A68930: a potent and specific agonist for the D-1 dopamine receptor.

J W Kebabian, C Briggs, D R Britton, K Asin, M DeNinno, R G MacKenzie, J F McKelvy, R Schoenleber

Index: Am. J. Hypertens. 3 , 40S-42S, (1990)

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Abstract

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.