N-(4-Methoxy-2-nitrophenyl)hexadecanamide, a palmitoylethanolamide analogue, reduces formalin-induced nociception

Roa-Coria, José Eduardo; Navarrete‐Vázquez, Gabriel; Fowler, Christopher J.; Flores‐Murrieta, Francisco J.; Déciga-Campos, Myrna; Granados‐Soto, Vinicio

doi:10.1016/j.lfs.2012.09.024

Cited by 10 publications

(5 citation statements)

References 53 publications

(75 reference statements)

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“…In mammals, the effects of cannabinoid substances in antinociception are also mediated by the activation of CB1 receptors in specific nociception-related central structures, which activates descending nociception control pathways [5]. In rodent models of acute nociception, cannabinoids acting via CB1 receptors, inhibit responses to noxious thermal [22] and mechanical [23] stimuli, as well as the nociceptive response to the formalin test [24][25][26]. This is the first evidence of the involvement of cannabinoid system in modulation of antinociception in fish.…”

Section: Discussionmentioning

confidence: 72%

Acute administration of a cannabinoid CB1 receptor antagonist impairs stress-induced antinociception in fish

Wolkers

Barbosa

Menescal-de-Oliveira

et al. 2015

Physiology & Behavior

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Section: Discussionmentioning

confidence: 72%

Acute administration of a cannabinoid CB1 receptor antagonist impairs stress-induced antinociception in fish

Wolkers

Barbosa

Menescal-de-Oliveira

et al. 2015

Physiology & Behavior

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“…This effect was absent in CB 2 knock-out mice and blocked by AM630, a CB 2 receptor inverse agonist. Local injection of the PEA analog N -(4-methoxy-2-nitrophenyl)hexadecanamide induces CB 1 - and CB 2 -dependent antinociception in rats (Roa-Coria et al, 2012). Similar results were observed with GW833972A, another putative CB 2 receptor agonist (Belvisi et al, 2008).…”

Section: Endocannabinoids and Painmentioning

confidence: 99%

Some Prospective Alternatives for Treating Pain: The Endocannabinoid System and Its Putative Receptors GPR18 and GPR55

et al. 2019

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Background: Marijuana extracts (cannabinoids) have been used for several millennia for pain treatment. Regarding the site of action, cannabinoids are highly promiscuous molecules, but only two cannabinoid receptors (CB1 and CB2) have been deeply studied and classified. Thus, therapeutic actions, side effects and pharmacological targets for cannabinoids have been explained based on the pharmacology of cannabinoid CB1/CB2 receptors. However, the accumulation of confusing and sometimes contradictory results suggests the existence of other cannabinoid receptors. Different orphan proteins (e.g., GPR18, GPR55, GPR119, etc.) have been proposed as putative cannabinoid receptors. According to their expression, GPR18 and GPR55 could be involved in sensory transmission and pain integration.Methods: This article reviews select relevant information about the potential role of GPR18 and GPR55 in the pathophysiology of pain.Results: This work summarized novel data supporting that, besides cannabinoid CB1 and CB2 receptors, GPR18 and GPR55 may be useful for pain treatment.Conclusion: There is evidence to support an antinociceptive role for GPR18 and GPR55.

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“…We have also confirmed the correlation between PEA and the endocannabinoid system via both in vivo and ex vivo experiments, using AM281, a CB1 antagonist able to reverse um-PEA analgesic effects; moreover, repeated um-PEA administration preserves CB1 receptor expression in the spinal cord. Accordingly, a recent study reported that the administration of an analog of PEA, N-(4-methoxy-2-nitrophenyl)hexadecanamide (HD), produced a dose-dependent antinociceptive effect in rats, which was significantly counteracted by AM281 administration [ 97 ]. Taken together, these findings provide an overview of the crosstalk between PPARs and cannabinoids, and the importance of their reciprocal regulation in the control of major physiological and pathophysiological functions.…”

Section: Discussionmentioning

confidence: 99%

The Beneficial Effects of Ultramicronized Palmitoylethanolamide in the Management of Neuropathic Pain and Associated Mood Disorders Induced by Paclitaxel in Mice

et al. 2022

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Chemotherapy-induced peripheral neuropathy (CIPN) is a common complication of antineoplastic drugs, particularly paclitaxel (PTX). It can affect the quality of patients’ lives and increase the risk of developing mood disorders. Although several drugs are recommended, they yielded inconclusive results in clinical trials. The aim of the present work is to investigate whether the palmitoylethanolamide (PEA) would reduce PTX-induced CIPN and associated mood disorders. Moreover, the role PPAR-α and the endocannabinoid system will also be investigated. CIPN was induced by intraperitoneally injection of PTX (8 mg/kg) every other day for a week. PEA, 30 mg/kg, was orally administrated in a bioavailable form (i.e., ultramicronized PEA, um-PEA) one hour after the last PTX injection, for 7 days. In the antagonism experiments, AM281 (1 mg/kg) and GW6471 (2 mg/kg) were administrated 30 min before um-PEA. Our results demonstrated that um-PEA reduced the development of hypersensitivity with the effect being associated with the reduction in spinal and hippocampal pro-inflammatory cytokines, as well as antidepressive and anxiolytic effects. Moreover, the PPAR-α and CB1 receptor antagonists blocked the behavioral and antinociceptive effects of um-PEA. Our findings suggest that um-PEA is a promising adjunct in CIPN and associated mood disorders through the activation of PPAR-α, which influences the endocannabinoid system.

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N-(4-Methoxy-2-nitrophenyl)hexadecanamide, a palmitoylethanolamide analogue, reduces formalin-induced nociception

Cited by 10 publications

References 53 publications

Acute administration of a cannabinoid CB1 receptor antagonist impairs stress-induced antinociception in fish

Acute administration of a cannabinoid CB1 receptor antagonist impairs stress-induced antinociception in fish

Some Prospective Alternatives for Treating Pain: The Endocannabinoid System and Its Putative Receptors GPR18 and GPR55

The Beneficial Effects of Ultramicronized Palmitoylethanolamide in the Management of Neuropathic Pain and Associated Mood Disorders Induced by Paclitaxel in Mice

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