棕榈酰乙醇胺增强了花生四烯酸乙醇胺对人类香草酸受体1的刺激作用。
Palmitoylethanolamide enhances anandamide stimulation of human vanilloid VR1 receptors.
作者信息
De Petrocellis L, Davis J B, Di Marzo V
机构信息
Endocannabinoid Research Group, Istituto di Cibernetica, Consiglio Nazionale delle Ricerche, Pozzuoli, Naples, Italy.
出版信息
FEBS Lett. 2001 Oct 12;506(3):253-6. doi: 10.1016/s0014-5793(01)02934-9.
In human embryonic kidney cells over-expressing the human vanilloid receptor type 1 (VR1), palmitoylethanolamide (PEA, 0.5-10 microM) enhanced the effect of arachidonoylethanolamide (AEA, 50 nM) on the VR1-mediated increase of the intracellular Ca2+ concentration. PEA (5 microM) decreased the AEA half-maximal concentration for this effect from 0.44 to 0.22 microM. 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 microM) 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.
在过表达人1型香草酸受体（VR1）的人胚肾细胞中，棕榈酰乙醇胺（PEA，0.5 - 10微摩尔）增强了花生四烯酸乙醇胺（AEA，50纳摩尔）对VR1介导的细胞内钙离子浓度升高的作用。PEA（5微摩尔）使产生此效应的AEA半数最大浓度从0.44微摩尔降至0.22微摩尔。PEA的作用并非由于抑制AEA水解或与非特异性位点结合，因为牛血清白蛋白（0.01 - 0.25%）能有效抑制AEA活性，且PEA还增强了低浓度VR1激动剂树脂毒素和辣椒素的作用。在特异性结合试验中评估发现，PEA（5微摩尔）增强了AEA对VR1受体的亲和力。这些数据表明，PEA可能是VR1介导的AEA作用的内源性增强剂。
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