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.
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.
Authors: José A Matta; Paul M Cornett; Rosa L Miyares; Ken Abe; Niaz Sahibzada; Gerard P Ahern Journal: Proc Natl Acad Sci U S A Date: 2008-06-23 Impact factor: 11.205
Authors: Michael J M Fischer; Andreas Leffler; Florian Niedermirtl; Katrin Kistner; Mirjam Eberhardt; Peter W Reeh; Carla Nau Journal: J Biol Chem Date: 2010-09-07 Impact factor: 5.157