129029-23-8
129029-23-8 結(jié)構(gòu)式
基本信息
3-(2-(4-(6-氟苯并[D]異惡唑-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]異惡唑-3-基)哌啶-1-基)乙基)-2,9-二甲基-4H-吡啶并[1,2-A]嘧啶-4-酮
Ocaperidona
Ocaperidone
Ocaperidone (R79598)
Ocaperidone USP/EP/BP
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-
5-hydroxytryptamine Receptor,Ocaperidone,inhibit,Serotonin Receptor,R 79598,Inhibitor,Dopamine Receptor,5-HT Receptor,R-79598
物理化學(xué)性質(zhì)
常見(jiàn)問(wèn)題列表
奧卡哌酮(3-[2-[4-(6-氟-1，2-苯并異噁唑-3-基)-1-哌啶基]-乙基]乙基]-2，9-二甲基-4H-吡啶并[1，2-a]嘧啶-4-酮)為神經(jīng)遞質(zhì)的拮抗劑，具體是多巴胺和血清素，是已知的抗精神病藥物。
奧卡哌酮事實(shí)上是不溶于水的。它的水溶解度小于或等于每毫升0.007毫克。在胃腸液中的溶解度也是非常低的，特別是在pH3.0的緩沖液中，在高于pH3.0的緩沖液中的溶解度與在水中的溶解度處于相同的范圍。
使用奧卡哌酮的治療征候主要是CNS區(qū)域，尤其為有效的精神抑制劑，特別適用于治療急性精神病(包括精神分裂癥、強(qiáng)制性障礙(OCD)、兩極型憂郁癥和圖雷特多綜合征。
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5-HT 2 Receptor 0.14 nM (Ki) |
a1-adrenergic receptor 0.46 nM (Ki) |
D 2 Receptor 0.75 nM (Ki) |
Histamine H 1 1.6 nM (Ki) |
a2-adrenergic receptor 5.4 nM (Ki) |
5-HT 1A Receptor 7.6 (pEC 50 , h5-HT 1A ) |
5-HT 1A Receptor 8.08 (pKi, h5-HT 1A ) |
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.
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.