Differential Vasorelaxant Effects of KR-30075, a New Cyclic AMP-phosphodiesterase Inhibitor, on Guinea-pig Pulmonary, Bovine Coronary and Renal Arteries

  • Jung, Yee-Suk (Korea Research Institute of Chemical Technology) ;
  • Kwon, Kwang-Il (College of Pharmacy, Chung Nam National University) ;
  • Zee, Ok-Pyo (Korea Research Institute of Chemical Technology)
  • Published : 1990.06.01

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 $F_{2a}$($PGF_{2a}$) were evaluated. KR-30075 was more potent than imazodan as a vasorelaxant against $PGF_{2a}$-induced contractions in bovine coronary and renal arteries, whereas against$K^+$induced contractions KR-30075 was less potent than imazodan in guieapig pulmonary arteries and more potent in bovine coronary arteries. KR-30075 was more potent against contractions induced by phenylephrine or $PGF_{2a}$ 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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