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
收藏
页码：795 / 804
页数：10
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