A68930: a potent agonist specific for the dopamine D1 receptor.
A68930, [1R, 3S] 1-aminomethyl-5,6-dihydroxy-3-phenylisochroman HCl, is a potent, partial agonist in the dopamine-sensitive adenylate cyclase model of the D1 dopamine receptor in fish retina. In the rat caudate-putamen model of the D1 dopamine receptor, A68930 is a potent (EC50 2.1 nM) full agonist. In contrast, A68930 is a much weaker (EC50 = 3,920 nM) full agonist in a biochemical model of the D2 dopamine receptor. A68930 also displays weak 2 agonist activity but the molecule is virtually inactive at the 1 and beta-adrenoceptors. When tested in rats bearing a unilateral 6-OHDA lesion of the nigro-neostriatal neurons, A68930 elicits prolonged (> 20 hr) contralateral turning.
Neuroscience Research Division, Abbott Laboratories, Abbott Park, IL 60061.
J W
JW
Kebabian
M P
MP
DeNinno
R
R
Schoenleber
R
R
MacKenzie
D R
DR
Britton
K E
KE
Asin
D000262:Adenylyl Cyclases / Q000378:metabolism; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D002347:Carps; D002421:Caudate Nucleus / Q000201:enzymology; D002839:Chromans / Q000494:pharmacology*; D018491:Dopamine Agonists / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D011699:Putamen / Q000201:enzymology; D051381:Rats; D017447:Receptors, Dopamine D1 / Q000819:agonists*; D012160:Retina / Q000378:metabolism; D012640:Seizures / Q000139:chemically induced
D002839:Chromans; D018491:Dopamine Agonists; D017447:Receptors, Dopamine D1; C065380:A 68930; D000262:Adenylyl Cyclases