Endoh M, Maruyama M, Taira N
J Cardiovasc Pharmacol. 1983 Jan-Feb;5(1):131-42. doi: 10.1097/00005344-198301000-00021.
Adenosine decreased the force of contraction of isolated rat left atria (direct action) and inhibited the positive inotropic action of isoproterenol (indirect action). The direct action of adenosine was not accompanied by changes in cyclic nucleotide levels, while the isoproterenol-induced increase in cyclic AMP level was reduced by the nucleoside. Reserpine pretreatment and pindolol did not affect the direct action of adenosine. Both the direct and indirect actions of adenosine were enhanced by dipyridamole and dilazep and inhibited by 1-methyl-3-isobutylxanthine and theophylline. Among adenosine derivatives, N6-phenylisopropyladenosine was most potent, and 2'-deoxyadenosine was least effective in inducing the negative inotropic action in the absence and presence of isoproterenol. In atria pretreated with islet-activating protein (IAP) both the direct and indirect actions of adenosine, and the actions of N6-phenylisopropyladenosine were markedly attenuated compared with those in nontreated atria. The isoproterenol-induced increase in cyclic AMP level was not reduced by adenosine in IAP-treated atria. These results indicate that adenosine produces a dual action on rat atria: it decreases the force of contraction directly by a mechanism independent of cyclic AMP metabolism, and inhibits the positive inotropic action of isoproterenol by reducing the drug-induced accumulation of cyclic AMP. IAP attenuates both of these inhibitory actions of adenosine on rat atria.
腺苷可降低离体大鼠左心房的收缩力(直接作用),并抑制异丙肾上腺素的正性肌力作用(间接作用)。腺苷的直接作用并未伴随环核苷酸水平的变化,而核苷可降低异丙肾上腺素诱导的环磷酸腺苷(cAMP)水平升高。利血平预处理和吲哚洛尔不影响腺苷的直接作用。双嘧达莫和地拉齐普可增强腺苷的直接和间接作用,而1-甲基-3-异丁基黄嘌呤和茶碱则抑制其作用。在腺苷衍生物中,N6-苯基异丙基腺苷诱导负性肌力作用的效力最强,而2'-脱氧腺苷在有无异丙肾上腺素存在时诱导负性肌力作用的效果最差。与未处理的心房相比,在用胰岛激活蛋白(IAP)预处理的心房中,腺苷的直接和间接作用以及N6-苯基异丙基腺苷的作用均明显减弱。在IAP处理的心房中,腺苷不会降低异丙肾上腺素诱导的cAMP水平升高。这些结果表明,腺苷对大鼠心房产生双重作用:它通过一种独立于cAMP代谢的机制直接降低收缩力,并通过减少药物诱导的cAMP积累来抑制异丙肾上腺素的正性肌力作用。IAP可减弱腺苷对大鼠心房的这两种抑制作用。