|
Compound was evaluated for the inhibition of gastrin-stimulated gastric acid secretion in conscious heidenhain pouch dogs when administered 1 mg/kg perorally
|
Canis lupus familiaris
|
53.0
%
|
|
|
Evaluated against tetragastrin stimulated gastric acid secretion in conscious Hiedenhain-pouch dogs at a dose of 22 mg/kg, po
|
Canis lupus familiaris
|
22.0
%
|
|
|
Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 1uM/Kg, on iv administration of the compound
|
Canis lupus familiaris
|
1.7
%
|
|
|
Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 4uM/Kg, on iv administration of the compound
|
Canis lupus familiaris
|
8.5
%
|
|
|
Maximum percent inhibition of acid output in penta gastrin-stimulated Heidenhain pouch dogs at a dose of 10 mg/kg, given intravenously (iv).
|
Canis lupus familiaris
|
1.02
%
|
|
|
Inhibition of histamine stimulated chronotropic response in isolated guinea pig right atrium (1*10e-6 g/mL)
|
Cavia porcellus
|
43.0
%
|
|
|
Inhibition of histamine-stimulated chronotropic response in the isolated guinea pig right atrium at 1*10e-6 g/mL
|
Cavia porcellus
|
43.0
%
|
|
|
inhibition of the histamine stimulated chronic response in the isolated guinea pig right atrium at 1x 10 e-6 g/mL
|
Cavia porcellus
|
43.0
%
|
|
|
Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium
|
Cavia porcellus
|
501.19
nM
|
|
|
In vitro inhibition of Histamine H2 receptor by measuring its ability to block the histamine-stimulated adenylate cyclase of guinea pig hippocampal homogenate
|
Cavia porcellus
|
501.19
nM
|
|
|
Histamine H2 receptor antagonistic activity
|
Cavia porcellus
|
3.7
ug.mL-1
|
|
|
H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium at 1x10E-6 g/mL.
|
Cavia porcellus
|
43.0
%
|
|
|
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.0
|
Cavia porcellus
|
954.99
nM
|
|
|
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.4
|
Cavia porcellus
|
398.11
nM
|
|
|
Antagonistic activity against Histamine H2 receptor expressed as the charge of receptor sensitivity was determined at pH 7.8
|
Cavia porcellus
|
371.54
nM
|
|
|
In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria.
|
Cavia porcellus
|
263.03
nM
|
|
|
Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes.
|
Cavia porcellus
|
302.0
nM
|
|
|
Histamine H2 receptor antagonism in isolated guinea pig right atrium at concentration of 1*10e-6 g/mL of histamine hydrochloride
|
Cavia porcellus
|
43.0
%
|
|
|
Antagonistic activity for inhibition of histamine H2 receptor from anesthetized rats
|
None
|
251.19
nM
|
|
|
Antagonistic activity by inhibition histamine H2 receptor from rats.
|
None
|
251.19
nM
|
|
|
Percentage inhibition for muscarinic acetylcholine receptor at concentration 10 e-5M.
|
None
|
2.0
%
|
|
|
Percentage inhibition for muscarinic acetylcholine receptor at concentration 10e-6 M.
|
None
|
2.0
%
|
|
|
Inhibition of P-gp was determined using rhodamine-assay in human CaCo-2 cells
|
None
|
4.0
%
|
|
|
Antisecretory activity evaluated by the inhibition of 14C -AP uptake in isolated rabbit parietal cells stimulated by exogenous histamine
|
Oryctolagus cuniculus
|
820.0
nM
|
|
|
In vivo gastric antisecretory activity in acute fistula rats (12.5 mg/kg, id)
|
Rattus norvegicus
|
51.4
%
|
|
|
Compound was measured for percentage inhibition of aspirin-induced ulcers at 10 mg/kg after po administration
|
Rattus norvegicus
|
67.0
%
|
|
|
Percent inhibition of gastric antisecretory activity in the 4 hr pylorus-ligated rat to that of control at a dose of 100 mg/kg
|
Rattus norvegicus
|
80.6
%
|
|
|
Inhibition of histamine stimulated gastric acid secretion in lumen perfused stomach of anesthetized rats (1 mg/kg iv)
|
Rattus norvegicus
|
53.0
%
|
|
|
Inhibition of aspirin induced gastric lesions in rats after peroral dose of 32 mg/kg
|
Rattus norvegicus
|
33.0
%
|
|
|
Inhibition of histamine stimulated gastric acid secretion in lumen perfused anaesthetized rats after 1 mg/kg intravenous dose
|
Rattus norvegicus
|
53.0
%
|
|
|
In Vivo gastric Mucosal protective activity against gastric mucosal lesions induced by 0.6 N HCl in rats. (200 mg/kg, po)
|
Rattus norvegicus
|
-42.2
%
|
|
|
Gastric antisecretory activity at the dose of 100 mg/kg in pylorus lygated rats
|
Rattus norvegicus
|
80.6
%
|
|
|
Inhibition of histamine-stimulated gastric acid secretion in lumen-perfused stomach of the anaesthetized rats when administered 1 mg/kg intravenously
|
Rattus norvegicus
|
22.0
%
|
|
|
Inhibition of stress-induced ulcer formation in rats by 10 mg/kg p.o. administration.
