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.

引用

页码：2325 / 2330

页数：6

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