Journal Article Synthesis and In Vitro Evaluation of Three Novel Radiotracers for Imaging of Metabotropic Glutamate Receptor Subtype 2 in Rat Brain

Kumata, Katsushi  ,  Yamasaki, Tomoteru  ,  Hatori, Akiko  ,  Zhang, Yiding  ,  Mori, Wakana  ,  Fujinaga, Masayuki  ,  Xie, Lin  ,  Ohkubo, Takayuki  ,  Nengaki, Nobuki  ,  Ming-Rong, Zhang

27 ( 14 )  , pp.3139 - 3143 , 2017-05 , Elsevier
The purpose of this study was to develop three new radiotracers, 1-(cyclopropylmethyl)-4-([11C/18F]substituted-phenyl)piperidin-1-yl-2-oxo-1,2-dihydropyridine-3-carbonitrile ([11C]1, [11C]2, and [18F]4), and to examine their specific bindings with metabotropic glutamate receptor subtype 2 (mGluR2) in rat brain sections by using in vitro autoradiography. These compounds were found to possess potent in vitro binding affinities (Ki: 8.0-34.1nM) for mGluR2 in rat brain homogenate. [11C]1, [11C]2, and [18F]4 were synthesized by [11C/18F]alkylation of the corresponding phenol precursors with [11C]methyl iodide or [18F]fluoroethyl bromide with >98% radiochemical purity and 80-130GBq/μmol specific activity at the end of synthesis. In vitro autoradiography indicated that these radiotracers showed heterogeneous specific bindings in mGluR2-rich brain regions, such as the cerebral cortex, striatum, hippocampus, and granular layer of the cerebellum.

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