Starowicz Katarzyna, Nigam Santosh, Di Marzo Vincenzo
Institute of Biomolecular Chemistry, Endocannabinoid Research Group, C.N.R., Pozzuoli, Naples, Italy.
Pharmacol Ther. 2007 Apr;114(1):13-33. doi: 10.1016/j.pharmthera.2007.01.005. Epub 2007 Feb 2.
Endovanilloids are defined as endogenous ligands and activators of transient receptor potential (TRP) vanilloid type 1 (TRPV1) channels. The first endovanilloid to be identified was anandamide (AEA), previously discovered as an endogenous agonist of cannabinoid receptors. In fact, there are several similarities, in terms of opposing actions on the same intracellular signals, role in the same pathological conditions, and shared ligands and tissue distribution, between TRPV1 and cannabinoid CB(1) receptors. After AEA and some of its congeners (the unsaturated long chain N-acylethanolamines), at least 2 other families of endogenous lipids have been suggested to act as endovanilloids: (i) unsaturated long chain N-acyldopamines and (ii) some lipoxygenase (LOX) metabolites of arachidonic acid (AA). Here we discuss the mechanisms for the regulation of the levels of the proposed endovanilloids, as well as their TRPV1-mediated pharmacological actions in vitro and in vivo. Furthermore, we outline the possible pathological conditions in which endovanilloids, acting at sometimes aberrantly expressed TRPV1 receptors, might play a role.
内源性香草素被定义为瞬时受体电位（TRP）香草酸受体1型（TRPV1）通道的内源性配体和激活剂。首个被鉴定出的内源性香草素是花生四烯乙醇胺（AEA），它之前被发现是大麻素受体的内源性激动剂。事实上，TRPV1和大麻素CB(1)受体在对相同细胞内信号的相反作用、在相同病理状况下的作用以及共享的配体和组织分布方面存在若干相似之处。继AEA及其一些同系物（不饱和长链N-酰基乙醇胺）之后，至少还有另外两类内源性脂质被认为可作为内源性香草素发挥作用：（i）不饱和长链N-酰基多巴胺和（ii）花生四烯酸（AA）的一些脂氧合酶（LOX）代谢产物。在此，我们讨论所提出的内源性香草素水平的调节机制，以及它们在体外和体内由TRPV1介导的药理作用。此外，我们概述了内源性香草素可能发挥作用的病理状况，这些内源性香草素有时作用于异常表达的TRPV1受体。
