1-aryl-4-[(1-tetralinyl)alkyl]piperazine: Alkylamido and alkylamino derivatives. Synthesis, 5-HT1A receptor affinity, and selectivity .3.

被引：33
|
作者：
Perrone, R [1 ]
Berardi, F [1 ]
Leopoldo, M [1 ]
Tortorella, V [1 ]
机构：
[1] PHARMACIA SPA, I-20014 NERVIANO, MI, ITALY
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1996年 / 39卷 / 16期
关键词：
D O I：
10.1021/jm960087s
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and binding profile on 5-HT1A, 5-HT2, D-1, D-2, alpha(1), and alpha(2) receptors of the N-4 long-chain arylpiperazines 22-40 are reported, where an amino or amido function is inserted into the intermediate chain linked to the a position of the tetralin nucleus. Unlike the buspirone analogues, for the amido derivatives studied in this paper, the terminal amide function of long-chain piperazines is not important for 5-HT1A receptor affinity binding, and its removal yields high-affinity 5-HT1A receptor agents.
引用
收藏
页码：3195 / 3202
页数：8
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