Receptor specificity defines algogenic properties of propofol and fospropofol.

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.

journal_name

Anesth Analg

journal_title

Anesthesia and analgesia

authors

Patwardhan A,Edelmayer R,Annabi E,Price T,Malan P,Dussor G

doi

10.1213/ANE.0b013e318258b9db

subject

Has Abstract

pub_date

2012-10-01 00:00:00

pages

837-40

issue

4

eissn

0003-2999

issn

1526-7598

pii

ANE.0b013e318258b9db

journal_volume

115

pub_type

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