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N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation.
J Pharmacol Sci. 2012; 118(2):156-60.JP

Abstract

Although the antinociceptive effects of N-palmitoyl-ethanolamine (PEA) were first characterized nearly 50 years ago, the identity of the mechanism that mediates these actions has not been elucidated. The present study investigated the contribution of K(+) channels on peripheral antinociception induced by the CB(2) agonist PEA. Nociceptive thresholds to mechanical paw stimulation of Wistar rats treated with intraplantar prostaglandin E(2) to induce hyperalgesia were measured, and other agents were also given by local injection. PEA (5, 10, and 20 µg/paw) elicited a local peripheral antinociceptive effect. This effect was antagonized by glibenclamide, a selective blocker of ATP-sensitive K(+) channels (20, 40, and 80 µg/paw). In addition, neither the voltage-dependent K(+) channel-specific blocker tetraethylammonium (30 µg/paw) nor the small and large conductance blockers of Ca(2+)-activated K(+) channels, dequalinium (50 µg/paw) and paxilline (20 µg/paw), respectively, were able to block the local antinociceptive effect of PEA. These results indicate that the activation of ATP-sensitive K(+) channels could be the mechanism that induces peripheral antinociception by PEA and that voltage-dependent K(+) channels and small and large conductance Ca(2+)-activated K(+) channels do not appear to be involved in this mechanism.

Authors+Show Affiliations

Department of Pharmacology, Institute of Biological Sciences (ICB), Federal University of Minas Gerais, Brazil.No affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

22343363

Citation

Romero, Thiago Roberto Lima, and Igor Dimitri Gama Duarte. "N-palmitoyl-ethanolamine (PEA) Induces Peripheral Antinociceptive Effect By ATP-sensitive K+-channel Activation." Journal of Pharmacological Sciences, vol. 118, no. 2, 2012, pp. 156-60.
Romero TR, Duarte ID. N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation. J Pharmacol Sci. 2012;118(2):156-60.
Romero, T. R., & Duarte, I. D. (2012). N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation. Journal of Pharmacological Sciences, 118(2), 156-60.
Romero TR, Duarte ID. N-palmitoyl-ethanolamine (PEA) Induces Peripheral Antinociceptive Effect By ATP-sensitive K+-channel Activation. J Pharmacol Sci. 2012;118(2):156-60. PubMed PMID: 22343363.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation. AU - Romero,Thiago Roberto Lima, AU - Duarte,Igor Dimitri Gama, PY - 2012/2/21/entrez PY - 2012/2/22/pubmed PY - 2012/6/16/medline SP - 156 EP - 60 JF - Journal of pharmacological sciences JO - J Pharmacol Sci VL - 118 IS - 2 N2 - Although the antinociceptive effects of N-palmitoyl-ethanolamine (PEA) were first characterized nearly 50 years ago, the identity of the mechanism that mediates these actions has not been elucidated. The present study investigated the contribution of K(+) channels on peripheral antinociception induced by the CB(2) agonist PEA. Nociceptive thresholds to mechanical paw stimulation of Wistar rats treated with intraplantar prostaglandin E(2) to induce hyperalgesia were measured, and other agents were also given by local injection. PEA (5, 10, and 20 µg/paw) elicited a local peripheral antinociceptive effect. This effect was antagonized by glibenclamide, a selective blocker of ATP-sensitive K(+) channels (20, 40, and 80 µg/paw). In addition, neither the voltage-dependent K(+) channel-specific blocker tetraethylammonium (30 µg/paw) nor the small and large conductance blockers of Ca(2+)-activated K(+) channels, dequalinium (50 µg/paw) and paxilline (20 µg/paw), respectively, were able to block the local antinociceptive effect of PEA. These results indicate that the activation of ATP-sensitive K(+) channels could be the mechanism that induces peripheral antinociception by PEA and that voltage-dependent K(+) channels and small and large conductance Ca(2+)-activated K(+) channels do not appear to be involved in this mechanism. SN - 1347-8648 UR - https://www.unboundmedicine.com/medline/citation/22343363/N_palmitoyl_ethanolamine__PEA__induces_peripheral_antinociceptive_effect_by_ATP_sensitive_K+_channel_activation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/JST.JSTAGE/jphs/11150FP DB - PRIME DP - Unbound Medicine ER -