Synthesis, sar and pharmacology of CP-293,019:: A potent, selective dopamine D4 receptor antagonist

被引：39

作者：

Sanner, MA ^{[1
]}

Chappie, TA ^{[1
]}

Dunaiskis, AR ^{[1
]}

Fliri, AF ^{[1
]}

Desai, KA ^{[1
]}

Zorn, SH ^{[1
]}

Jackson, ER ^{[1
]}

Johnson, CG ^{[1
]}

Morrone, JM ^{[1
]}

Seymour, PA ^{[1
]}

Majchrzak, MJ ^{[1
]}

Faraci, WS ^{[1
]}

Collins, JL ^{[1
]}

Duignan, DB ^{[1
]}

Di Prete, CC ^{[1
]}

Lee, JS ^{[1
]}

Trozzi, A ^{[1
]}

机构：

[1] Pfizer Inc, Pfizer Cent Res, Groton, CT 06340 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(98)00108-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel, potent and selective pyrido[1,2-a]pyrazine dopamine D-4 receptor antagonists are reported including CP-293,019 (D-4 K-i = 3.4 nM, D-2 K-i > 3,310 nM), which also inhibits apomorphine-induced hyperlocomotion in rats after oral dosing. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：725 / 730

页数：6

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