Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors

FEBS Letters

Di Marzo, Vincenzo²  De Petrocellis, Luciano¹  Davis, John B³ 

[1] Endocannabinoid Research Group, Istituto di Cibernetica, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Ex-comprensorio Olivetti, Fabbricato 70, 80078 Pozzuoli (Naples), Italy;Istituto per la Chimica di Molecole di Interesse Biologico, Consiglio Nazionale delle Ricerche, Via Campi Flegrei 34, Ex-comprensorio Olivetti, Fabbricato 70, 80078 Pozzuoli (Naples), Italy;Neurology-CEDD, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK

关键词: Endocannabinoid;    Vanilloid;    Receptor;    Cannabinoid;    Capsaicin;    Calcium;    AEA;    arachidonoylethanolamide;    PEA;    palmitoylethanolamide;    HEK;    human embryonic kidney;    hVR1;    human vanilloid receptor type 1;    CB1;    cannabinoid receptor type 1;    CB2;    cannabinoid receptor type 2;    FAAH;    fatty acid amide hydrolase;    BSA;    bovine serum albumin;    RTX;    resiniferatoxin;    [Ca2+]i;    intracellular calcium concentration;   

DOI  :  10.1016/S0014-5793(01)02934-9

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

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 Ca²⁺ 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.

【 授权许可】

Unknown