The anti-inflammatory mediator palmitoylethanolamide enhances the levels of 2-arachidonoyl-glycerol and potentiates its actions at TRPV1 cation channels
Laboratory studyHumansDogsOther animals
- Design
- Laboratory study
- Subjects
- Human keratinocyte cultures; Ascaris-hypersensitive beagle dogs given a single oral dose; healthy human volunteers given a single oral dose; HEK-293 cells expressing TRPV1
- Dose used in the study
- Dogs: ultramicronised PEA 30 mg/kg once. Volunteers: micronised PEA 300 mg once. Cells: 10 to 20 micromolar
- Duration
- Blood sampled over 8 hours in dogs and 6 hours in people
- What was measured
- Plasma and cell levels of 2-arachidonoylglycerol (2-AG) by mass spectrometry; calcium responses of TRPV1-expressing cells
What the authors reported
Oral PEA raised plasma 2-AG about 2-fold in people and about 20-fold in dogs, and 3-fold in keratinocytes. 2-AG activated TRPV1 channels, and PEA increased the desensitisation of TRPV1 to capsaicin. The authors propose this as one route by which PEA acts without binding cannabinoid receptors itself.
Limits of this study
A mechanism study with small numbers, mostly in cells; the human and dog arms measured a blood marker after one dose, not a clinical effect. Two authors are from Epitech. The entourage effect is a hypothesis this paper supports, not a demonstrated clinical mechanism.
Source
PubMed 25598150 · doi:10.1111/bph.13084
Entry checked against the abstract on PubMed on 2026-09-22. The dose shown is the dose the researchers used. It is not a recommendation. How to read this page.