The Tramadol Metabolite, O-Desmethyl Tramadol, Inhibits 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes

@article{Horishita2006TheTM,
  title={The Tramadol Metabolite, O-Desmethyl Tramadol, Inhibits 5-Hydroxytryptamine Type 2C Receptors Expressed in Xenopus Oocytes},
  author={Takafumi Horishita and Kouichiro Minami and Yasuhito Uezono and Munehiro Shiraishi and Junichi Ogata and Takashi Okamoto and Akio Shigematsu},
  journal={Pharmacology},
  year={2006},
  volume={77},
  pages={93 - 99}
}
Purpose: Tramadol is widely used clinically as an analgesic, yet the mechanism by which it produces antinociception remains unclear. O-Desmethyl tramadol, the main metabolite of tramadol, is a more potent analgesic than tramadol. We reported previously that tramadol inhibits the 5-hydroxytryptamine (5-HT) type 2C receptor (5-HT2CR), a G-protein-coupled receptor that is expressed widely within brain and that mediates several effects of 5-HT, including nociception, feeding, and locomotion. The… 

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