低剂量乙醇与一种神经活性甾体产生正向相互作用，从而调节大鼠γ-氨基丁酸A型（GABA(A)）受体功能。
Low doses of ethanol and a neuroactive steroid positively interact to modulate rat GABA(A) receptor function.
作者信息
Akk Gustav, Steinbach Joe Henry
机构信息
Department of Anesthesiology, Washington University School of Medicine, Campus Box 8054, 660 S. Euclid Avenue, St Louis, MO 63110, USA.
出版信息
J Physiol. 2003 Feb 1;546(Pt 3):641-6. doi: 10.1113/jphysiol.2002.032300.
Fast inhibitory responses in the central nervous system are mediated by the GABA(A) receptor. The activation and function of the GABA(A) receptor can be modulated by a variety of compounds including benzodiazepines, barbiturates and neuroactive steroids. Modulation of the GABA(A) receptor function by ethanol has been observed in some but not all studies. We have studied the effect of ethanol at concentrations corresponding to light intoxication on the function of the recombinant GABA(A) receptor containing alpha1beta2gamma2 subunits. The experiments were performed both in the absence and presence of low, subthreshold concentrations of a neuroactive steroid. The results demonstrate that, in the presence of the steroid, 0.05 % (9 mM) ethanol potentiates the GABA(A) receptor function by increasing the channel mean open duration. No effect was observed on the channel closed time durations. The data suggest that ethanol influences channel closing with no effect on the affinity of the receptor for GABA or the channel opening rate constant.
中枢神经系统中的快速抑制反应由GABA(A)受体介导。GABA(A)受体的激活和功能可被多种化合物调节，包括苯二氮䓬类、巴比妥类和神经活性甾体。在一些但并非所有研究中都观察到乙醇对GABA(A)受体功能的调节作用。我们研究了与轻度中毒相对应浓度的乙醇对含α1β2γ2亚基的重组GABA(A)受体功能的影响。实验在不存在和存在低浓度、阈下浓度神经活性甾体的情况下均进行。结果表明，在甾体存在的情况下，0.05%（9 mM）乙醇通过增加通道平均开放持续时间来增强GABA(A)受体功能。未观察到对通道关闭持续时间的影响。数据表明乙醇影响通道关闭，而对受体对GABA的亲和力或通道开放速率常数无影响。
Zotero 插件