Endocannabinoid Transporter Inhibitors

This review gives an overview of the current knowledge of endocannabinoid transporter, its biochemical characterization, localization and most relevant features including its role in the uptake of both anandamide and 2-arachidonoylglycerol and its interaction with the vanilloid system. Also, a major emphasis is laid on the structure-affinity relationship studies which have led to novel and more potent and selective inhibitors of the endocannabinoid transporter. Special attention is also paid to the promising therapeutic applications of these inhibitors since the transporter has been revealed as an important target for the treatment of diverse pathologies such as neurodegenerative diseases.