Home Metabolism PPAR activator Palmitoylethanolamide For research use only.

Palmitoylethanolamide

Synonyms: Palmidrol|N-palmitoylethanolamine

Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.

Palmitoylethanolamide Chemical Structure

Palmitoylethanolamide Chemical Structure

CAS No. 544-31-0

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Palmitoylethanolamide Related Products

Signaling Pathway

PPAR Signaling Pathways

PPAR Signaling Pathway

Biological Activity

Description Palmitoylethanolamide (PEA, Palmidrol, N-palmitoylethanolamine) is an endogenous fatty acid amide and selectively activates PPAR-α in vitro with an EC50 value of 3.1±0.4 μM.
Targets
PPARα [1]
(In HeLa cells)
3.1 μM(EC50)
In vitro
In vitro PEA protects cultured mouse cerebellar granule cells from glutamate toxicity and enhances microglial cell motility. In the mitochondrial fraction from cells stimulated with PEA, steroidogenic acute regulatory protein (StAR) and cytochrome P450 enzyme(P450scc) expression increases, both comprising proteins considered to be involved in crucial steps of neurosteroid formation. Moreover, PEA shows a protective effect, reducing malondialdehyde formation in cells treated with L-buthionine-(S,R)-sulfoximine, a glutathione depletor and the effect of PEA is partially inhibited by finasteride, a 5a-reductase inhibitor[2].
Cell Research Cell lines Rat C6 glioma cells
Concentrations 10 μM
Incubation Time 24 h
Method C6 glioma cells (300 000⁄P60 dish) or astrocyte primary culture are incubated in serum-free DMEM at 37℃ for at least 24 h before each experiment. Then, cells are treated with PEA (10 μM) for 24 h in serum-free medium, in the presence and absence of GW6471 (10 μM) added 30 min before ethanolamide treatment. The concentration of PEA is chosen on the basis of preliminary experiments, assessing drug efficacy without modifi-cation of cell viability. PEA and GW6471 are first dissolved in absolute ethanol and then diluted with DMEM. The final ethanol concentration was< 0.5%. Mitochondrial protein extracts from C6 or astrocytes are obtained. Alternatively after 24 h of starvation in serum-free DMEM, C6 cells are treated with FIN (100 nM). After 30 min, PEA (10 μM) and⁄or ALLO (3 μM) is added and, 30 min later, are stimulated with BSO (10 mM). After 18 h, MDA is evaluated. In this set of experiments, FIN and⁄or PEA are dissolved in dimethylsulphoxide (DMSO) and then diluted with DMEM (0.1% final DMSO concentration).
In Vivo
In vivo PEA attenuates inflammation in wild-type mice but has no effect in mice deficient in PPAR-α. PEA has been shown to inhibit peripheral inflammation and mast-cell degranulation as well as to exert neuroprotective and antinociceptive effects in rats and mice. These actions are accompanied by changes in nitric oxide production, neutrophil influx, and expression of proinflammatory proteins such as inducible nitric oxide synthase and cyclooxygenase-2[1]. In addition to its known anti-inflammatory activity, PEA regulates many pathophysiological processes, including pain perception, convulsions, and neurotoxicity. In the central nervous system (CNS), where PEA is present at detectable levels, its concentrations significantly increase under pathological conditions, such as excitotoxicity, brain ischaemia and neuroinflammation[2].
Animal Research Animal Models C57BL6 mice, male C57BL6 PPAR-α-/- mice
Dosages 10 mg/kg
Administration i.p
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06040164 Not yet recruiting
PreDiabetes|Diabetes Mellitus Type 2|Obesity|Oral Dysbiosis|Mouth Disease
Fundación Pública Andaluza para la Investigación de Málaga en Biomedicina y Salud
 October 1 2023 --
NCT05849792 Completed
Exercise|Physical Fitness|Depression|Adult ALL|Psychological
University of Cadiz|Consejería de Salud y Familia (Junta de Andalucía)|Institute of Biomedical research and innovation of Cádiz (INIBICA)
 September 1 2019 Not Applicable
NCT03564379 Completed
Healthy
Janssen Research & Development LLC
 June 12 2018 Phase 1
NCT01092845 Completed
Healthy|Sleep
Pfizer
 April 2010 Phase 1
NCT01370720 Unknown status
Irritable Bowel Syndrome
MARIA CRISTINA COMELLI|CM&D Pharma Limited
 February 2010 Phase 2

Chemical Information & Solubility

Molecular Weight 299.49 Formula

C18H37NO2
CAS No. 544-31-0 SDF Download Palmitoylethanolamide SDF
Smiles CCCCCCCCCCCCCCCC(=O)NCCO
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 59 mg/mL

DMSO : 5 mg/mL ( (16.69 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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