 nM
Displacement of [3H]DAMGO from MOR in guinea pig brain membranes after 120 mins by scintillation counting method Cavia porcellus 5.2 nM
Displacement of [3H]diprenorphine from human MOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay Homo sapiens 4.2 nM
Displacement of [3H]diprenorphine from human DOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay Homo sapiens 104.1 nM
Displacement of [3H]diprenorphine from human KOR expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting assay Homo sapiens 36.8 nM
Agonist activity at human MOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay Homo sapiens 147.0 nM
Agonist activity at human DOR expressed in CHO cell membranes assessed as stimulation of [35S]-GTPgammaS binding incubated for 1 hr by by liquid scintillation counting assay Homo sapiens 593.0 nM
Displacement of [3H]-diprenorphine from rat mu-type opioid receptor expressed in rat C6 cell membranes incubated for 1 hr by liquid scintillation counting method Rattus norvegicus 6.3 nM
Displacement of [3H]-diprenorphine from rat delta-type opioid receptor expressed in rat C6 cell membranes incubated for 1 hr by liquid scintillation counting method Rattus norvegicus 171.0 nM
Displacement of [3H]-diprenorphine from human kappa-type opioid receptor expressed in CHO cell membranes incubated for 1 hr by liquid scintillation counting method Homo sapiens 61.0 nM
Agonist activity at rat Mu-type opioid receptor expressed in rat C6 cell membranes assessed as stimulation of [35S]GTPgammaS binding incubated for 1 hr by liquid scintillation counting method Rattus norvegicus 194.0 nM
Displacement of [3H]DAMGO from mu opioid receptor in guinea pig brain membranes after 120 mins by scintillation counting analysis Cavia porcellus 3.9 nM
Displacement of [3H]DPDPE from delta opioid receptor in rat membranes after 120 mins by scintillation counting analysis Rattus norvegicus 2.0 nM
Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig brain membrane after 120 mins by scintillation counting analysis Cavia porcellus 35.0 nM
Displacement of [3H]-diprenorphine from MOR (unknown origin) Homo sapiens 410.0 nM
Displacement of [3H]-DAMGO from full length human MOR expressed in chem5 cells incubated for 60 mins by liquid scintillation counter Homo sapiens 6.08 nM
Inhibition of mu opioid receptor in guinea pig brain membranes Cavia porcellus 3.5 nM
Displacement of [3H]-diprenorphin from human mu opioid receptor incubated for 1 hr Homo sapiens 410.0 nM
Agonist activity at human MOR expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation by EIA method Homo sapiens 4.3 nM
Displacement of [3H] dihydromorphine from guinea pig brain opioid receptor Cavia porcellus 1.0 nM
Agonist activity at human MOR expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by luminescence assay Homo sapiens 4.7 nM
Activity at human MOR expressed in CHOK1 cells co-expressing beta-arrestin2 EFC assessed as beta-arrestin2 EFC recruitment measured after 90 mins by PathHunter assay Homo sapiens 379.6 nM
Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay Homo sapiens 5.0 nM
Agonist activity at human kappa opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay Homo sapiens 330.0 nM
Agonist activity at human delta opiod receptor expressed in CHO-K1 cells assessed as increase in forskolin induced cAMP production measured after 30 mins by HitHunter luminescence based assay Homo sapiens 780.0 nM
Agonist activity at human mu opiod receptor expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay Homo sapiens 380.0 nM
Antinociceptive activity in male B6-SJL mouse administered subcutaneously daily for 9 days and measured on day 9 by warm water tail-flick assay Mus musculus 11.6 mg kg-1
Agonist activity at human delta opioid receptor assessed as inhibition of forskolin-induced cAMP accumulation Homo sapiens 79.12 nM
Agonist activity at human mu opioid receptor assessed as inhibition of forskolin-induced cAMP accumulation Homo sapiens 203.97 nM
Displacement of [3H]DAMGO from human recombinant mu opioid receptor expressed in HEK293 cells incubated for 120 mins by radiometric scintillation analysis Homo sapiens 4.19 nM
Displacement of [3H]DAMGO from rat mu opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method Rattus norvegicus 6.9 nM
Displacement of [3H]DPDPE from rat delta opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method Rattus norvegicus 116.8 nM
Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membrane measured after 30 mins by liquid scintillation counting method Homo sapiens 76.9 nM
Agonist activity at rat mu opioid receptor expressed in CHO cell membrane incubated for 1 hr by [35S]GTPgammaS binding based liquid scintillation counting method Rattus norvegicus 123.5 nM
Agonist activity at MOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay Homo sapiens 71.6 nM Agonist activity at MOR (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay Homo sapiens 70.79 nM
Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Nb33 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay Homo sapiens 416.87 nM
Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay Homo sapiens 8.71 nM
Agonist activity at human mu opioid receptor expressed in HEK293T cells assessed as arrestin-3 recruitment preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay Homo sapiens 79.43 nM

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Resources Reference
ChEBI 17303
ChEMBL CHEMBL70
DrugBank DB00295
DrugCentral 1845
FDA SRS 76I7G6D29C
Human Metabolome Database HMDB0014440
Guide to Pharmacology 1627
KEGG C01516
PDB MOI
PharmGKB PA450550
PubChem 5288826
SureChEMBL SCHEMBL2997
ZINC ZINC000003812983
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