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J Med Chem. 1983 Dec;26(12):1769-72.

alpha-Adrenergic activities of some substituted 2-(aminomethyl)imidazolines.

Abstract

A series of 2-(aminomethyl)imidazolines related to the alpha-adrenergic antagonist phentolamine was prepared and evaluated for alpha-adrenergic agonist and antagonist activities in the isolated, field-stimulated rat vas deferens. Affinities for alpha-adrenergic receptors were determined by displacement of [3H]clonidine and [3H]prazosin from membrane binding sites of calf cerebral cortex. This series provided a variety of alpha-adrenergic profiles, with some of the (aminomethyl)imidazolines being nonselective alpha 1- and alpha 2-adrenergic antagonists like phentolamine, while others were either nonselective alpha 1- and alpha 2-agonists or mixed alpha 1-agonists/alpha 2-antagonists.

PMID:
6139481
DOI:
10.1021/jm00366a022
[Indexed for MEDLINE]

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