Receptor specificity defines algogenic properties of propofol and fospropofol

Amol Patwardhan; Rebecca Edelmayer; Emil Annabi; Theodore Price; Phil Malan; Gregory Dussor

doi:10.1213/ANE.0b013e318258b9db

Receptor specificity defines algogenic properties of propofol and fospropofol

Amol Patwardhan, Rebecca Edelmayer, Emil Annabi, Theodore Price, Phil Malan, Gregory Dussor

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

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.

Original language	English (US)
Pages (from-to)	837-840
Number of pages	4
Journal	Anesthesia and analgesia
Volume	115
Issue number	4
DOIs	https://doi.org/10.1213/ANE.0b013e318258b9db
State	Published - Oct 2012

ASJC Scopus subject areas

Anesthesiology and Pain Medicine

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title = "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.",

author = "Amol Patwardhan and Rebecca Edelmayer and Emil Annabi and Theodore Price and Phil Malan and Gregory Dussor",

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T1 - Receptor specificity defines algogenic properties of propofol and fospropofol

AU - Patwardhan, Amol

AU - Edelmayer, Rebecca

AU - Annabi, Emil

AU - Price, Theodore

AU - Malan, Phil

AU - Dussor, Gregory

PY - 2012/10

Y1 - 2012/10

N2 - 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.

AB - 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.

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Receptor specificity defines algogenic properties of propofol and fospropofol

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