MORPHOLINOALKYLINDENES AS ANTINOCICEPTIVE AGENTS - NOVEL CANNABINOID RECEPTOR AGONISTS

被引：20

作者：

KUMAR, V ^{[1
]}

ALEXANDER, MD ^{[1
]}

BELL, MR ^{[1
]}

EISSENSTAT, MA ^{[1
]}

CASIANO, FM ^{[1
]}

CHIPPARI, SM ^{[1
]}

HAYCOCK, DA ^{[1
]}

LUTTINGER, DA ^{[1
]}

KUSTER, JE ^{[1
]}

MILLER, MS ^{[1
]}

STEVENSON, JI ^{[1
]}

WARD, SJ ^{[1
]}

机构：

[1] STERLING WINTHROP PHARMACEUT RES DIV,DEPT NEUROSCI,COLLEGEVILLE,PA 19426

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 04期

关键词：

D O I：

10.1016/0960-894X(95)00040-Z

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Indene analogs of pravadoline exhibited antinociceptive activity in several animal models. The inhibition of prostaglandin (PG) synthesis in mouse brain microsomes was diminished in these pravadoline analogs, but they were potent in inhibiting electrically stimulated contractions in the mouse vas deferens (MVD) preparations. Binding studies with ligand WIN 55212-2 have aided to demonstrate that the morpholinoalkylindene binding site is functionally equivalent with cannabinoid binding site. The antinociceptive activity of the indene derivatives appears to be mediated by increased affinity for the cannabinoid receptor.

引用

页码：381 / 386

页数：6

共 12 条

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