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Bezafibrate, a potent hypolipidemic agent, was studied as potentially preventive in the atherosclerosis-associated vascular hyperresponsiveness to α-adrenoceptors agonists in rats. Contractile responses to norepinephrine (NE) were determined in isolated tail arteries of rats fed an atherogenic or a standard diet. Atherogenic diet was biochemically confirmed to induce hypercholesterolemia. Used for 1 month, atherogenic diet increased pressor responses to NE in physiologic salt solution (PSS) and Ca2+-free PSS. When bezafibrate (100 mg/kg orally, p.o.) was administered simultaneously with atherogenic diet for 1 month, the effect was inhibited, but bezafibrate administered from day 15 of our experiment had no effect on vasoconstrictor responses to NE. Bezafibrate prevented changes in contractile responses of rat tail artery in the early stages of atherogenesis.