Thakkar J, Tang S B, Sperelakis N, Wahler G M
Department of Physiology and Biophysics, University of Cincinnati College of Medicine, OH 45267-0576.
Can J Physiol Pharmacol. 1988 Aug;66(8):1092-5. doi: 10.1139/y88-178.
Cyclic GMP inhibits the slow inward Ca current of cardiac cells. This effect could be due to a cyclic GMP-mediated phosphorylation of the Ca channel (or some protein modifying Ca channel activity), or alternatively, to enhanced degradation of cyclic AMP owing to stimulation of a phosphodiesterase by cyclic GMP. To test the latter possibility, we examined the effect of extracellular 8-bromo-cyclic GMP on cyclic AMP levels in guinea pig papillary muscles, in parallel with electrophysiological experiments. Isoproterenol (10(-6) M) significantly increased the cyclic AMP levels and induced Ca-dependent slow action potentials. Superfusion with 8-bromo-cyclic GMP (10(-3) M) inhibited the slow action potentials induced by isoproterenol. However, muscles superfused with 8-bromo-cyclic GMP had cyclic AMP levels identical to those of muscles superfused with isoproterenol alone. Similarly, 8-bromo-cyclic GMP had no effect on the increase in cyclic AMP levels of muscles treated with forskolin (10(-6) M) or histamine (10(-6) M). We conclude that the inhibitory effect of cyclic GMP on slow Ca channels in guinea pig ventricular cells is not due to a decrease in the cyclic AMP levels. We hypothesize that a cyclic GMP-mediated phosphorylation is the most likely explanation for the Ca channel inhibition observed in this preparation.
环磷酸鸟苷(cGMP)抑制心肌细胞的缓慢内向钙电流。这种效应可能是由于cGMP介导的钙通道磷酸化(或某种修饰钙通道活性的蛋白质),或者是由于cGMP刺激磷酸二酯酶导致环磷酸腺苷(cAMP)降解增强。为了验证后一种可能性,我们在进行电生理实验的同时,研究了细胞外8-溴环磷酸鸟苷对豚鼠乳头肌中cAMP水平的影响。异丙肾上腺素(10^(-6) M)显著提高了cAMP水平并诱导了钙依赖性慢动作电位。用8-溴环磷酸鸟苷(10^(-3) M)灌注抑制了异丙肾上腺素诱导的慢动作电位。然而,用8-溴环磷酸鸟苷灌注的肌肉的cAMP水平与仅用异丙肾上腺素灌注的肌肉相同。同样,8-溴环磷酸鸟苷对用福斯高林(10^(-6) M)或组胺(10^(-6) M)处理的肌肉中cAMP水平的升高没有影响。我们得出结论,cGMP对豚鼠心室细胞中慢钙通道的抑制作用不是由于cAMP水平的降低。我们推测,cGMP介导的磷酸化是该制剂中观察到的钙通道抑制的最可能解释。