中枢神经系统药物的构效关系研究。十二。1-[4-(4-芳基-1-哌嗪基)丁基]-3,4-二氢-2(1H)-喹啉酮：具有潜在抗精神病活性的新型5-HT1A、5-HT2和D2配体。
Structure-activity relationship studies of CNS agents. XII. 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones: new 5-HT1A, 5-HT2 and D2 ligands with a potential antipsychotic activity.
作者信息
Mokrosz J L, Chojnacka-Wójcik E, Dereń-Wesołek A, Kłodzińska A, Maćkowiak M, Bielecka Z, Paluchowska M H
机构信息
Department of Medicinal Chemistry, Polish Academy of Sciences, Kraków.
出版信息
Drug Des Discov. 1994 Apr;11(3):197-203.
The synthesis of three 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones (5-7) was described and the receptor binding profile (5-HT1A, 5-HT2, alpha 1, D1, D2) was determined. It was found that m-chloro (5) and o-methoxy (6) derivatives are potent antagonists of the 5-HT1A, 5-HT2 and D2 receptors. It was shown that compound 6 resembles very well some atypical antipsychotics and may be considered as a novel agent of this class of drugs.
描述了三种1-[4-(4-芳基-1-哌嗪基)丁基]-3,4-二氢-2(1H)-喹啉酮(5-7)的合成，并测定了受体结合谱(5-HT1A、5-HT2、α1、D1、D2)。发现间氯(5)和邻甲氧基(6)衍生物是5-HT1A、5-HT2和D2受体的强效拮抗剂。结果表明，化合物6与某些非典型抗精神病药物非常相似，可被视为这类药物的新型制剂。
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