The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor
The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor
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DOI：
10.1016/s0014-2999(02)01532-7
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发表时间：
2002-04-26
影响因子：
5
通讯作者：
Altar, CA
中科院分区：
文献类型：
--
作者：
Jordan, S;Koprivica, V;Altar, CA
阿立哌唑，7-{4-[4-（2-氨基乙基）苯基}（2，3-二氯苯基）-1-哌嗪基]丁氧基}-3，4-二氢-2（1H）-喹啉酮，一种对多巴胺D2受体具有部分激动剂活性的新型抗精神病药，与中国仓鼠卵巢细胞膜中的重组人5-HT 1A受体（h5-HT 1A）以高亲和力结合，并显示出有效的，在鸟苷-5 '-O-（3-[S-35]硫代）-三磷酸（[S-35] GTP γ S）结合试验中，对5-HT 1A受体的部分激动作用被选择性5-HT 1A受体拮抗剂完全阻断。与5-HT 1A受体的相互作用可能有助于阿立哌唑对精神分裂症症状的总体疗效。包括焦虑、抑郁、认知和阴性症状，以及其有利的副作用特征。结合先前证明阿立哌唑对多巴胺D2受体的有效部分激动作用的研究，本研究表明阿立哌唑是第一种多巴胺-5-羟色胺系统稳定剂。(C)2002 Elsevier Science B. V.保留所有权利。
Aripiprazole, 7-{4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy}-3,4-dihydro-2(1H)-quinolinone, a novel antipsychotic with partial agonist activity at dopamine D2 receptors, bound with high affinity to recombinant human 5-HT1A receptors (h5-HT1A) in Chinese hamster ovary cell membranes and displayed potent, partial agonism at 5-HT1A receptors in a guanosine-5'-O-(3-[S-35]thio)-triphosphate ([S-35]GTPgammaS)-binding assay that was blocked completely by a selective 5-HT1A receptor antagonist. An interaction with 5-HT1A receptors may contribute to the overall efficacy of aripiprazole against symptoms of schizophrenia. including anxiety, depression, cognitive and negative symptoms, and to its favorable side-effect profile. Combined with previous studies demonstrating the potent partial agonism of aripiprazole at dopamine D2 receptors, this study suggests aripiprazole is the first dopamine-serotonin system stabilizer. (C) 2002 Elsevier Science B.V. All rights reserved.