title: Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
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.
authors.affiliation: Pfizer Central Research, Groton, CT 06340, USA.
authors.forename: M A
authors.initials: MA
authors.lastname: Sanner
authors.forename: T A
authors.initials: TA
authors.lastname: Chappie
authors.forename: A R
authors.initials: AR
authors.lastname: Dunaiskis
authors.forename: A F
authors.initials: AF
authors.lastname: Fliri
authors.forename: K A
authors.initials: KA
authors.lastname: Desai
authors.forename: S H
authors.initials: SH
authors.lastname: Zorn
authors.forename: E R
authors.initials: ER
authors.lastname: Jackson
authors.forename: C G
authors.initials: CG
authors.lastname: Johnson
authors.forename: J M
authors.initials: JM
authors.lastname: Morrone
authors.forename: P A
authors.initials: PA
authors.lastname: Seymour
authors.forename: M J
authors.initials: MJ
authors.lastname: Majchrzak
authors.forename: W S
authors.initials: WS
authors.lastname: Faraci
authors.forename: J L
authors.initials: JL
authors.lastname: Collins
authors.forename: D B
authors.initials: DB
authors.lastname: Duignan
authors.forename: C C
authors.initials: CC
authors.lastname: Prete Di
authors.forename: J S
authors.initials: JS
authors.lastname: Lee
authors.forename: A
authors.initials: A
authors.lastname: Trozzi
mesh_terms: D000818:Animals; D001058:Apomorphine / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D065127:Dopamine D2 Receptor Antagonists; D015195:Drug Design; D006220:Haloperidol / Q000494:pharmacology; D007202:Indicators and Reagents; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects*; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D050638:Receptors, Dopamine D4; D013329:Structure-Activity Relationship
chemical_list: C111732:CP 293019; D018492:Dopamine Antagonists; D065127:Dopamine D2 Receptor Antagonists; C493601:Drd4 protein, rat; D007202:Indicators and Reagents; D011719:Pyrazines; D011743:Pyrimidines; D050638:Receptors, Dopamine D4; D006220:Haloperidol; D001058:Apomorphine