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

Article abstract of DOI:10.1016/S0960-894X(98)00108-5

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