Endoh M
Jpn J Pharmacol. 1979 Dec;29(6):855-64. doi: 10.1254/jjp.29.855.
On the dog isolated right ventricular muscle, experiments were carried out in order to elucidate the characteristics of the cholinergic antagonism against the positive inotropic action (PIA) induced via different subcellular mechanisms. The relationship between cyclic AMP and cyclic GMP levels, and contractile force during cholinergic antagonism was assessed. Carbachol (10 microM) by itself decreased only slightly the tension developed, but inhibited prominently the PIAs of isoprenaline, histamine, glucagon, theophylline and papaverine. The action of dibutyryl cyclic AMP was inhibited less than PIAs of other agents mentioned above. In contrast, carbachol did not affect the PIAs of calcium and g-strophanthin. The antagonism by carbachol of PIAs of isoprenaline, histamine, glucagon, theophylline and papaverine was accompanied by a reduction of the intracellular cyclic AMP level elevated previously by these agents, and by an elevation of the intracellular cyclic GMP level. A good correlation was found between changes in the tension developed, and cyclic AMP and cyclic GMP levels during the cholinergic antagonism of PIAs induced by these agents in the dog ventricular myocardium.
在犬离体右心室肌上进行实验,以阐明胆碱能拮抗作用针对通过不同亚细胞机制诱导的正性肌力作用(PIA)的特征。评估了胆碱能拮抗作用期间环磷酸腺苷(cAMP)和环磷酸鸟苷(cGMP)水平与收缩力之间的关系。卡巴胆碱(10微摩尔)单独使用时仅轻微降低所产生的张力,但显著抑制异丙肾上腺素、组胺、胰高血糖素、茶碱和罂粟碱的正性肌力作用。二丁酰环磷酸腺苷的作用受抑制程度小于上述其他药物的正性肌力作用。相反,卡巴胆碱不影响钙和毒毛花苷G的正性肌力作用。卡巴胆碱对异丙肾上腺素、组胺、胰高血糖素、茶碱和罂粟碱正性肌力作用呈拮抗作用,同时伴有这些药物先前升高的细胞内环磷酸腺苷水平降低,以及细胞内环磷酸鸟苷水平升高。在犬心室心肌中,这些药物诱导的正性肌力作用的胆碱能拮抗作用期间,所产生的张力变化与环磷酸腺苷和环磷酸鸟苷水平之间存在良好的相关性。