Ahrens Jörg, Leuwer Martin, de la Roche Jeanne, Foadi Nilufar, Krampfl Klaus, Haeseler Gertrud
Department of Anaesthesiology, Hannover Medical School, Hannover, Germany.
Pharmacology. 2009;83(2):95-8. doi: 10.1159/000180125. Epub 2008 Dec 9.
Modulation of inhibitory synaptic transmission within the central nervous system contributes considerably to the anaesthetic effects of propofol and its analogues in vivo. We have studied the effects of the non-anaesthetic propofol analogue 2,6-di-tert-butylphenol on rat alpha(1)beta(2)gamma(2) GABA(A) receptors expressed in a mammalian expression system (HEK 293 cells) using the whole-cell patch clamp technique. Our experiments showed that 2,6-di-tert-butylphenol completely lacks co-activation and direct activation of the inhibitory GABA(A) receptor. Our results support the assumption that modulation of inhibitory GABA(A) receptor function is responsible for the anaesthetic effects of propofol in vivo.
中枢神经系统内抑制性突触传递的调节对丙泊酚及其类似物在体内的麻醉作用有很大贡献。我们使用全细胞膜片钳技术，研究了非麻醉性丙泊酚类似物2,6-二叔丁基苯酚对在哺乳动物表达系统（HEK 293细胞）中表达的大鼠α(1)β(2)γ(2) GABA(A)受体的影响。我们的实验表明，2,6-二叔丁基苯酚完全缺乏对抑制性GABA(A)受体的共激活和直接激活作用。我们的结果支持这样一种假设，即抑制性GABA(A)受体功能的调节是丙泊酚在体内产生麻醉作用的原因。
