Receptor specificity defines algogenic properties of propofol and fospropofol

Anesth Analg. 2012 Oct;115(4):837-40. doi: 10.1213/ANE.0b013e318258b9db. Epub 2012 May 14.

Abstract

Background: Propofol-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).

Methods: We tested the hypothesis using electrophysiology and behavioral studies.

Results: Our 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.

Conclusions: The lack of algogenic activity in fospropofol is most likely the result of its inability to activate TRPA1 on nociceptors.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Cells, Cultured
  • Hypnotics and Sedatives / administration & dosage*
  • Hypnotics and Sedatives / adverse effects
  • Injections, Intravenous
  • Male
  • Pain / chemically induced
  • Pain / metabolism*
  • Prodrugs / administration & dosage
  • Prodrugs / adverse effects
  • Propofol / administration & dosage*
  • Propofol / adverse effects
  • Propofol / analogs & derivatives*
  • Rats
  • Rats, Sprague-Dawley
  • TRPA1 Cation Channel
  • TRPC Cation Channels / agonists
  • TRPC Cation Channels / biosynthesis*

Substances

  • Hypnotics and Sedatives
  • Prodrugs
  • TRPA1 Cation Channel
  • TRPC Cation Channels
  • Trpa1 protein, rat
  • fospropofol
  • Propofol