Zbicz K L, Wilson W A
J Pharmacol Exp Ther. 1981 Apr;217(1):222-7.
Pentobarbital and phenobarbital inhibit repetitive firing of action potentials in neurons of Aplysia by enhancing the normal process of spike frequency adaptation. Voltage clamp studies reveal a slowly developing outward current which is unique to neurons demonstrating spike frequency adaptation. Enhancement of this current by barbiturates was demonstrated and is the probable mechanism by which these drugs enhance adaptation. In experiments in which the pH of the applied drug solutions was altered, barbiturates were more effective in increasing both the slow outward current and adaptation at low pH, suggesting the unionized, acid form, of the drug is responsible for these effects. The concentrations of phenobarbital which were effective closely resembled plasma levels expected to be anticonvulsant.
戊巴比妥和苯巴比妥通过增强动作电位频率适应的正常过程,抑制海兔神经元动作电位的重复发放。电压钳研究揭示了一种缓慢发展的外向电流,这是表现出动作电位频率适应的神经元所特有的。已证实巴比妥类药物可增强这种电流,这可能是这些药物增强适应性的机制。在改变所用药物溶液pH值的实验中,巴比妥类药物在低pH值时更有效地增加缓慢外向电流和适应性,表明药物的非离子化酸性形式是造成这些效应的原因。有效的苯巴比妥浓度与预期具有抗惊厥作用的血浆水平非常相似。