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Local Kappa Opioid Receptor Activation Decreases Temporomandibular Joint Inflammation

Local Kappa Opioid Receptor Activation Decreases Temporomandibular Joint Inflammation

Tânia C Chicre-Alcântara, Karla E Torres-Chávez, Luana Fischer, Juliana T Clemente-Napimoga, Vilma Melo, Carlos Amílcar Parada, Claudia Herrera Tambeli

Inflammation. 2012 Feb;35(1):371-6.

PMID: 21484425

Abstract:

In an attempt to decrease central side effects associated with the use of opioids, some strategies have been developed by targeting peripheral opioid receptors. In this context, kappa receptors are of major interest, since, in contrast to other opioid receptors, their activation is not associated with potent peripheral side effects. We have recently demonstrated that local activation of kappa opioid receptors significantly decreases formalin-induced temporomandibular joint nociception; however, whether it also decreases temporomandibular joint inflammation is not known. To address this issue, we evaluated if a specific kappa opioid receptor agonist, U50,488 (trans-(1S,2S)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide hydrochloride hydrate), administered into the temporomandibular joint decreases formalin-induced plasma extravasation and neutrophil migration. Ipsilateral, but not contralateral, administration of U50,488 into the temporomandibular joint blocked formalin-induced plasma extravasation and neutrophil migration in a dose-dependent manner. This anti-inflammatory effect was reversed by the ipsilateral, but not contralateral, administration of the kappa opioid receptor antagonist nor-BNI (nor-binaltorphimine dihydrochloride). This study demonstrates that local activation of kappa opioid receptors decreases two important parameters of temporomandibular joint inflammation, that is, plasma extravasation and neutrophil migration, in a dose-dependent and antagonist-reversible manner. This anti-inflammatory effect taken together with the potent antinociceptive effect, suggests that drugs targeting peripheral kappa opioid receptors are promising for the treatment of inflammatory temporomandibular joint pain and probably, other articular pain conditions with an inflammatory basis.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
ALP114528799	(−)-trans-(1S,2S)-U-50488 hydrochloride hydrate		114528-79-9 (anhydrous)	Price

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