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新型1-芳基-4-（联芳基亚甲基）哌嗪类化合物作为具有多巴胺D（2）受体和5-羟色胺5-HT（1A）受体亲和力的潜在非典型抗精神病药物

New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.

作者信息

Feenstra R W, de Moes J, Hofma J J, Kling H, Kuipers W, Long S K, Tulp M T, van der Heyden J A, Kruse C G

机构信息

Solvay Pharmaceuticals, Research Laboratories, PO Box 900, 1380 DA, Weesp, The Netherlands.

出版信息

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2345-9. doi: 10.1016/s0960-894x(01)00425-5.

DOI:10.1016/s0960-894x(01)00425-5
PMID:11527728
Abstract

This paper describes the syntheses of several 1-aryl-4-(biarylmethylene)piperazines and the results of the determination of their affinity for D(2) and 5-HT(1A) receptors. A selection of these compounds was evaluated in vivo, resulting in the identification of a drug candidate which is being clinically evaluated as a potential atypical antipsychotic with reduced extrapyrimidal side effects.

摘要

本文描述了几种1-芳基-4-(联芳基亚甲基)哌嗪的合成及其对D(2)和5-HT(1A)受体亲和力的测定结果。对其中一些化合物进行了体内评估，从而鉴定出一种候选药物，该药物正在作为一种具有减少锥体外系副作用的潜在非典型抗精神病药物进行临床评估。

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