N-(1-benzylpyrrolidin-3-yl)arylbenzamides as potent and selective human dopamine D4 antagonists

被引：8

作者：

Egle, I ^{[1
]}

Barriault, N ^{[1
]}

Bordeleau, M ^{[1
]}

Drage, J ^{[1
]}

Dube, L ^{[1
]}

Peragine, J ^{[1
]}

Mazzocco, L ^{[1
]}

Arora, J ^{[1
]}

Jarvie, K ^{[1
]}

Tehim, A ^{[1
]}

机构：

[1] NPS Pharmaceut Inc, Mississauga, ON L4V 1V7, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 19期

关键词：

dopamine; D-4; antagonists;

D O I：

10.1016/j.bmcl.2004.07.045

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of N-(1-benzylpyrrolidin-3-yl)arylbenzamides 8 has been prepared, and their structure-activity relationships studied. Potent ligands selective for human D-4 (hD(4)) over hD(2) and alpha(1) have been identified. One example was determined to be an antagonist in a cAMP assay, with an IC50 of 1500 nM. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4847 / 4850

页数：4

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