First demonstration of in vivo mapping for regional brain monoacylglycerol lipase using PET with [11C]SAR127303.
Neuroimage
; 176: 313-320, 2018 08 01.
Article
en En
| MEDLINE
| ID: mdl-29738910
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, k4â¯=â¯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 cortexâ¯>â¯striatumâ¯>â¯hippocampusâ¯>â¯thalamusâ¯>â¯cerebellumâ¯>â¯hypothalamusâ¯≈â¯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 (râ¯>â¯0.4, Pâ¯<â¯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.
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MEDLINE
Asunto principal:
Encéfalo
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Tomografía de Emisión de Positrones
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Neuroimagen
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Modelos Teóricos
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Monoacilglicerol Lipasas
Límite:
Animals
Idioma:
En
Revista:
Neuroimage
Asunto de la revista:
DIAGNOSTICO POR IMAGEM
Año:
2018
Tipo del documento:
Article