Imanishi S, McAllister R G, Surawicz B
J Pharmacol Exp Ther. 1978 Nov;207(2):294-303.
Rhythmic automatic depolarizations (RAD) were produced in guinea-pig papillary muscles depolarized to membrane potentials at which depolarizations depend on membrane currents passing through the slow channel. Verapamil depressed the RAD and decreased their overshoot. These verapamil effects were dependent on its concentration either in the bath (in vitro) or in plasma and myocardium (in vivo). Increase in [Ca++] counteracted the effects of verapamil on RAD. Lidocaine concentrations ranging from 4 to 16 mg/l had no effect on overshoot and only a slight effect on the rate of RAD. We conclude that RAD are more sensitive to nonlethal and presumably therapeutic concentrations of verapamil than to high, presumably toxic, concentrations of lidocaine.
在豚鼠乳头肌中产生了节律性自动去极化(RAD),这些乳头肌被去极化至膜电位,此时去极化依赖于通过慢通道的膜电流。维拉帕米抑制了RAD并降低了它们的超射值。这些维拉帕米的作用取决于其在浴液(体外)或血浆及心肌(体内)中的浓度。[Ca++]的增加抵消了维拉帕米对RAD的作用。浓度在4至16毫克/升之间的利多卡因对超射值没有影响,对RAD的速率只有轻微影响。我们得出结论,RAD对非致死性且可能具有治疗作用的维拉帕米浓度比高浓度、可能有毒的利多卡因浓度更敏感。