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Molecular Pharmacology, Vol 7, 1-7, Copyright © 1971 by the American Society for Pharmacology and Experimental Therapeutics

The Effect of Alpha, Beta, and Dopamine Receptor-Blocking Agents on the Stimulation of Rat Erythrocyte Adenyl Cyclase by Dihydroxyphenethylamines and Their beta-Hydroxylated Derivatives

HERBERT SHEPPARD 1 and CHARLES R. BURGHARDT 1

1 Hoffmann-La Roche Inc., Research Division, Department of Pharmacology, Nutley, New Jersey 07110

A study was made of the activation of rat erythrocyte adenyl cyclase by dopamine, D(-)-norepinephrine, and their N-methyl and N-isopropyl derivatives. The concentrations required for 50% maximal stimulation (ED50) for norepinephrine, epinephrine, and isoproterenol were 5, 0.69, and 0.24 µM, respectively. For dopamine, N-isopropyldopamine, and N-methyldopamine the ED50 values were 84, 8, and 6.8 µM. While the maximum stimulation achieved with norepinephrine and its N-alkylated derivatives was the same, that for dopamine and its derivatives varied with potency. It was postulated that the D(-)-configuration of the beta-hydroxylated series, in contrast to the deoxy analogues, induced a more activating conformational change in the cyclase. This was supported by the finding that L(+)-isoproterenol was equipotent with N-isopropyldopamine. Propranolol, chlorpromazine, haloperidol, phentolamine, serotonin, and phenoxybenzamine inhibited to the same extent the stimulation of adenyl cyclase produced by N-methyldopamine and norepinephrine. At low concentrations of inhibitor the stimulation by norepinephrine, but not by dopamine, could be reduced. These observations, along with the inactivity of apomorphine as a stimulator of adenyl cyclase, negate the existence of a specific dopamine receptor associated with the rat erythrocyte adenyl cyclase.

Submitted on July 9, 1970




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