The Tramadol Metabolite O-Desmethyl Tramadol Inhibits Substance P–Receptor Functions Expressed in Xenopus Oocytes

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概要

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• Tramadol has been widely used as analgesic. O-Desmethyl tramadol (ODT) is one of the main metabolites of tramadol, having much greater analgesic potency than tramadol itself. Substance P receptors (SPR) are well known to modulate nociceptive transmission within the spinal cord. In this study, we investigated the effects of ODT on SPR expressed in Xenopus oocytes by examining SP-induced Ca2+-activated Cl− currents. ODT inhibited the SPR-induced Cl− currents at pharmacologically relevant concentrations. The protein kinase C (PKC) inhibitor bisindolylmaleimide I did not abolish the inhibitory effects of ODT on SP-induced Ca2+-activated Cl− currents. The results suggest that the tramadol metabolite ODT inhibits the SPR functions, which may be independent of activation of PKC-mediated pathways.

著者

• Uezono Yasuhito

  Division Of Pharmacology Department Of Translational Medical Sciences Nagasaki University Graduate S

• Yokoyama Toru

  Department Of Mechanical Engineering Faculty Of Engineering Yokohama National University

• MINAMI Kouichiro

  Department of Anesthesiology, University of Occupational and Environmental Health, School of Medicin

• OGATA Junichi

  Department of Anesthesiology, University of Occupational and Environmental Health, School of Medicin

• Minami Kouichiro

  Department Of Anesthesiology And Critical Care Medicine Jichi Medical University

• Yokoyama Toru

  Department Of Anesthesiology And Critical Care Medicine Jichi Medical University

• Ogata Junichi

  Department Of Anesthesiology And Critical Care Medicine Jichi Medical University

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