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Rapid broad-spectrum analgesia through activation of peroxisome proliferator-activated receptor-. J Pharmacol Exp Ther 319:1051–1061 (2006)
| Venue: | Mattace-Raso G, Meli R, Hohmann A, Calignano A, and Piomelli D |
| Citations: | 20 - 0 self |
BibTeX
@ARTICLE{Loverme06rapidbroad-spectrum,
author = {Jesse Loverme and Roberto Russo and Giovanna La Rana and Jin Fu and Jesse Farthing and Rosaria Meli and Andrea Hohmann and Antonio Calignano and Daniele Piomelli},
title = {Rapid broad-spectrum analgesia through activation of peroxisome proliferator-activated receptor-. J Pharmacol Exp Ther 319:1051–1061},
journal = {Mattace-Raso G, Meli R, Hohmann A, Calignano A, and Piomelli D},
year = {2006}
}
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Abstract
Severe pain remains a major area of unmet medical need. Here we report that agonists of the nuclear receptor PPAR- (per-oxisome proliferator-activated receptor-) suppress pain be-haviors induced in mice by chemical tissue injury, nerve dam-age, or inflammation. The PPAR- agonists GW7647 [2-(4-(2-(1-cyclohexanebutyl)-3-cyclohexylureido)ethyl)phenylthio)-2-methylpropionic acid], Wy-14643 [4-chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid], and palmitoylethanolamide (PEA) reduced nocifensive behaviors elicited in mice by intraplantar (i.pl.) injection of formalin or i.p. injection of magnesium sulfate. These effects were absent in PPAR--null mice yet occurred within minutes of agonist administration in wild-type mice, sug-gesting that they were mediated through a transcription-independent mechanism. Consistent with this hypothesis,
