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. doi: 10.1016/s0960-894x(98)00108-5.
M A Sanner  1 ,  T A Chappie ,  A R Dunaiskis ,  A F Fliri ,  K A Desai ,  S H Zorn ,  E R Jackson ,  C G Johnson ,  J M Morrone ,  P A Seymour ,  M J Majchrzak ,  W S Faraci ,  J L Collins ,  D B Duignan ,  C C Prete Di ,  J S Lee ,  A Trozzi
Affiliations
  • 1. Pfizer Central Research, Groton, CT 06340, USA.
PMID: 9871530 DOI: 10.1016/s0960-894x(98)00108-5
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.

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