Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
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.
Sanner
M A
MA
Pfizer Central Research, Groton, CT 06340, USA.
Chappie
T A
TA
Dunaiskis
A R
AR
Fliri
A F
AF
Desai
K A
KA
Zorn
S H
SH
Jackson
E R
ER
Johnson
C G
CG
Morrone
J M
JM
Seymour
P A
PA
Majchrzak
M J
MJ
Faraci
W S
WS
Collins
J L
JL
Duignan
D B
DB
Prete Di
C C
CC
Lee
J S
JS
Trozzi
A
A
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
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