DESIGN, SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME 4-DAMP-RELATED COMPOUNDS

被引：5
|
作者：
TUMIATTI, V
SPAMPINATO, S
RECANATINI, M
MINARINI, A
MELCHIORRE, C
CHIARINI, A
BUDRIESI, R
机构：
[1] UNIV BOLOGNA,DEPT PHARMACEUT SCI,I-40126 BOLOGNA,ITALY
[2] UNIV BOLOGNA,DEPT PHARMACOL,I-40126 BOLOGNA,ITALY
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 20期
关键词：
D O I：
10.1016/0960-894X(95)00403-G
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two constrained analogues (4a and 4b) of both 4-DAMP (1) and spiro-DAMP (2) were designed, and their biological profiles at muscarinic receptor subtypes were assessed by functional and binding assays. It turned out that these constrained analogues display a modest, if any, M(2)/M(3) selectivity ratio. However, most interestingly, they proved to be highly selective for muscarinic M(1) receptors.
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页码：2325 / 2330
页数：6
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