CAS 181629-93-6|SB 228357

Introduction:Basic information about CAS 181629-93-6|SB 228357, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameSB 228357
CAS Number181629-93-6Molecular Weight431.38300
Density1.398g/cm3Boiling Point625.4ºC at 760mmHg
Molecular FormulaC22H17F4N3O2Melting Point/
MSDS/Flash Point332ºC

Names

NameN-(3-fluoro-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
SynonymMore Synonyms

SB 228357 BiologicalActivity

DescriptionSB228357 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 VivoSB228357 (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.

Chemical & Physical Properties

Density1.398g/cm3
Boiling Point625.4ºC at 760mmHg
Molecular FormulaC22H17F4N3O2
Molecular Weight431.38300
Flash Point332ºC
Exact Mass431.12600
PSA54.46000
LogP5.64770
Vapour Pressure1.48E-15mmHg at 25°C
Index of Refraction1.599
InChIKeyRRJLJKRFFRZRAF-UHFFFAOYSA-N
SMILESCOc1cc2c(cc1C(F)(F)F)N(C(=O)Nc1cc(F)cc(-c3cccnc3)c1)CC2

Safety Information

Safety Phrases22-24/25
WGK Germany3

Synonyms

Tocris-1375
Lopac-S-2318
CAS 1423-63-8|1-(5-BROMOBENZO[B]THIOPHEN-3-YL)ETHANONE
CAS 1447-88-7|Hispidulin
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