221671-61-0
221671-61-0 structure
- Name: SR 146131
- Chemical Name: (2-{[4-(4-Chloro-2,5-dimethoxyphenyl)-5-(2-cyclohexylethyl)-1,3-t hiazol-2-yl]carbamoyl}-5,7-dimethyl-1H-indol-1-yl)acetic acid
- CAS Number: 221671-61-0
- Molecular Formula: C32H36ClN3O5S
- Molecular Weight: 610.16300
- Catalog: Signaling Pathways GPCR/G Protein Cholecystokinin Receptor
- Create Date: 2016-01-18 18:04:24
- Modify Date: 2024-01-12 23:55:01
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SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist.
| Name | (2-{[4-(4-Chloro-2,5-dimethoxyphenyl)-5-(2-cyclohexylethyl)-1,3-t hiazol-2-yl]carbamoyl}-5,7-dimethyl-1H-indol-1-yl)acetic acid |
|---|---|
| Synonyms |
SR 146131
MFCD09970590 |
| Description | SR 146131 is a potent, orally available, and selective nonpeptide (cholecystokinin 1) receptor agonist. |
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| Related Catalog | |
| Target |
Cholecystokinin 1 receptor[1] |
| In Vitro | SR 146131 inhibits in the binding of [125I]-BH-CCK-8S to CCK1sites on 3T3-hCCK1 cell membranes with an IC50 value of 0.56 ± 0.10 nM. At much higher concentrations, SR 146131 also inhibits the binding of radiolabeled CCK to CCK2sites in CHO-hCCK2 membranes with an IC50 of 162 ± 27 nM. SR 146131 is a potent CCK1 agonist on several intracellular events linked to CCK1 receptor activation in various cell types: on [Ca2+]i release and IP1 formation, SR 146131 appears as a full CCK1 receptor agonist in the 3T3-hCCK1 cells, but a partial CCK1receptor agonist on MAPK activation and early gene expression in this cell line. SR 146131 also acts as a partial agonist in the two neuroblastoma cell lines[1]. |
| 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]. |
| Cell Assay | 3T3-hCCK1 cells grown to subconfluence in 6-well cluster plates are washed with fresh medium. Twenty-four hours later, the cells are stimulated for 15 min with various concentrations of CCK-8S or SR 146131[1]. |
| Animal Admin | Rats[1] Male Sprague-Dawley rats are fasted for 18 h, and allowed access to food for only 6 h between 10 AM and 4 PM each day. Water is available ad libitum. At the end of this adaptation phase, rats are administered SR 146131 (0.03-3 mg/kg p.o.). One hour after SR 146131 administration, a weighed amount of food is introduced into the cage, and food intake is measured 1, 3, 6, and 23 h after SR 146131 administration[1]. Mice[1] SR 146131 (0.01-1 pg) is solubilized in DMSO (1 mg/mL), diluted to the required concentrations with water, and injected (in 1 μL) into one striatum in awake, hand-restrained female CD1 mice (25-30 g). After injection, the animals are placed individually in Plexiglas cages (10 × 10 × 15 cm). Turning behavior in mice is monitored[1]. |
| References |
| Molecular Formula | C32H36ClN3O5S |
|---|---|
| Molecular Weight | 610.16300 |
| Exact Mass | 609.20600 |
| PSA | 134.41000 |
| LogP | 8.28600 |