Mullin M J, Hunt W A
Life Sci. 1984 Jan 16;34(3):287-92. doi: 10.1016/0024-3205(84)90601-5.
The effects of ethanol and pentobarbital on voltage-sensitive sodium channels in whole brain (rat) synaptosomes were studied using isotopic flux measurements. Incubation of synaptosomes with ethanol or pentobarbital in vitro inhibited veratridine-stimulated 22Na+ uptake. The effect of ethanol is dose-dependent, occurs at sublethal, pharmacologically relevant concentrations and is fully reversible. These results suggest that ethanol and pentobarbital directly interfere with sodium channel function in nervous tissue. Alterations in sodium channel function may be a possible mechanism for the central nervous system (CNS) depressant action of ethanol and related compounds.
利用同位素通量测量法研究了乙醇和戊巴比妥对全脑(大鼠)突触体中电压敏感性钠通道的影响。在体外将突触体与乙醇或戊巴比妥一起孵育可抑制藜芦碱刺激的22Na+摄取。乙醇的作用具有剂量依赖性,在亚致死的、药理学相关浓度下出现,并且是完全可逆的。这些结果表明乙醇和戊巴比妥直接干扰神经组织中的钠通道功能。钠通道功能的改变可能是乙醇及相关化合物对中枢神经系统(CNS)产生抑制作用的一种可能机制。