AFFINITY OF 2-(TETRAHYDROISOQUINOLIN-2-YLMETHYL)IMIDAZOLINE AND 2-(ISOINDOLIN-2-YLMETHYL)IMIDAZOLINE FOR ALPHA-ADRENOCEPTORS - DIFFERENTIAL AFFINITY OF IMIDAZOLINES FOR THE [H-3] IDAZOXAN-LABELED ALPHA-2-ADRENOCEPTOR VS THE [H-3] YOHIMBINE-LABELED SITE

被引：13

作者：

CLARK, RD ^{[1
]}

BERGER, J ^{[1
]}

GARG, P ^{[1
]}

WEINHARDT, KK ^{[1
]}

SPEDDING, M ^{[1
]}

KILPATRICK, AT ^{[1
]}

BROWN, CM ^{[1
]}

MACKINNON, AC ^{[1
]}

机构：

[1] SYNTEX RES CTR,EDINBURGH EH14 4AP,SCOTLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 02期

关键词：

D O I：

10.1021/jm00164a021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-(tetrahydroisoquinolin-2-ylmethyl)- and 2-(isoindolin-2-ylmethyl)imidazolines were prepared and tested for α2and α2-adrenoceptor affinity with radioligand binding. Several compounds, 5-fluoro-(5h), 5-chloro-(5j), 5,8-dimethoxy-(5r), and 5,8-dimethoxy-1-methyl-(5s) 2-(tetrahydroisoquinolin-2-ylmethyl)imidazoline, were found to be selective α2-adrenoceptor ligands on the basis of displacement of [3H]yohimbine from rat cerebral cortical membranes. One compound, 2-[(8-chloro tetrahydroisoquinolin-2-yl)methyi]imidazoline (5m), showed a 36-fold difference in affinity for the [3H]idazoxan-labeled α2-adrenoceptor relative to the [3H]yohimbine-labeled site, which may be evidence for α2-adrenoceptor subtypes. © 1990, American Chemical Society. All rights reserved.

引用

页码：596 / 600

页数：5

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