Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.

Abstract:

:A series of novel, potent and selective pyrido[1,2-a]pyrazine dopamine D4 receptor antagonists are reported including CP-293,019 (D4 Ki = 3.4 nM, D2 Ki > 3,310 nM), which also inhibits apomorphine-induced hyperlocomotion in rats after oral dosing.

journal_name

Bioorg Med Chem Lett

authors

Sanner MA,Chappie TA,Dunaiskis AR,Fliri AF,Desai KA,Zorn SH,Jackson ER,Johnson CG,Morrone JM,Seymour PA,Majchrzak MJ,Faraci WS,Collins JL,Duignan DB,Prete Di CC,Lee JS,Trozzi A

doi

10.1016/s0960-894x(98)00108-5

subject

Has Abstract

pub_date

1998-04-07 00:00:00

pages

725-30

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960894X98001085

journal_volume

8

pub_type

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