• Anesthesia and analgesia · Oct 2012

    Receptor specificity defines algogenic properties of propofol and fospropofol.

    • Amol Patwardhan, Rebecca Edelmayer, Emil Annabi, Theodore Price, Phil Malan, and Gregory Dussor.
    • Department of Anesthesiology, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA.
    • Anesth. Analg.. 2012 Oct 1;115(4):837-40.

    BackgroundPropofol-evoked injection site pain is not observed with fospropofol. We hypothesized that unlike propofol, fospropofol does not activate the irritant receptor, transient receptor potential 1 (TRPA1).MethodsWe tested the hypothesis using electrophysiology and behavioral studies.ResultsOur data demonstrate that propofol (100 μM) evokes an inward current only in TRPA1-expressing neurons. However, fospropofol (100 μM and 1 mM) is unable to evoke depolarizing currents in either TRPA1-positive or TRPA1-negative neurons. Both propofol and fospropofol produced general anesthesia.ConclusionsThe lack of algogenic activity in fospropofol is most likely the result of its inability to activate TRPA1 on nociceptors.

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