181629-93-6

181629-93-6 structure

Name: SB 228357
Chemical Name: N-(3-fluoro-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
CAS Number: 181629-93-6
Molecular Formula: C₂₂H₁₇F₄N₃O₂
Molecular Weight: 431.38300
Create Date: 2018-12-27 20:57:47
Modify Date: 2024-01-11 22:36:26
SB228357 is a selective, potent oral active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects[1][2].

Name	N-(3-fluoro-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
Synonyms	Tocris-1375 Lopac-S-2318

Description	SB228357 is a selective, potent oral active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects[1][2].
Target	5-HT2A Receptor:6.9 (pKi) 5-HT2C Receptor:9 (pKi) 5-HT2B Receptor:8 (pKi)
In Vivo	SB228357 (0-10 mg/kg; oral administration; for 90 minutes; male Sprague Dawley rats) treatment significantly reverses Haloperidol-induced catalepsy[2]. Animal Model: Male Sprague Dawley rats (200-250 g) injected with Haloperidol[2] Dosage: 0 mg/kg, 0.32 mg/kg, 1 mg/kg, 3.2 mg/kg, 10 mg/kg Administration: Oral administration; for 90 minutes Result: Significantly reversed Haloperidol-induced catalepsy.
References	[1]. Bromidge SM, et al. Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent. J Med Chem. 2000 Mar 23;43(6):1123-34. [2]. Reavill C, et al. Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist. Br J Pharmacol. 1999 Feb;126(3):572-4.

Safety Phrases	22-24/25
WGK Germany	3