Ocaperidone (Synonyms: R79598)
目录号: PL09173 纯度: ≥99%
CAS No. :129029-23-8
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中文名称
Ocaperidone
中文别名
奥卡哌酮;3-[2-[4-(6-氟苯并[d]异恶唑-3-基)哌啶-1-基]乙基]-2,9-二甲基-4H-吡啶并[1,2-a]嘧啶-4-酮
英文名称
Ocaperidone
英文别名
4H-Pyrido[1,2-a]pyrimidin-4-one,3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl-;Ocaperidone;3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethylpyrido[1,2-a]pyrimidin-4-one;4H-Pyrido[1,2-a]pyrimidin-4-one,3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-...;3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl-4H-pyrido[1,2-a]py;3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl-4H-pyrido[l,2-a]pyrimidin-4-one;3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl-pyrido[1,2-a]pyrimidin-4-one;Ocaperidona;Ocaperidona [INN-Spanish];Ocaperidone (USAN);Ocaperidonum;Ocaperidonum [INN-Latin];ocaperiodone;UNII-26HUS7139V;3-[2-[4-(6-Fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one;3-(2-(4-(6-Fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-2,9-dimethyl-4H-pyrido[1,2-a]pyrimidin-4-one;R79598
Cas No.
129029-23-8
分子式
C24H25N4O2F
分子量
420.48
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
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。
生物活性
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT 2 and dopamine D 2 antagonist, and a 5-HT 1A agonist, with K i s of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT 2 , a 1 -adrenergic receptor, dopamine D 2 , histamine H 1 and a 2 -adrenergic receptor, respectively, and a pEC 50 and pK i of 7.60 and 8.08 for h5-HT 1A .
性状
Solid
IC50 & Target[1][2]
5-HT2 Receptor 0.14 nM (Ki) D2 Receptor
体外研究(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. Ocaperidone shows 5-HT1A receptor agonist activity, with a pEC50 and pKi of 7.60 and 8.08. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Ocaperidone shows a potent occupation of 5HT 2 receptor via in vivo binding in the frontal cortex of rats with an ED 50 of 0.04 mg/kg, and 0.1 4-0.1 6 mg/kg for D 2 receptor in the striatum and the nucleus accumbens. Ocaperidone (R 79598) antagonizes dopamine D 2 and 5-HT 2 , and shows a a partial generalization to buspirone with an ED 50 of 0.163 mg/kg. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 16.67 mg/mL (39.65 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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