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

Article Details

Citation

Copy to clipboard

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

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

Bioorg Med Chem Lett. 1998 Apr 7;8(7):725-30.

PubMed ID

9871530 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Apomorphine	Dopamine D4 receptor	Protein	Humans	Yes	Agonist	Details

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Clozapine	Dopamine D2 receptor	Ki (nM)	155	N/A	N/A	Details
Clozapine	Dopamine D4 receptor	Ki (nM)	47	N/A	N/A	Details
Haloperidol	Dopamine D2 receptor	Ki (nM)	0.84	N/A	N/A	Details