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Canna~Fangled Abstracts

Endocannabinoid Metabolism and Transport as Drug Targets

By September 21, 2022September 26th, 2022No Comments

. 2023;2576:201-211.

doi: 10.1007/978-1-0716-2728-0_16.

Francesca Ciaramellano 1 2, Federico Fanti 3, Lucia Scipioni 2 4, Mauro Maccarrone 2 4, Sergio Oddi 5 6
Affiliations 

Abstract

The wide distribution of the endocannabinoid system (ECS) throughout the body and its pivotal pathophysiological role offer promising opportunities for the development of novel therapeutic drugs for treating several diseases. However, the need for strategies to circumvent the unwanted psychotropic and immunosuppressive effects associated with cannabinoid receptor agonism/antagonism has led to considerable research in the field of molecular alternatives, other than type-1 and type-2 (CB1/2) receptors, as therapeutic targets to indirectly manipulate this pro-homeostatic system. In this context, the use of selective inhibitors of proteins involved in endocannabinoid (eCB) transport and metabolism allows for an increase or decrease of the levels of N-arachidonoylethanolamine (AEA) and 2-arachidonoylglycerol (2-AG) in the sites where these major eCBs are indeed needed. This chapter will briefly review some preclinical and clinical evidence for the therapeutic potential of ECS pharmacological manipulation.

Keywords: 2-Arachidonoylglycerol, Anandamide, Drug design, Metabolic routes, Signal transduction, Transport mechanisms

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