MUSCARINIC AGONISTS AS ANALGESICS - ANTINOCICEPTIVE ACTIVITY VERSUS M(1) ACTIVITY - SAR OF ALKYLTHIO-TZTPS AND RELATED 1,2,5-THIADIAZOLE ANALOGS

被引：20

作者：

SAUERBERG, P ^{[1
]}

OLESEN, PH ^{[1
]}

SHEARDOWN, MJ ^{[1
]}

SUZDAK, PD ^{[1
]}

SHANNON, HE ^{[1
]}

BYMASTER, FP ^{[1
]}

CALLIGARO, DO ^{[1
]}

MITCH, CH ^{[1
]}

WARD, JS ^{[1
]}

SWEDBERG, MDB ^{[1
]}

机构：

[1] ELI LILLY & CO, LILLY CORP CTR, LILLY RES LABS, INDIANAPOLIS, IN 46285 USA

来源：

LIFE SCIENCES | 1995年 / 56卷 / 11-12期

关键词：

MUSCARINIC AGONISTS; ANTINOCICEPTION; PI HYDROLYSIS; SAR;

D O I：

10.1016/0024-3205(95)00014-W

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Alkylthio-TZTPs (3-(3-alkylthio-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1- methylpyridines) and corresponding azabicyclic analogs were tested for ml efficacy in cloned human ml receptors and for antinociceptive activity in the mouse grid shock assay. The ml (%PI) SAR were distinctly different from the analgesia and the salivation SAR, suggesting that analgesia is mediated by neither ml nor M(3) muscarinic receptors.

引用

页码：807 / 814

页数：8

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