| Identification | Back Directory | [Name]
SR 146131 | [CAS]
221671-61-0 | [Synonyms]
SR 146131
NFDFTMICKVDYLQ-UHFFFAOYSA-N
1H-Indole-1-acetic acid, 2-[[[4-(4-chloro-2,5-dimethoxyphenyl)-5-(2-cyclohexylethyl)-2-thiazolyl]amino]carbonyl]-5,7-dimethyl- | [Molecular Formula]
C32H36ClN3O5S | [MDL Number]
MFCD09970590 | [MOL File]
221671-61-0.mol | [Molecular Weight]
610.16 |
| Chemical Properties | Back Directory | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
4.01±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist. | [in vivo]
SR 146131 completely inhibits gastric and gallbladder emptying in mice (ED50 of 66 and 2.7 μg/kg p.o., respectively). SR 146131 dose dependently reduces food intake in fasted rats (from 0.1 mg/kg p.o.), in nonfasted rats in which food intake has been highly stimulated by the administration of neuropeptide Y (1–36) (from 0.3 mg/kg p.o.), in fasted gerbils (from 0.1 mg/kg p.o.), and in marmosets maintained on a restricted diet (from 3 mg/kg p.o.). SR 146131 (10 mg/kg p.o.) also increases the number of Fos-positive cells in the hypothalamic paraventricular nucleus of rats. Locomotor activity of mice is reduced by orally administered SR 146131 (from 0.3 mg/kg p.o.)[1]. | [IC 50]
CCKAR | [References]
[1] Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies. J Pharmacol Exp Ther. 1999 May;289(2):742-51. PMID:10215648
[2] Bignon E, et al. SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization. J Pharmacol Exp Ther. 1999 May;289(2):752-61. PMID:10215649 |
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