Abstract
The interaction of several phenethylamines with the rat adipose tissue adrenergic receptor system has been studied utilizing the release of free fatty acids as an index of the interaction. It has been established that structural modifications of the basic phenethylamine molecule produced marked changes in the affinity of the agonists for this system and, to a lesser degree, in the intrinsic activity constants. N -Substitution of large alkyl functions increased affinity most markedly. Hydroxylation of the β carbon of the ethylamino side chain also enhanced affinity, while changes in the ring substitution produced changes varying from complete loss of all activity to alterations in the affinity constants. Phenethylamine, tyramine, ephedrine, amphetamine, and metanephrine were found to be inactive in this system. The catechol nucleus appears to confer optimal activity upon the agonist molecule, but structural modifications, particularly upon the side chain nitrogen, markedly affect the ability of the molecule to release free fatty acids from adipose tissue, in vitro .
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