First demonstration of in vivo mapping for regional brain monoacylglycerol lipase using PET with [¹¹C]SAR127303.

ABSTRACT: Monoacylglycerol lipase (MAGL) is a main regulator of the endocannabinoid system within the central nervous system (CNS). Recently, [¹¹C]SAR127303 was developed as a promising radioligand for MAGL imaging. In this study, we aimed to quantify regional MAGL concentrations in the rat brain using positron emission tomography (PET) with [¹¹C]SAR127303. An irreversible two-tissue compartment model (2-TCMi, k₄ = 0) analysis was conducted to estimate quantitative parameters (k₃, K_i^2-TCMi, and λk₃). These parameters were successfully obtained with high identifiability (<10 %COV) for the following regions ranked in order from highest to lowest: cingulate cortex > striatum > hippocampus > thalamus > cerebellum > hypothalamus

SUBMITTER: Yamasaki T 

PROVIDER: S-EPMC5976552 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature