Schrader J, Baumann G, Gerlach E
Pflugers Arch. 1977 Nov 25;372(1):29-35. doi: 10.1007/BF00582203.
Infusion of adenosine into the coronary arteries of isolated guinea pig hearts produced a dose-dependent inhibition of dP/dtmax caused by bolus injections of isoproterenol (4 X 10(-11) moles). Threshold concentration of adenosine was 10(-7) M and maximal inhibition (90%) occurred at 10(-5) M. Coronary dilation induced by papaverine did not influence the contractile response to catecholamines. In addition to its influence on cardiac performance, adenosine (10(-5) M) effectively inhibited the isoproterenol (10(-7)M) induced initial rise in myocardial levels of cyclic 3'5'-AMP, glucose-1-phosphate and glucose-6-phosphate. Adenosine also antagonized the effect of isoproterenol on adenylate cyclase activity in a crude membrane preparation from guinea pig ventricles; it was without effect on the activity of the membrane phosphodiesterase. Theophylline inhibited the actions of adenosine both on adenylate cyclase activity and on contractile force development. Upon infusion of isoproterenol (3 X 10(-7)M) into the coronary arteries of the isolated heart (perfusion at constant pressure), the adenosine concentration in the effluent perfusate increased within 45 s from 10(-8) M to about 10(-6) M. It thus appears conceivable that in ventricular myocardium endogenously formed adenosine may serve 2 functions: dilation of the coronary arteries and limitation of the inotropic and metabolic effects of catecholamines.
向离体豚鼠心脏的冠状动脉内注入腺苷，可对由异丙肾上腺素（4×10⁻¹¹摩尔）单次注射所引起的dP/dtmax产生剂量依赖性抑制。腺苷的阈值浓度为10⁻⁷M，最大抑制作用（90%）出现在10⁻⁵M时。罂粟碱引起的冠状动脉扩张并不影响对儿茶酚胺的收缩反应。除了对心脏功能的影响外，腺苷（10⁻⁵M）还能有效抑制异丙肾上腺素（10⁻⁷M）诱导的心肌中3',5'-环磷酸腺苷、葡萄糖-1-磷酸和葡萄糖-6-磷酸水平的初始升高。腺苷还能拮抗异丙肾上腺素对豚鼠心室粗制膜制剂中腺苷酸环化酶活性的作用；它对膜磷酸二酯酶的活性没有影响。茶碱抑制腺苷对腺苷酸环化酶活性和收缩力发展的作用。向离体心脏的冠状动脉内注入异丙肾上腺素（3×10⁻⁷M）（恒压灌注）后，流出的灌注液中的腺苷浓度在45秒内从10⁻⁸M增加到约10⁻⁶M。因此，可以设想在心室心肌中内源性生成的腺苷可能具有两种功能：扩张冠状动脉以及限制儿茶酚胺的变力和代谢作用。
