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SB 242084
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SB 242084图片
CAS NO:181632-25-7
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
SB 242084 是一种 5-HT2C 受体拮抗剂 (pKi=9.0)，其选择性分别是 5-HT2A 和 5-HT2B 受体的 158 倍和 100 倍。
Cas No.181632-25-7
别名6-氯-2,3-二氢-5-甲基-N-[6-[(2-甲基-3-吡啶基)氧]-3-吡啶基]-1H-吲哚-1-酰胺盐酸盐
化学名6-chloro-5-methyl-N-(6-((2-methylpyridin-3-yl)oxy)pyridin-3-yl)indoline-1-carboxamide
Canonical SMILESCC1=CC2=C(C=C1Cl)N(C(NC3=CN=C(C=C3)OC4=C(C)N=CC=C4)=O)CC2
分子式C21H19ClN4O2
分子量394.85
溶解度≥ 39.5mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SB 242084 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 antagonistin 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].

References:
[1]. Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
[2]. Bromidge SM, et al. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J Med Chem. 1997 Oct 24;40(22):3494-6.
[3]. Dalton GL, et al. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology (Berl). 2006 Mar;185(1):45-57.