|
Rattus norvegicus
|
33.0
%
|
|
|
The antiulcer activity against stress-induced ulcer in rats by 30 mg/kg peroral administration.
|
Rattus norvegicus
|
39.0
%
|
|
|
inhibition of histamine stimulated gastric secretion in lumen perfused stomach of anesthetized rats at 1 mg/kg intravenously
|
Rattus norvegicus
|
53.0
%
|
|
|
Inhibition of histamine stimulated gastric acid secretion in lumen perfused stomach of anesthetized rats at 1 mg/kg i.v. dose
|
Rattus norvegicus
|
53.0
%
|
|
|
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 10 uM
|
Cavia porcellus
|
0.0
%
|
|
|
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
|
4.1
%
|
|
|
Inhibition of histamine-stimulated chronotropic response in isolated guinea pig right atrium at 1*10e-6 g/mL
|
Cavia porcellus
|
43.0
%
|
|
|
Inhibition of histamine-stimulated gastric acid secretion in lumen-perfused stomach of anesthetized rats after 1 mg/kg iv administration
|
Rattus norvegicus
|
53.0
%
|
|
|
Inhibition of histamine H2 receptor
|
None
|
781.0
nM
|
|
|
Displacement of radiolabeled cimetidine from human histamine H2 receptor
|
Homo sapiens
|
180.0
nM
|
|
Displacement of radiolabeled cimetidine from human histamine H2 receptor
|
Homo sapiens
|
170.0
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
|
8.1
%
|
|
|
Inhibition of water-immersion stress-induced ulcer formation in rat at 30 mg/kg
|
Rattus norvegicus
|
74.0
%
|
|
|
TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in Xenopus laevis oocytes
|
Xenopus laevis
|
590.0
nM
|
|
|
TP_TRANSPORTER: inhibition of TEA uptake (TEA: 20 uM, Cimetidine: 5000 uM) in OCT3-expressing HRPE cells
|
None
|
90.0
%
|
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
40.3
%
|
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
24.8
%
|
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
-6.2
%
|
|
|
inhibition of human PAD4 preincubated at 10 uM for 15 mins before substrate addition measured after 20 mins by spectrophotometry
|
Homo sapiens
|
1.0
%
|
|
|
inhibition of human PAD4 preincubated at 1 uM for 15 mins before substrate addition measured after 20 mins by spectrophotometry
|
Homo sapiens
|
0.0
%
|
|
|
Binding affinity to human histamine H2 receptor by radioligand displacement assay
|
Homo sapiens
|
270.0
nM
|
|
|
Binding affinity to human histamine H2 receptor by radioligand displacement assay
|
Homo sapiens
|
140.0
nM
|
|
Binding affinity to human histamine H2 receptor by radioligand displacement assay
|
Homo sapiens
|
140.0
nM
|
|
|
Gastroprotective activity in Wistar rat assessed as inhibition of HCl/ethanol-induced gastric ulcer at 100 mg/kg, ip administered 30 mins prior to HCl/ethanol challenge measured after 1 hr relative to vehicle-treated control
|
Rattus norvegicus
|
74.03
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
120.2
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
96.42
%
|
|
|
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
|
Homo sapiens
|
70.79
nM
|
|
Displacement of [3H]Cimetidine from histamine H2 receptor (unknown origin)
|
Homo sapiens
|
70.0
nM
|
|
|
Antiulcer activity in albino rat pyloric ligation model assessed as inhibition of gastric volume at 100 mg/kg, po administered as single dose 1 hr prior ligation relative to control
|
Rattus norvegicus
|
14.0
%
|
|
|
Antiulcer activity in albino rat pyloric ligation model assessed as inhibition of total acid output at 100 mg/kg, po administered as single dose 1 hr prior ligation relative to control
|
Rattus norvegicus
|
37.0
%
|
|
|
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
|
Homo sapiens
|
500.0
nM
|
|
Displacement of [125I]APT from human recombinant histamine H2 receptor expressed in CHO cells after 120 mins by scintillation counting
|
Homo sapiens
|
490.0
nM
|
|
|
Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
|
Homo sapiens
|
4.13
%
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
12.6
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-4.2
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
3.14
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
12.46
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
19.7
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
3.16
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
2.1
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
-12.58
%
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
17.13
%
|
|
|
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
|
-0.07
%
|
|
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
|
-0.07
%
|
|
