title: Effects of propofol on various AMPA-, kainate- and NMDA-selective glutamate receptor channels expressed in Xenopus oocytes.
abstract: 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.
authors.affiliation: Department of Neuropharmacology, Niigata University, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Yamakura
authors.forename: K
authors.initials: K
authors.lastname: Sakimura
authors.forename: K
authors.initials: K
authors.lastname: Shimoji
authors.forename: M
authors.initials: M
authors.lastname: Mishina
mesh_terms: D000818:Animals; D003001:Cloning, Molecular; D004305:Dose-Response Relationship, Drug; D015870:Gene Expression; D009865:Oocytes / Q000737:chemistry*; D018408:Patch-Clamp Techniques; D015742:Propofol / Q000494:pharmacology*; D012333:RNA, Messenger / Q000235:genetics; D018091:Receptors, AMPA / Q000187:drug effects* / Q000648:ultrastructure; D018092:Kainic Acid Receptors / Q000187:drug effects* / Q000648:ultrastructure; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects* / Q000648:ultrastructure; D014982:Xenopus laevis
chemical_list: D015742:Propofol; D012333:RNA, Messenger; D018091:Receptors, AMPA; D018092:Kainic Acid Receptors; D016194:Receptors, N-Methyl-D-Aspartate