Abstract
Effects of a general intravenous anesthetic 2,6-diisopropylphenol (propofol) on various glutamate receptor (GluR) channels were examined on the α1 and α1 α2 GluR channels selective for α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), the β2 γ2 GluR channels selective for kainate, and the ε2 χ1 and ε3 χ1 and ϵ3 χ1 N-methyl- d-aspartate (NMDA) receptor channels expressed in Xenopus oocytes. Propofol suppressed the current responses of the α1 α2 , β2 γ2 , ε2 χ1 and ε3 χ1 channels in a dose-dependent manner, whereas it enhanced the current responses of the α1 channel. The extents of inhibition were in the order ε2/χ > ε3/χ1 > β2/γ2 > α1/α2 channels. During perfusion of 500 μM propofol, the α1 α2 , β2 γ2 , ϵ2 χ1 and ε3 χ1 channels were progressively suppressed. Furthermore, 10 min perfusion of 20 μM propofol inhibited the ε2 χ1 channel by 24%. These results suggest that clinical concentrations (∼35 μM) of propofol suppress the NMDA receptor channels slightly.
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