1-[ω-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5-pyrrolidinediones as 5-HT1A receptor ligands:: Study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity

被引:15
作者
López-Rodríguez, ML
Morcillo, MJ
Rovat, TK
Fernández, E
Sanz, AM
Orensanz, L
机构
[1] Univ Complutense, Fac Ciencias Quim, Dept Quim Organ 1, Madrid 28040, Spain
[2] Univ Nacl Educ Distancia, Fac Ciencias, Madrid 28040, Spain
[3] Hosp Ramon & Cajal, Madrid 28034, Spain
关键词
D O I
10.1016/S0960-894X(98)00074-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the present paper, we report the synthesis and the binding profile on 5-HT1A, alpha(1), and D-2 receptors of a new series of imide-arylpiperazines 3. The study oft he length of the alkyl chain and the imide substructure allows us to suggest some important differences between the no-pharmacophoric sites of both 5-HT1A and alpha(1)-adrenergic receptors, which could be of great importance in order to design new selective ligands. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:581 / 586
页数:6
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