Effects of Rp-8-Br-cGMPS, a selective inhibitor of activation of cyclic GMP-dependent protein kinase by cyclic GMP, on relaxation of the rat aortic smooth muscle induced by nitroglycerin and nitroprusside.

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  • cGMP依存性プロテインキナーゼのcyclic GMPによる活性化を選択的に抑制する物質であるRp-8-Br-guanosine 3',5'-cyclic monophosphorothioate(Rp-8-Br-cGMPS)の、ニトログリセリン、ニトロプルシッドによるラット大動脈平滑筋弛緩に対する作用

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To examine the importance of activation of cyclic GMP-dependent protein kinase (protein kinase G) by cyclic GMP in relaxation of vascular smooth muscle by nitroglycerin and nitroprusside, effects of Rp-8-Br-guanosine 3' ,5'-cyclic monophosphorothioate (Rp-8-Br-cGMPS), a selective, membrane permeable inhibitor of activation of protein kinase G by cyclic GMP, were studied using the isolated ring preparations of the rat aorta. Relaxation of high K^+ -contracted preparations by nitroglycerin and nitroprusside which has been repeatedly shown to occur in association with lowering of Ca^<2+> sensitivity of contractile protein was effectively counteracted by Rp-8-Br-cGMPS in harmony with our recent findings on the intimate connection of Ca^<2+> sensitivity lowering with activation of protein kinase G, while relaxation of phenylephrine-contracted preparations generally considered to proceed in connection with lowering of intracellular concentrations of Ca^<2+> was not.

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