McFarland Matthew J, Barker Eric L
Department of Medical Chemistry and Molecular Pharmacology, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN 47907-2091, USA.
Pharmacol Ther. 2004 Nov;104(2):117-35. doi: 10.1016/j.pharmthera.2004.07.008.
N-Arachidonylethanolamine (anandamide) is an endogenous agonist of the cannabinoid CB1 and CB2 receptors and displays many of the same receptor-mediated physiological effects as delta9-tetrahydrocannabinol (delta9-THC), the active component of marijuana. As with any neurotransmitter, there must be tight control of anandamide receptor-mediated signaling and a means of rapid removal of the molecule from the system. Thus, the process by which anandamide is transported into the cell for metabolism has been a topic of much interest and has been implicated as a potential drug target in the treatment of several disease states that are reported to have an association with the endocannabinoid system. In this review, we will discuss the current models proposed for the mechanism of anandamide transport, the progress that has been made in the development of compounds that specifically inhibit anandamide transport, the observed effects of anandamide transport inhibition in vivo, and finally, potential therapeutic applications of compounds that inhibit anandamide transport.
N-花生四烯酸乙醇胺（花生四烯酸乙醇胺）是大麻素CB1和CB2受体的内源性激动剂，具有许多与δ9-四氢大麻酚（δ9-THC）相同的受体介导的生理效应，δ9-THC是大麻的活性成分。与任何神经递质一样，必须严格控制花生四烯酸乙醇胺受体介导的信号传导，并有一种从系统中快速清除该分子的方法。因此，花生四烯酸乙醇胺被转运到细胞内进行代谢的过程一直是人们非常感兴趣的话题，并且被认为是治疗几种据报道与内源性大麻素系统相关的疾病状态的潜在药物靶点。在这篇综述中，我们将讨论目前提出的花生四烯酸乙醇胺转运机制模型、特异性抑制花生四烯酸乙醇胺转运的化合物开发进展、体内花生四烯酸乙醇胺转运抑制的观察效果，以及最后，抑制花生四烯酸乙醇胺转运的化合物的潜在治疗应用。
