Conformational Requirements for Vascular -Adrenergic Activity

Abstract
Semi-rigid analogs of trans .alpha.- and .beta.-rotameric conformations of dopamine and epinine were studied for their .alpha.-adrenergic activity on isolated rabbit aortic strips. 2-Amino-6,7-dihydroxytetrahydronaphthalene and its N-methyl derivative (analogous to the trans .beta.-rotamer of dopamine) were 30- to 50-fold more potent than 2-amino-5,6-dihydroxytetrahydronaphthalene and its N-methyl derivatives, respectively, indicating that the trans .beta.-rotamer, rather than the trans .alpha.-rotamer, is the preferred conformation for action on the .alpha.-adrenergic receptors.

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