SYNTHESIS, SAR AND PHARMACOLOGY OF CP-293,019 - A POTENT, SELECTIVE DOPAMINE D-4 RECEPTOR ANTAGONIST

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 DIPRETE CC LEE JS TROZZI A
Citation
Ma. Sanner et al., SYNTHESIS, SAR AND PHARMACOLOGY OF CP-293,019 - A POTENT, SELECTIVE DOPAMINE D-4 RECEPTOR ANTAGONIST, Bioorganic & medicinal chemistry letters, 8(7), 1998, pp. 725-730
Citations number
18
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
7
Year of publication
1998
Pages
725 - 730
Database
ISI
SICI code
0960-894X(1998)8:7<725:SSAPOC>2.0.ZU;2-9
Abstract
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 L td. All rights reserved.