SB 242084 hydrochloride

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.

SB 242084 dihydrochloride (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2C receptor in SH-SY5Y cells.SB 242084 dihydrochloride (1-100 nM; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC. 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.

SB 242084 dihydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests.SB 242084 dihydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats.SB 242084 dihydrochloride (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats.SB 242084 dihydrochloride (160-640 μg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo. Animal Model:Male Sprague-Dawley (CD) rats.Dosage:0.1-1 mg/kg Administration:Intraperitoneal injection; single; 20 min pre-test Result: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 hydrochloride

Endocrinology/Hormones

5-HT Receptor

5-HT Receptor

Neurological Disease

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1049747-87-6

467.8

C21H19ClN4O2 ? 2HCl

>98% (HPLC)

10 mM in DMSO

CC1=NC=CC=C1OC(N=C2)=CC=C2NC(N3CCC4=C3C=C(Cl)C(C)=C4)=O.Cl.Cl

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

(-20℃)

With Ice Pack

≥ 2 years