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

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

Affiliation

  • 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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