Evolution in pharmacologic thinking around the natural analgesic palmitoylethanolamide: from nonspecific resistance to PPAR-α agonist and effective nutraceutical

@article{Hesselink2013EvolutionIP,
  title={Evolution in pharmacologic thinking around the natural analgesic palmitoylethanolamide: from nonspecific resistance to PPAR-$\alpha$ agonist and effective nutraceutical},
  author={Jan M Keppel Hesselink},
  journal={Journal of Pain Research},
  year={2013},
  volume={6},
  pages={625 - 634}
}
  • J. Hesselink
  • Published 8 August 2013
  • Biology, Medicine
  • Journal of Pain Research
The history of development of new concepts in pharmacology is a highly interesting topic. This review discusses scientific insights related to palmitoylethanolamide (PEA) and its progression over a period of six decades, especially in light of the work of the science sociologists, Ludwig Fleck and Thomas Kuhn. The discovery of the cannabis receptors and the nuclear peroxisome proliferator-activated receptors was the beginning of a completely new understanding of many important homeostatic… Expand
Palmitoylethanolamide: A Natural Compound for Health Management
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Palmitoylethanolamide: A Useful Adjunct in Chemotherapy ProvidingAnalgesia and Neuroprotection
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TLDR
6 clinical trials in a total of nearly 4000 people were performed and published last century, specifically studying PEA as a therapy for influenza and the common cold, and the results support the effectiveness and safety of PEA in flu and respiratory infections. Expand
Professor Rita Levi-Montalcini on Nerve Growth Factor, Mast Cells and Palmitoylethanolamide, an Endogenous Anti-Inflammatory and Analgesic Compound
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PEA has been evaluated since 1993 in a variety of pain indications such as sciatic pain, low back pain, diabetic pain, neuropathic pain, pain due to arthritis in a total of 2000 patients and is therefore the best-documented nutraceutical around. Expand
The palmitoylethanolamide and oleamide enigmas : are these two fatty acid amides cannabimimetic?
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PEA is a sleep inducing lipid whose mechanism of action is far from being understood and although it does not bind with high affinity to CB1 or CB2 receptors, it exhibits some cannabimimetic actions which could be explained at least in part by entourage effects. Expand
New Targets in Pain, Non-Neuronal Cells, and the Role of Palmitoyletha- nolamide
Persistent pain in neuropathic conditions is often quite refractory to conventional analgesic therapy, with most patients obtaining, at best, only partial relief of symptoms. The tendency stillExpand
Palmitoylethanolamide Is a Disease-Modifying Agent in Peripheral Neuropathy: Pain Relief and Neuroprotection Share a PPAR-Alpha-Mediated Mechanism
TLDR
Results strongly suggest that PEA, via a PPAR-α-mediated mechanism, can directly intervene in the nervous tissue alterations responsible for pain, starting to prevent macrophage infiltration. Expand
Molecular evidence for the involvement of PPAR-δ and PPAR-γ in anti-inflammatory and neuroprotective activities of palmitoylethanolamide after spinal cord trauma
TLDR
It is indicated that PPAR-δ and PPar-γ can also contribute to the anti-inflammatory activity of PEA in SCI, as evaluated by the degree of spinal cord inflammation and tissue injury, neutrophil infiltration, proinflammmatory cytokine, inducible nitric oxide synthase expression and motor function. Expand
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The late 1950s several workers showed that arachis and some other oils contained very potent anti-inflammatory components quite apart from the polyunsaturated fatty acids, which suggests that the supposed efficacy of these acids in some clinical situations could be due to trace substances rather than the lipid itself. Expand
Effects of Palmitoylethanolamide on Signaling Pathways Implicated in the Development of Spinal Cord Injury
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It is indicated that PEA reduces inflammation and tissue injury associated with SCI and suggest a regulatory role for endogenous PPAR-α signaling in the inflammatory response associated with spinal cord trauma. Expand
Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α
TLDR
PEA treatment results in decreased numbers of infiltrating astrocytes during Aβ challenge, resulting in significant neuroprotection, and could represent a promising pharmacological tool because it is able to reduce Aβ-evoked neuroinflammation and attenuate its neurodegenerative consequences. Expand
Peroxisome Proliferator-Activated Receptor α Mediates Acute Effects of Palmitoylethanolamide on Sensory Neurons
TLDR
Data support the conclusion that the activity of DRG neurons is rapidly modulated by PEA through a PPARα-dependent mechanism, and agents that increase theActivity of PPAR α may provide a therapeutic strategy to reduce tumor-evoked pain. Expand
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