PHARMACODYNAMIC AND METABOLISM STUDIES ON A NEW CORONARY VASODILATOR, N-(2-HYDROXYETHYL) NICOTINAMIDE NITRATE (SG-75)

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Pharmacodynamics and metabolism of N-(2-hydroxyethyl) nicotinamide nitrate (SG-75) were investigated in rats in relation to its main metabolic product. When SG-75 was orally administered, SG-75 and SG-86, a denitrate compound of SG-75, appeared in the blood. Within 7 hr, approximately 60% of the administered SG-75 were recovered in the urine as SG-86. When administered intraduodenally, SG-75 was rapidly absorbed and transferred in an unaltered form into the portal vein. SG-75 possessed hypotensive and coronary vasodilating actions, while SG-86 had little effect on the cardiovascular system. The coronary vasodilating effects of SG-75 (0.3-30 μg i.a.) were unaffected by the continuous infusion of SG-86 into the coronary perfusion system, even in large doses (50 μg/min, or 500 μg/min).
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