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KMID : 0043319900130020136
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Archives of Pharmacal Research
1990 Volume.13 No. 2 p.136 ~ p.141
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Differential Vasorelaxant Effects of KR-30075, a New Cyclic AMP-phosphodiesterase Inhibitor, on Guinea-pig Pulmonary, Bovine Coronary and Renal Arteries
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Jung YS
Kwon KI/Zee OP
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Abstract
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The vasorelaxant effects of KR-30075 in guinea-pig pulmonary, bovine coronary and renal arterial strips contracted by either K+-depolarization, phenylephrine, or prostaglandin F2alpha(PGF2alpha)were evaluated. KR-30075 was more potent than imazodan as a vasorelaxant against PGF2alpha-induced contractions in bovine coronary and renal arteries, whereas against K+-induced contractions KR-30075 was less potent than imazodan in guinea-pig pulmonary arteries and more potent in bovine coronary arteries. KR-30075 was more potent against contractions induced by phenylephrine or PGF2alpha 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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