SYNTHESIS, PHYSICOCHEMICAL AND CONFORMATIONAL PROPERTIES OF (3R,4R)-3-(3-CYCLOPROPYL-1,2,4-OXADIAZOL-5-YL)-1-AZABICYCLO[2.2.1]HEPTANE, A NOVEL M(1) SELECTIVE MUSCARINIC PARTIAL AGONIST

被引:11
作者
BAKER, R
SHOWELL, GA
STREET, LJ
SAUNDERS, J
HOOGSTEEN, K
FREEDMAN, SB
HARGREAVES, RJ
机构
[1] MERCK SHARP & DOHME LTD,DEPT BIOCHEM,HARLOW CM20 2QR,ESSEX,ENGLAND
[2] MERCK SHARP & DOHME LTD,RAHWAY,NJ 07065
[3] MERCK SHARP & DOHME LTD,DEPT PHARMACOL,HARLOW CM20 2QR,ESSEX,ENGLAND
关键词
D O I
10.1039/c39920000817
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The cyclopropyloxadiazole derivative described in the title has been shown to be a functionally selective M1 partial agonist with antagonist properties in M2 and M3 muscarinic receptor assays; conformational studies indicate free rotation around the oxadiazole-azanorbornane bond, whilst X-ray studies reveal that the cyclopropyl group is in conjugation with the oxadiazole C=N bond.
引用
收藏
页码:817 / 819
页数:3
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