Ravens U, Wang X L, Wettwer E
Department of Pharmacology, University of Essen, W. Germany.
J Pharmacol Exp Ther. 1989 Jul;250(1):364-70.
The effects of alpha adrenoceptor stimulation with noradrenaline were investigated in rat ventricular myocytes after blockade of beta receptors with propranolol (1 microM). At room temperature and low stimulation frequency (0.5 Hz), noradrenaline evoked a phentolamine-sensitive increase in contraction amplitude by 22%. The action potentials of myocytes were prolonged. When the sodium current was inactivated by depolarization in whole-cell voltage clamp experiments, noradrenaline caused a small, but highly variable increase in net inward current and shifted the current-voltage relation between -30 and -5 mV to the hyperpolarizing direction. These effects were absent when K+ currents were inhibited by Cs+ substitution. After inhibition of the Ca++ current with Cd++ (0.1 mM), noradrenaline decreased the peak transient outward current; it reduced the steady-state outward current in a concentration-dependent manner (pD2 value, 6.9), but had no effect on the amplitude of the transient component of outward current. Noradrenaline reduced holding current at -40 mV. The inward branch of the inward rectifier was not affected. The noradrenaline-induced changes in membrane currents were significantly smaller in the presence of phentolamine (10 microM). They are therefore considered to be mediated by alpha adrenoceptor stimulation. The reduction in outward currents can explain the prolongation in action potential duration which could contribute to the increase in contractility.
在用普萘洛尔(1微摩尔)阻断β受体后,研究了去甲肾上腺素对大鼠心室肌细胞α肾上腺素能受体的刺激作用。在室温及低刺激频率(0.5赫兹)下,去甲肾上腺素引起收缩幅度增加22%,该增加对酚妥拉明敏感,同时心肌细胞动作电位延长。在全细胞电压钳实验中,当钠电流因去极化而失活时,去甲肾上腺素引起净内向电流有小幅度但高度可变的增加,并使-30至-5毫伏之间的电流-电压关系向超极化方向移动。当用铯替代抑制钾电流时,这些效应消失。在用镉(0.1毫摩尔)抑制钙电流后,去甲肾上腺素降低了峰值瞬时外向电流;它以浓度依赖的方式降低稳态外向电流(pD2值为6.9),但对外向电流瞬时成分的幅度没有影响。去甲肾上腺素降低了-40毫伏时的钳制电流,内向整流器的内向分支未受影响。在存在酚妥拉明(10微摩尔)时,去甲肾上腺素引起的膜电流变化明显较小。因此,这些变化被认为是由α肾上腺素能受体刺激介导的。外向电流的减少可以解释动作电位时程的延长,这可能有助于收缩力的增加。