Abstract

The vasorelaxant effects of KR-30075 in guinea-pig pulmonary, bovine coronary and renal arterial strips contracted by either K+-depolarization, phenylephrine, or prostaglandin F2α (FGF2α) were evaluated. KR-30075 was more potent than imazodan as a vasorelaxant against PGF2α-induced contractions in bovine coronary and renal arteries, whereas against K+-induced contractions KR-30075 was less potent than imazodan in guineapig pulmonary arteries and more potent in bovine coronary arteries. KR-30075 was more potent against contractions induced by phenylephrine or PGF2α than the contractions induced by K+. This profile of activity for KR-30075 was similar to that of imazodan and dissimilar from the calcium entry blocking agent nifedipine. There was no vascular selectivity of KR-30075 between bovine coronary and renal arterial strip preparations. In conclusion, this study shows that KR-30075 represents the vasorelaxant effects on guinea-pig pulmonary, bovine coronary and renal arteries without specific vascular selectivity. The vasorelaxant profile of KR-30075, with different sources of vascular smooth muscle, is unlike that of calcium entry blocking agent and more similar to the profile of the agent that inhibit cyclic nucleotide phosphodiesterase.

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