Palmitoyl Ethanolamide-d₄

Palmitoyl ethanolamide-d₄ (PEA-d₄) is intended for use as an internal standard for the quantification of PEA (Item No. 90350) by GC- or LC-MS. PEA is an endogenous fatty N-acyl ethanolamine and a derivative of the endocannabinoid arachidonoyl ethanolamide (AEA; Item No. 90050).^1,2 It selectively activates peroxisome proliferator-activated receptor α (PPARα; EC₅₀ = 3.1 µM) over PPARβ/δ and PPARγ in HeLa cells expressing the human receptors.³ PEA binds to RBL-2H3 basophil membranes (IC₅₀ = 1 nM), which endogenously express cannabinoid 2 (CB₂), but not CB₁, receptors, and inhibits antigen-induced serotonin release from RBL-2H3 cells (EC₅₀ = 0.27 µM).² It prevents decreases in paw withdrawal latency in a radiant heat hypersensitivity test, an effect that can be reversed by the CB₁ receptor antagonist SR141716 (rimonabant; Item No. 9000484), PPARγ antagonist GW 9662 (Item No. 70785), and transient receptor potential vanilloid 1 (TRPV1) antagonist capsazepine (Item No. 10007518), in a mouse model of neuropathic pain induced by chronic constriction injury of the sciatic nerve.⁴ PEA (10 mg/kg) decreases carrageenan-induced paw edema in wild-type, but not Ppara^-/-, mice.³ It inhibits tonic convulsions induced by pentylenetetrazole (PTZ; Item No. 18682) in rats when administered at a dose of 40 mg/kg.⁵ Formulations containing palmitoyl ethanolamide have been used as dietary supplements.

WARNING This product is not for human or veterinary use.