中文名 | Ocaperidone |
英文名 | Ocaperidone |
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 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 |
英文别名 | R79598 Ocaperidona Ocaperidone Ocaperidone (R79598) 3-[2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl]-2,9-dimethylpyrido[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 4H-Pyrido[1,2-a]pyrimidin-4-one, 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-2,9-dimethyl- |
CAS | 129029-23-8 |
化学式 | C24H25FN4O2 |
分子量 | 420.48 |
熔点 | 180.0 to 184.0 °C |
存储条件 | 2-8°C |
外观 | 粉末或结晶 |
颜色 | White to Light yellow |
体外研究 | Ocaperidone has high affinify at 5-HT 2 and dopamine D 2 , with K i s of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5HT 2 , a 1 -adrenergic, dopamine D 2 , histamine H 1 and a 2 -adrenergic, respectively. Ocaperidone shows 5-HT 1A receptor agonist activity, with a pEC 50 and pK i of 7.60 and 8.08. |
体内研究 | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.378 ml | 11.891 ml | 23.782 ml |
5 mM | 0.476 ml | 2.378 ml | 4.756 ml |
10 mM | 0.238 ml | 1.189 ml | 2.378 ml |
5 mM | 0.048 ml | 0.238 ml | 0.476 ml |
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