Rick C E, Ye Q, Finn S E, Harrison N L
Department of Anesthesia and Critical Care, Whitman Labs, University of Chicago, IL 60637, USA.
Neuroreport. 1998 Feb 16;9(3):379-83. doi: 10.1097/00001756-199802160-00004.
Two sets of chimeras between alphaxalone-sensitive GABA(A) receptor alpha2 or beta1 subunits and the alphaxalone-insensitive glycine receptor alpha1 subunit were constructed to determine the structural domains important for the modulatory actions of neuroactive steroids. These data suggest that the site of action for neurosteroids on GABA(A) receptors is not the same as that for volatile anesthetics and ethanol, but is on the N-terminal side of the middle of TM2.
构建了两组嵌合体,一组由对alphaxalone敏感的GABA(A)受体α2或β1亚基与对alphaxalone不敏感的甘氨酸受体α1亚基组成,另一组由对alphaxalone不敏感的甘氨酸受体α1亚基与对alphaxalone敏感的GABA(A)受体α2或β1亚基组成,以确定对神经活性类固醇调节作用至关重要的结构域。这些数据表明,神经甾体在GABA(A)受体上的作用位点与挥发性麻醉剂和乙醇的作用位点不同,而是位于跨膜区2中部的N端一侧。