Identification of propofol binding sites in a nicotinic acetylcholine receptor with a photoreactive propofol analog.

@article{Jayakar2013IdentificationOP,
  title={Identification of propofol binding sites in a nicotinic acetylcholine receptor with a photoreactive propofol analog.},
  author={Selwyn S. Jayakar and William P Dailey and Roderic G. Eckenhoff and Jonathan B. Cohen},
  journal={The Journal of biological chemistry},
  year={2013},
  volume={288 9},
  pages={
          6178-89
        }
}
Propofol, a widely used intravenous general anesthetic, acts at anesthetic concentrations as a positive allosteric modulator of γ-aminobutyric acid type A receptors and at higher concentration as an inhibitor of nicotinic acetylcholine receptors (nAChRs). Here, we characterize propofol binding sites in a muscle-type nAChR by use of a photoreactive analog of propofol, 2-isopropyl-5-[3-(trifluoromethyl)-3H-diazirin-3-yl]phenol (AziPm). Based upon radioligand binding assays, AziPm stabilized the… CONTINUE READING

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