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Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors
Author(s) -
De Petrocellis Luciano,
Davis John B,
Di Marzo Vincenzo
Publication year - 2001
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(01)02934-9
Subject(s) - palmitoylethanolamide , anandamide , resiniferatoxin , chemistry , trpv1 , receptor , capsaicin , stimulation , endocannabinoid system , endocrinology , capsazepine , medicine , pharmacology , biochemistry , cannabinoid receptor , agonist , biology , transient receptor potential channel
In human embryonic kidney cells over‐expressing the human vanilloid receptor type 1 (VR1), palmitoylethanolamide (PEA, 0.5–10 μM) enhanced the effect of arachidonoylethanolamide (AEA, 50 nM) on the VR1‐mediated increase of the intracellular Ca 2+ concentration. PEA (5 μM) decreased the AEA half‐maximal concentration for this effect from 0.44 to 0.22 μM. The PEA effect was not due to inhibition of AEA hydrolysis or adhesion to non‐specific sites, since bovine serum albumin (0.01–0.25%) potently inhibited AEA activity, and PEA also enhanced the effect of low concentrations of the VR1 agonists resiniferatoxin and capsaicin. PEA (5 μM) enhanced the affinity of AEA for VR1 receptors as assessed in specific binding assays. These data suggest that PEA might be an endogenous enhancer of VR1‐mediated AEA actions.