The inactivation of anandamide, the main and most widely studied endocannabinoid to date, has progressively gained support as a process of crucial importance in controlling the biological action both in time and place of this Nacylethanolamine. Within the components that account for the inactivation of anandamide, the membrane anandamide transporter (ANT) constitutes a focus of major attention since it represents one of the most important therapeutic possibilities to enhance the endocannabinoid signalling pathways avoiding the undesirable psychotropic side effects elicit by the action of other direct exogenous agonists in the central nervous system (CNS). The potential implications of the ANT in several CNS-related pathologies, together with the current hypotheses under investigation about its therapeutic applications as well as the most recent additions to the family of compounds able to inhibit the anandamide uptake, are discussed in this review.
Keywords: endogenous cannabinoid system, anandamide transporter, inhibitors of endocannabinoid uptake, therapeutic applications of anandamide uptake inhibitors
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