α亚基异构体影响丙泊酚对GABA(A)受体的调节。
Alpha subunit isoform influences GABA(A) receptor modulation by propofol.
作者信息
Krasowski M D, O'Shea S M, Rick C E, Whiting P J, Hadingham K L, Czajkowski C, Harrison N L
机构信息
Department of Anesthesia and Critical Care, University of Chicago, IL 60637, USA.
出版信息
Neuropharmacology. 1997 Jul;36(7):941-9. doi: 10.1016/s0028-3908(97)00074-9.
Abstract
We have investigated the role of the alpha subunit in the modulation of gamma-aminobutyric acid type A (GABA(A)) receptors by the general anesthetic propofol, using whole-cell patch clamp recordings made from distinct stable fibroblast cell lines which expressed only alpha1beta3gamma2 or alpha6beta3gamma2 GABA(A) receptors. At clinically relevant anesthetic concentrations, propofol potentiated submaximal GABA currents in alpha1beta3gamma2 receptors to a far greater degree than those in alpha6beta3gamma2 receptors. The alpha subunit influenced the efficacy of propofol for modulation, but not its potency. In contrast, direct gating of the ion channel by propofol, in the absence of GABA, was significantly larger in the alpha6 than the alpha1 containing receptors. The potentiation of submaximal GABA by trichloroethanol, and the potentiation and direct gating by methohexital was also studied, and showed the same relative trends as propofol.
摘要
我们使用全细胞膜片钳记录技术，研究了α亚基在全身麻醉药丙泊酚对A型γ-氨基丁酸（GABA(A)）受体的调制作用中所起的作用，这些记录来自仅表达α1β3γ2或α6β3γ2 GABA(A)受体的不同稳定成纤维细胞系。在临床相关的麻醉浓度下，丙泊酚对α1β3γ2受体的亚最大GABA电流的增强程度远大于对α6β3γ2受体的增强程度。α亚基影响丙泊酚调制的效能，但不影响其效力。相比之下，在没有GABA的情况下，丙泊酚对离子通道的直接门控作用在含α6的受体中比含α1的受体中明显更大。还研究了三氯乙醇对亚最大GABA的增强作用，以及美索比妥的增强作用和直接门控作用，结果显示出与丙泊酚相同的相对趋势。
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