The discovery of potent and selective dopamine D4 receptor antagonists

被引：11

作者：

Faraci, WS ^{[1
]}

Zorn, SH ^{[1
]}

Sanner, MA ^{[1
]}

Fliri, A ^{[1
]}

机构：

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

来源：

CURRENT OPINION IN CHEMICAL BIOLOGY | 1998年 / 2卷 / 04期

关键词：

D O I：

10.1016/S1367-5931(98)80131-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The identification of a novel dopamine receptor subtype, referred to as the D4 receptor, which binds the atypical antipsychotic drug clozapine with high potency, has led to the initiation of a drug discovery program that aims to find novel inhibitors of this receptor subtype. A selective screening strategy was utilized, in which 4500 compounds chosen on the basis of structural similarities to known biogenic amine receptor antagonists were tested against both the D4 and D2 dopamine receptor subtypes. A potent D4-selective compound was discovered.

引用

页码：535 / 540

页数：6

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