Huguenard J R, Wilson W A
J Pharmacol Exp Ther. 1985 Jan;232(1):228-31.
A slow outward current has been demonstrated in Aplysia giant neurons which serves to suppress repetitive firing. The barbiturates phenobarbital and pentobarbital enhance the slow outward current and the suppression of repetitive firing. In this study, the effects of diphenylbarbituric acid, which shows anticonvulsant activity in mice and rats but possesses minimal sedative properties, were tested on slow outward current and firing behavior. Diphenylbarbituric acid enhances slow outward current and suppresses repetitive firing at lower concentrations than phenobarbital and pentobarbital. Because diphenylbarbituric acid is effective at enhancing slow outward current but does not produce sedation, this property of barbiturates is apparently not associated with the sedative properties of these drugs, but rather is important for the anticonvulsant effects.
在海兔巨型神经元中已证实存在一种缓慢外向电流,其作用是抑制重复放电。巴比妥类药物苯巴比妥和戊巴比妥可增强这种缓慢外向电流并抑制重复放电。在本研究中,测试了二苯基巴比妥酸对缓慢外向电流和放电行为的影响,二苯基巴比妥酸在小鼠和大鼠中显示出抗惊厥活性,但镇静特性极小。与苯巴比妥和戊巴比妥相比,二苯基巴比妥酸在较低浓度时就能增强缓慢外向电流并抑制重复放电。由于二苯基巴比妥酸在增强缓慢外向电流方面有效但不产生镇静作用,巴比妥类药物的这一特性显然与这些药物的镇静特性无关,而是对抗惊厥作用很重要。