@article{oai:repo.qst.go.jp:00048941, author = {Yamasaki, Tomoteru and Mori, Wakana and Zhang, Yiding and Hatori, Akiko and Fujinaga, Masayuki and Wakizaka, Hidekatsu and Kurihara, Yusuke and Lu, Wang and Nengaki, Nobuki and Ohya, Tomoyuki and Liang, Huan and Ming-Rong, Zhang and Yamasaki, Tomoteru and Mori, Wakana and Zhang, Yiding and Hatori, Akiko and Fujinaga, Masayuki and Wakizaka, Hidekatsu and Kurihara, Yusuke and Lu, Wang and Nengaki, Nobuki and Ohya, Tomoyuki and Liang, Huan and Ming-Rong, Zhang}, journal = {NeuroImage}, month = {May}, note = {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, Ki2-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 ≈ pons. In vitro autoradiographs using [11C]SAR127303 showed a heterogeneous distribution of radioactivity, as seen in the PET images. The Ki2-TCMi and λk3 values correlated relatively highly with in vitro binding (r > 0.4, P < 0.005). The Ki2-TCMi values showed high correlation and low underestimation (<10%) compared with the slope of a Patlak plot analysis with linear regression (KiPatlak). In conclusion, we successfully estimated regional net uptake value of [11C]SAR127303 reflecting MAGL concentrations in rat brain regions for the first time.}, pages = {313--320}, title = {First demonstration of in vivo mapping for regional brain monoacylglycerol lipase using PET with [11C]SAR127303}, volume = {176}, year = {2018} }