A68930: a potent and specific agonist for the D-1 dopamine receptor.
A68930 (5,6-dihydroxy-3-phenyl-1-aminomethyl-isochroman) is a potent (EC50 = 2.5 nmol/L) partial agonist at the D-1 dopamine receptor. In contrast, A68930 is a much weaker agonist (EC50 = 3,920 nmol/L) at the D-2 dopamine receptor. The orientation of the 3-phenyl substituent in the molecule is critical for the affinity and selectivity of the molecule towards the D-1 receptor in vitro and in vivo. The role of the D-1 receptor in the functioning of the basal ganglia is discussed.
Kebabian
J W
JW
Abbott Laboratories, Neuroscience Research Division, Pharmaceutical Discovery, Abbott Park, Illinois 60064.
Briggs
C
C
Britton
D R
DR
Asin
K
K
DeNinno
M
M
MacKenzie
R G
RG
McKelvy
J F
JF
Schoenleber
R
R
D000818:Animals; D001578:Benzopyrans / Q000494:pharmacology*; D002839:Chromans / Q000494:pharmacology*; D003342:Corpus Striatum / Q000502:physiology; D003714:Denervation; D004298:Dopamine / Q000502:physiology; D006892:Hydroxydopamines; D016627:Oxidopamine; D010300:Parkinson Disease / Q000188:drug therapy; D051381:Rats; D011954:Receptors, Dopamine / Q000502:physiology*; D017447:Receptors, Dopamine D1; D013237:Stereoisomerism
D001578:Benzopyrans; D002839:Chromans; D006892:Hydroxydopamines; D011954:Receptors, Dopamine; D017447:Receptors, Dopamine D1; D016627:Oxidopamine; C065380:A 68930; D004298:Dopamine