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
  • 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… 

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References

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Palmitoylethanolamide: A Natural Body-Own Anti-Inflammatory Agent, Effective and Safe against Influenza and Common Cold

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.

Professor Rita Levi-Montalcini on Nerve Growth Factor, Mast Cells and Palmitoylethanolamide, an Endogenous Anti-Inflammatory and Analgesic Compound

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.

The palmitoylethanolamide and oleamide enigmas : are these two fatty acid amides cannabimimetic?

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.

Palmitoylethanolamide Is a Disease-Modifying Agent in Peripheral Neuropathy: Pain Relief and Neuroprotection Share a PPAR-Alpha-Mediated Mechanism

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.

Molecular evidence for the involvement of PPAR-δ and PPAR-γ in anti-inflammatory and neuroprotective activities of palmitoylethanolamide after spinal cord trauma

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.

SLOW ENCEPHALOPATHIES, INFLAMMATORY RESPONSES, AND ARACHIS OIL

Effects of Palmitoylethanolamide on Signaling Pathways Implicated in the Development of Spinal Cord Injury

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.

Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α

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.

Peroxisome Proliferator-Activated Receptor α Mediates Acute Effects of Palmitoylethanolamide on Sensory Neurons

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.

Effects of palmitoylethanolamide on intestinal injury and inflammation caused by ischemia‐reperfusion in mice

It is demonstrated that PEA significantly attenuated the degree of intestinal injury and inflammation caused by I/R injury, and the positive effects of PEA were at least in part dependent on the PPAR‐α pathway.
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