trans-2,6-, 3,6-and 4,6-diaza-5,6,6a,7,8,12b-hexahydrobenzo[C]phenanthrene-10,11-diols as dopamine agonists

被引：8

作者：

Gu, YG ^{[1
]}

Bayburt, EK ^{[1
]}

Michaelides, MR ^{[1
]}

Lin, CW ^{[1
]}

Shiosaki, K ^{[1
]}

机构：

[1] Abbott Labs, Pharmaceut Discovery, Neurosci Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(99)00214-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The title compounds were synthesized by replacing the thiophene moiety of A-86929(2a) with variously substituted pyridines. Dopamine D-1 and D-2 binding and adenylate cyclase assays indicate that 4,6-diaza compounds 15 are potent and selective full D1 agonists when R-1 is H or a small substituent and R-2 = H, with D1 binding affinity and adenylate cyclase functional potency equivalent to that of A-86929(2a). (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：1341 / 1346

页数：6

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