Synthesis and in vitro evaluation of three novel radiotracers for imaging of metabotropic glutamate receptor subtype 2 in rat brain |
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Authors: | Katsushi Kumata Tomoteru Yamasaki Akiko Hatori Yiding Zhang Wakana Mori Masayuki Fujinaga Lin Xie Takayuki Okubo Nobuki Nengaki Ming-Rong Zhang |
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Affiliation: | 1. Department of Radiopharmaceuticals Development, National Institute of Radiological Sciences, National Institutes for Quantum and Radiological Science and Technology, Chiba 263-8555, Japan;2. SHI Accelerator Services Co., 1-17-6 Osaki, Shinagawa-ku, Tokyo 141-0032, Japan |
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Abstract: | 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: 8.0–34.1 nM) 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 80–130 GBq/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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Keywords: | In vitro autoradiography Metabotropic glutamate receptor 2 Positron emission tomography Radiotracer Schizophrenia |
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