SB 242084

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB 242084 是一种有效、选择性、脑渗透性 5-HT2C 受体拮抗剂。

SB 242084 is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes; also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors; inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays; potently inhibits m-chlorophenylpiperazine (mCPP)-induced hypolocomotion in rats, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o.

Cell Viability Assay Cell Line:SH-SY5Y cells Concentration:100 nM Incubation Time:45 min Result:Antagonized 5-HT induced concentration-related increase in PI hydrolysis.RT-PCR Cell Line:RPTC cells Concentration:1-100 nM Incubation Time:24 h Result:Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.

Animal Model:Male Sprague-Dawley (CD) rats.Dosage:0.1-1 mg/kg Administration:Intraperitoneal injection; single; 20 min pre-testResult:Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.Animal Model:Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model).Dosage:5 mg/kg Administration:Intraperitoneal injection; single; 20 min pre-test Result:Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.Animal Model:Rats. Dosage:5, 10 mg/kg Administration:Intraperitoneal injection; single Result:Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

SB-242084 | SB242084

Endocrinology/Hormones

5-HT Receptor

5-HT Receptor

Neurological Disease

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181632-25-7

467.78

C21H19ClN4O2

>98% (HPLC)

DMSO: ≥ 44 mg/mL

CC1=CC2=C(C=C1Cl)N(CC2)C(=O)NC3=CN=C(C=C3)OC4=C(N=CC=C4)C.Cl.Cl

1H-Indole-1-carboxamide, 6-chloro-2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-

(-20℃)

With Ice Pack

≥ 2 years