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1049747-87-6 | SB 242084 (hydrochloride)

SB 242084 (hydrochloride) NLT 98%

SKU : MC504192

CAS Number : 1049747-87-6

Molecular Formula : C21H21Cl3N4O2 | Molecular Weight : 467.78

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name SB 242084 (hydrochloride)
CAS Number 1049747-87-6
MDL Number MFCD02684417
Molecular Formula C21H21Cl3N4O2
Molecular Weight 467.78
Introduction of 1049747-87-6 :

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. IC50 value: 9.0(pKi) [1] Target: 5-HT2C antagonist in vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1]. in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

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