The new antihypertensive I1-receptor agonist (4) was rationally synthetized by the insertion of a phenyl group in the ortho position of the aromatic ring of the I1-selective antagonist (3). This “antagonism-agonism” modulation, highlights the existence of expected analogies between I1- and alpha2-adrenoreceptor systems. Chirality proves to be crucial for the activation of I1-receptors, since the cardiovascular effects are produced exclusively by the (S)-(+)-4 enantiomer.
Rational design of the new antihypertensive I1-receptor ligand 2-(2-Biphenyl-2-yl-1-methyl-ethyl)-4,5-dihydro-1H-imidazole
PIERGENTILI, Alessandro;QUAGLIA, Wilma;
2005-01-01
Abstract
The new antihypertensive I1-receptor agonist (4) was rationally synthetized by the insertion of a phenyl group in the ortho position of the aromatic ring of the I1-selective antagonist (3). This “antagonism-agonism” modulation, highlights the existence of expected analogies between I1- and alpha2-adrenoreceptor systems. Chirality proves to be crucial for the activation of I1-receptors, since the cardiovascular effects are produced exclusively by the (S)-(+)-4 enantiomer.File in questo prodotto:
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