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罗 20 - 1724 和异丁基甲基黄嘌呤对大鼠心室肌收缩基础力及β - 肾上腺素能受体介导反应的不同影响。

Differential effects of Ro 20-1724 and isobutylmethylxanthine on the basal force of contraction and beta-adrenoceptor-mediated response in the rat ventricular myocardium.

作者信息

Katano Y, Endoh M

机构信息

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

出版信息

Biochem Biophys Res Commun. 1990 Feb 28;167(1):123-9. doi: 10.1016/0006-291x(90)91739-f.

Abstract

Effects of Ro 20-1724, a selective inhibitor of soluble cGMP-insensitive type IV phosphodiesterase, on the force and cAMP levels were compared with those of 3-isobutyl-1-methylaxanthine, a non-selective inhibitor, in the rat ventricular myocardium. Ro 20-1724 scarcely affected the basal force of contraction and cAMP levels, whereas it enhanced the positive intropic effect and cAMP accumulation induced by isoproterenol more effectively than 3-isobutyl-1-methylxanthine. These results imply that inhibition of the soluble cGMP-insensitive type IV PDE by Ro 20-1724 may be crucially involved in the regulation of myocardial contractility through the interaction with cAMP generation in the rat ventricular myocardium.

摘要

在大鼠心室肌中,将可溶性环鸟苷酸不敏感的IV型磷酸二酯酶的选择性抑制剂Ro 20 - 1724对心肌收缩力和环磷酸腺苷(cAMP)水平的影响,与非选择性抑制剂3 - 异丁基 - 1 - 甲基黄嘌呤的影响进行了比较。Ro 20 - 1724几乎不影响基础收缩力和cAMP水平,然而,与3 - 异丁基 - 1 - 甲基黄嘌呤相比,它能更有效地增强异丙肾上腺素诱导的正性肌力作用和cAMP积累。这些结果表明,Ro 20 - 1724对可溶性环鸟苷酸不敏感的IV型磷酸二酯酶的抑制作用,可能通过与大鼠心室肌中cAMP生成的相互作用,在心肌收缩力的调节中起关键作用。

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