A novel monoacylglycerol lipase-targeted ¹⁸F-labeled probe for positron emission tomography imaging of brown adipose tissue in the energy network.

ABSTRACT: Monoacylglycerol lipase (MAGL) constitutes a serine hydrolase that orchestrates endocannabinoid homeostasis and exerts its function by catalyzing the degradation of 2-arachidonoylglycerol (2-AG) to arachidonic acid (AA). As such, selective inhibition of MAGL represents a potential therapeutic and diagnostic approach to various pathologies including neurodegenerative disorders, metabolic diseases and cancers. Based on a unique 4-piperidinyl azetidine diamide scaffold, we developed a reversible and peripheral-specific radiofluorinated MAGL PET ligand [¹⁸F]FEPAD. Pharmacokinetics and binding studies on [¹⁸F]FEPAD revealed its outstanding specificity and selectivity towards MAGL in brown adipose tissue (BAT) - a tissue that is known to be metabolically active. We employed

SUBMITTER: Cheng R 

PROVIDER: S-EPMC9622914 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature