Rp-8-溴鸟苷-3',5'-环一磷酸硫酯抑制硝酸甘油引起的兔主动脉舒张。

Rp-8-Br-guanosine-3',5'-cyclic monophosphorothioate inhibits relaxation elicited by nitroglycerin in rabbit aorta.

作者信息

Nakazawa M, Imai S

机构信息

Department of Pharmacology, Niigata University School of Medicine, Japan.

出版信息

Eur J Pharmacol. 1994 Feb 21;253(1-2):179-81. doi: 10.1016/0014-2999(94)90775-7.

DOI:10.1016/0014-2999(94)90775-7

PMID:8013545

Abstract

To ascertain whether the activation of cyclic GMP-dependent protein kinase is involved in the relaxant effects of nitroglycerin, the effects of Rp-8-Br-guanosine-3',5'-cyclic monophosphorothioate (Rp-8-Br-cGMPS), an inhibitor of activation of G-kinase by cyclic GMP, were studied. In the isolated rabbit aorta contracted by phenylephrine, Rp-8-Br-cGMPS (30 microM) competitively inhibited the relaxation elicited by 8-Br-cGMP, but not that elicited by 8-Br-cyclic AMP, indicating that Rp-8-Br-cGMPS is a specific inhibitor of activation of cyclic GMP-dependent protein kinase by cyclic GMP. The relaxation elicited by nitroglycerin was inhibited by Rp-8-Br-cGMPS.

摘要

为了确定环鸟苷酸依赖性蛋白激酶的激活是否参与硝酸甘油的舒张作用，研究了Rp-8-溴鸟苷-3',5'-环一磷酸硫代酯（Rp-8-Br-cGMPS），一种环鸟苷酸激活G激酶的抑制剂的作用。在由去氧肾上腺素收缩的离体兔主动脉中，Rp-8-Br-cGMPS（30微摩尔）竞争性抑制8-溴环鸟苷酸引起的舒张，但不抑制8-溴环腺苷酸引起的舒张，表明Rp-8-Br-cGMPS是环鸟苷酸激活环鸟苷酸依赖性蛋白激酶的特异性抑制剂。硝酸甘油引起的舒张被Rp-8-Br-cGMPS抑制。