sb-242084

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 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].

SB 242084 是5-HT2C 选择性抑制剂，pKi 值9.0，是一种精神活性药物和研究化学品。

SB 242084 monohydrochloride 是一种高选择性、竞争性及高亲和力(pKi=9.0)的5-HT2C受体拮抗剂,能够透过血脑屏障.该化合物不仅能提升中脑腹侧被盖区 (VTA) 的多巴胺能神经元基础活性,也能增加伏隔核的多巴胺释放.此外,SB 242084 monohydrochloride 通过5-HT2A受体提高线粒体基因的表达及氧化代谢.该化合物在研究焦虑、抑郁、精神分裂症的阴性症状以及急性器官损伤领域显示出显著潜力.