1. A68930: a potent agonist specific for the dopamine D1 receptor.
- Author
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Kebabian JW, DeNinno MP, Schoenleber R, MacKenzie R, Britton DR, and Asin KE
- Subjects
- Adenylyl Cyclases metabolism, Animals, Behavior, Animal drug effects, Carps, Caudate Nucleus enzymology, Enzyme Activation drug effects, Putamen enzymology, Rats, Retina metabolism, Seizures chemically induced, Chromans pharmacology, Dopamine Agonists pharmacology, Receptors, Dopamine D1 agonists
- Abstract
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.
- Published
- 1992
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