Synthesis and in vitro structure-activity relationship of 13-tert-butyl-ergoline derivatives as 5-HT1A receptor ligands

被引：5

作者：

Mantegani, S

Brambilla, E

Caccia, C

Fornaretto, MG

McArthur, RA

Varasi, M

机构：

[1] Pharmacia and Upjohn SpA, Viale Louis Pasteur 10

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1997年 / 32卷 / 10期

关键词：

ergoline derivative; 13-tert-butyl-ergoline; 5-HT1A affinity; selectivity;

D O I：

10.1016/S0223-5234(99)80065-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 13-tert-butyl-ergoline derivatives was prepared and evaluated for affinity to adrenergic, dopaminergic and serotonergic receptor sites. Selectivity for 5-HT1A receptors versus alpha(1), alpha(2), D-1, D-2, and 5-HT2 appears to be influenced by the presence of the tert-butyl moiety at position 13 of the ergoline skeleton. Some compounds within this series display nanomolar 5-HT1A affinity and hundred-fold selectivity versus the other receptors considered.

引用

页码：795 / 804

页数：10

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