Effects of Palmitoylethanolamide on Aqueous Humor Outflow

Kumar, Akhilesh; Qiao, Zhuanhong; Kumar, Pritesh; Song, Zhao-Hui

doi:10.1167/iovs.11-9294

Cited by 28 publications

(22 citation statements)

References 41 publications

(83 reference statements)

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“…Romano & Lograno () also showed a time‐dependent vasorelaxant response to anandamide and PEA in the bovine ophthalmic artery, but this effect was inhibited by a PPARα, but not a PPARγ, antagonist. Kumar et al () showed that PEA increases aqueous humour outflow in porcine eyes, which is inhibited by PPARα antagonism or knockdown.…”

Section: Physiological Responses To Cannabinoids Mediated By Pparsmentioning

confidence: 99%

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An update on PPAR activation by cannabinoids

O’Sullivan

2016

British J Pharmacology

358

251

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Some cannabinoids activate the different isoforms of PPARs (α, β and γ), as shown through the use of reporter gene assays, binding studies, selective antagonists and knockout studies. Activation of all isoforms, but primarily PPARα and γ, mediates some (but not all) of the analgesic, neuroprotective, neuronal function modulation, anti‐inflammatory, metabolic, anti‐tumour, gastrointestinal and cardiovascular effects of some cannabinoids, often in conjunction with activation of the more traditional target sites of action such as the cannabinoid CB1 and CB2 receptors and the TRPV1 ion channel. PPARs also mediate some of the effects of inhibitors of endocannabinoid degradation or transport. Cannabinoids may be chaperoned to the PPARs by fatty acid binding proteins. The aims of this review are to update the evidence supporting PPAR activation by cannabinoids and to review the physiological responses to cannabinoids that are mediated, and not mediated, by PPAR activation.

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Section: Physiological Responses To Cannabinoids Mediated By Pparsmentioning

confidence: 99%

“…Scuderi et al , ; De Novellis et al , ; Khasabova et al , ; Kumar et al , ; Romano and Lograno, ; Ambrosino et al , ; Citraro et al , ; Esposito et al , ; Borrelli et al , ; Hind et al , …”

Section: Introductionunclassified

An update on PPAR activation by cannabinoids

O’Sullivan

2016

British J Pharmacology

358

251

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“…In rat hippocampal organotypic cultures, PEA was able to reduce b-amyloid-evoked astrogliosis in a manner inhibited by PPARa, but not PPARg, antagonists [103]. PEA, in combination with the FAAH inhibitor URB597, enhanced trabecular meshwork aqueous humor outflow in porcine eyes in vitro [104]. This was not blocked by rimonabant, but was partially reversed by SR144528 or GW6471, a PPARa antagonist.…”

Section: Ppar Activation By Phytocannabinoids and Endocannabinoidsmentioning

confidence: 90%

Common Receptors for Endocannabinoid-Like Mediators and Plant Cannabinoids

Alexander¹

2015

The Endocannabinoidome

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“…One of these is N‐palmitoyl ethanol amide (PEA) an endogenous N‐acylethanolamine widely distributed in different tissues and having the characteristic of increasing its level after stress or injuries associated with neuropathic pain . The biochemical action of PEA involves multiple receptors and its good affinity for peroxisome‐proliferative receptor α (PPARα) and cannabinoid‐like G‐protein‐coupled receptors (GPR55 and GPR119) . The activation of PPARα culminates in switching off the nuclear factor kappa‐B (NF‐κB), blocking the proinflammatory mediators involved in neuropathic pain .…”

mentioning

confidence: 99%

“…14 The biochemical action of PEA involves multiple receptors and its good affinity for peroxisome-proliferative receptor α (PPARα) and cannabinoid-like G-protein-coupled receptors (GPR55 and GPR119). 15 The activation of PPARα culminates in switching off the nuclear factor kappa-B (NF-κB), blocking the proinflammatory mediators involved in neuropathic pain. 16 The concomitant stimulation by PEA of GPR55 and GPR119 reflects its influence on ion channels.…”

mentioning

confidence: 99%

N‐Palmitoyl Ethanol Amide Pharmacological Treatment in Patients With Nonsurgical Lumbar Radiculopathy

Chirchiglia

Paventi

Seminara³

et al. 2018

The Journal of Clinical Pharma

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Palmitoyl ethanol amide (PEA) is an endogenous substance that plays a role in neuropathic pain. In this article, we evaluated both the safety and the efficacy of ultramicronized PEA (um-PEA) in the treatment of low back pain related to nonsurgical lumbar radiculopathy. In this prospective single-blind study, patients with low back pain related to nonsurgical lumbar radiculopathy received the fixed combination acetaminophen/codeine (500 mg + 30 mg/d) for 7 days, and then it was stopped and changed to um-PEA (1200 mg/d) for 30 days. Patients without an improvement in pain or disability started a second cycle of treatment with um-PEA (600 mg/d in tablets) for 30 days and then acetaminophen/codeine for 30 days. A total of 155 patients were included in the analysis. After the first cycle of treatment we recorded an improvement of pain in all patients with mild pain (visual analog scale score from 3-4 to 1) and in 75% of the patients with moderate pain (visual analog scale score from 5-6 to 2). After the second cycle, we recorded an improvement of pain and disability in all patients with moderate pain (P < .01), but in 26% of patients with severe pain we did not record any improvement in disability (P > .05). In conclusion we evaluated the role of um-PEA in patients with lumbar radiculopathy with a long-term follow-up (24 months) and put in evidence the effectiveness and the safety of this formulation in patients with mild and moderate pain.

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Effects of Palmitoylethanolamide on Aqueous Humor Outflow

Abstract: Our results demonstrate that PEA increases aqueous humor outflow through the TM pathway and these effects are mediated by GPR55 and PPARα receptors through activation of p42/44 MAPK.

Cited by 28 publications

References 41 publications

An update on PPAR activation by cannabinoids

An update on PPAR activation by cannabinoids

Common Receptors for Endocannabinoid-Like Mediators and Plant Cannabinoids

N‐Palmitoyl Ethanol Amide Pharmacological Treatment in Patients With Nonsurgical Lumbar Radiculopathy

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