Yamakura T, Sakimura K, Shimoji K, Mishina M
Department of Neuropharmacology, Niigata University, Japan.
Neurosci Lett. 1995 Mar 31;188(3):187-90. doi: 10.1016/0304-3940(95)11431-u.
Effects of a general intravenous anesthetic 2,6-diisopropylphenol (propofol) on various glutamate receptor (GluR) channels were examined on the alpha 1 and alpha 1/alpha 2 GluR channels selective for alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), the beta 2/gamma 2 GluR channels selective for kainate, and the epsilon 2/zeta 1 and epsilon 3/zeta 1 N-methyl-D-aspartate (NMDA) receptor channels expressed in Xenopus oocytes. Propofol suppressed the current responses of the alpha 1/alpha 2, beta 2/gamma 2, epsilon 2/zeta 1 and epsilon 3/zeta 1 channels in a dose-dependent manner, whereas it enhanced the current responses of the alpha 1 channel. The extents of inhibition were in the order epsilon 2/zeta 1 > epsilon 3/zeta 1 > beta 2/gamma 2 > alpha 1/alpha 2 channels. During perfusion of 500 microM propofol, the alpha 1/alpha 2, beta 2/gamma 2, epsilon 2/zeta 1 and epsilon 3/zeta 1 channels were progressively suppressed. Furthermore, 10 min perfusion of 20 microM propofol inhibited the epsilon 2/zeta 1 channel by 24%. These results suggest that clinical concentrations (approximately 35 microM) of propofol suppress the NMDA receptor channels slightly.
研究了全身静脉麻醉药2,6 - 二异丙基苯酚（丙泊酚）对非洲爪蟾卵母细胞中表达的多种谷氨酸受体（GluR）通道的影响，这些通道包括对α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）具有选择性的α1和α1/α2 GluR通道、对海人藻酸具有选择性的β2/γ2 GluR通道以及ε2/ζ1和ε3/ζ1 N-甲基-D-天冬氨酸（NMDA）受体通道。丙泊酚以剂量依赖性方式抑制α1/α2、β2/γ2、ε2/ζ1和ε3/ζ1通道的电流反应，而增强α1通道的电流反应。抑制程度顺序为ε2/ζ1>ε3/ζ1>β2/γ2>α1/α2通道。在灌注500微摩尔丙泊酚期间，α1/α2、β2/γ2、ε2/ζ1和ε3/ζ1通道逐渐受到抑制。此外，灌注20微摩尔丙泊酚10分钟可使ε2/ζ1通道抑制24%。这些结果表明，临床浓度（约35微摩尔）的丙泊酚对NMDA受体通道有轻微抑制作用。
