Ocaperidone

Ocaperidone 是一种有效的安定剂，为 5-HT2 和多巴胺 D2 的拮抗剂，5-HT1A 的激动剂，对 5-HT2，a1-adrenergic 受体，dopamine D2，组胺 H1 和 a2-adrenergic 受体的 Ki 值分别为 0.14 nM，0.46 nM，0.75 nM，1.6 nM 和 5.4 nM，对 h5-HT1A 的 pEC50 和 pKi 值分别为 7.60 和 8.08。

中文名：奥卡哌酮

英文名：Ocaperidone; R79598

CAS 号： 129029-23-8

分子式：C₂₄H₂₅FN₄O₂

分子量：420.48

纯度：>98.0%

Description	Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
Target	5-HT2 Receptor;a1-adrenergic receptor;D2 Receptor;Histamine H1
In Vitro	Ocaperidone has high affinify at 5-HT2 and dopamine D2, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5HT2, a1-adrenergic, dopamine D2, histamine H1 and a2-adrenergic, respectively[1]. Ocaperidone shows 5-HT1A receptor agonist activity, with a pEC50 and pKi of 7.60 and 8.08[2].
In Vivo	Ocaperidone shows a potent occupation of 5HT2 receptor via in vivo binding in the frontal cortex of rats with an ED50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D2 receptor in the striatum and the nucleus accumbens[1]. Ocaperidone (R 79598) antagonizes dopamine D2 and 5-HT2, and shows a a partial generalization to buspirone with an ED50 of 0.163 mg/kg[3].
References	[1]. Leysen JE, et al. In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone. Mol Pharmacol. 1992 Mar;41(3):494-508. [2]. Cosi C, et al. Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells. Eur J Pharmacol. 2001 Dec 14;433(1):55-62. [3]. Rijnders HJ, et al. The discriminative stimulus properties of buspirone involve dopamine-2 receptor antagonist activity. Psychopharmacology (Berl). 1993;111(1):55-61.