Propofol Inhibits Muscarinic Acetylcholine Receptor-Mediated Signal Transduction in Xenopus Oocytes Expressing the Rat M1 Receptor

The Japanese Journal of Pharmacology

Yoshihisa Nagase³  Futoshi Izumi²  Koji Sumikawa¹  Yasuhito Uezono²  Muneshige Kaibara³  Kohtaro Taniyama³ 

[1] Department of Anesthesiology, Nagasaki University School of Medicine;Department of Pharmacology, University of Occupational and Environmental Health, School of Medicine;Department of Pharmacology, Nagasaki University School of Medicine

关键词: Propofol;    Muscarinic receptor;    m1 Receptor;    Xenopus oocyte;    G protein;   

DOI  :  10.1254/jjp.79.319

学科分类：药理学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(25)Cited-By(17)The effects of propofol, 2, 6-diisopropylphenol, an intravenous general anesthetic, on signal transduction mediated by the rat M1 muscarinic acetylcholine (ACh) receptor (M1 receptor) were examined in electrophysiological studies by analyzing receptor-stimulated, Ca2+-activated Cl--current responses in the Xenopus oocyte expression system. In oocytes expressing the M1 receptor, ACh induced the Ca2+activated Cl- current, in a dose-dependent manner (EC50=114 nM). Propofol (5 - 50 μM) reversibly and dose-dependently inhibited induction of the Ca2+-activated Cl- current by ACh (100 nM) (IC50=5.6 μM). To determine a possible site affected by propofol in this signal transduction, we tested the effects of this anesthetic (10 μM) on the activation of current by injection of CaCl2 and aluminum fluoride (AlF4-). Propofol did not affect activation of the current by the intracellular injected Ca2+, or activation of the current by the intracellular injected AlF4-. These results indicate that propofol does not affect G protein, the inositol phosphate turnover, release of Ca2+ from Ca2+ store or the Ca2+-activated Cl- channel. Propofol apparently inhibits the M1 receptor-mediated signal transduction at the receptor site and/or the site of interaction between the receptor and associated G protein.

【 授权许可】

Unknown