Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4).
Radiosynthesis and evaluation of 5-methyl-N-(4-[(11)C]methylpyrimidin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine ([(11)C]ADX88178) as a novel radioligand for imaging of metabotropic glutamate receptor subtype 4 (mGluR4).
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DOI：
10.1016/j.bmcl.2015.12.008
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发表时间：
2016-01
影响因子：
2.7
通讯作者：
Masayuki Fujinaga;Tomoteru Yamasaki;N. Nengaki;M. Ogawa;K. Kumata;Yoko Shimoda;Joji Yui;Lin Xie;Yiding Zhang;K. Kawamura;Ming-Rong Zhang
中科院分区：
文献类型：
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作者：
Masayuki Fujinaga;Tomoteru Yamasaki;N. Nengaki;M. Ogawa;K. Kumata;Yoko Shimoda;Joji Yui;Lin Xie;Yiding Zhang;K. Kawamura;Ming-Rong Zhang
ADX88178 (1) has been recently developed as a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4). The aim of this study was to develop [11C]1as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor3, [11C]1was efficiently synthesized by introducing an [11C]methyl group into a pyrimidine ring via C–11C coupling and deprotection reactions, in 16 ± 6% radiochemical yield (n= 10). At the end of synthesis, 0.54–1.10 GBq of [11C]1was acquired with >98% radiochemical purity and 90–120 GBq/μmol of specific activity. In vitro autoradiography and ex vivo biodistribution study in rat brains showed specific binding of [11C]1in the cerebellum, striatum, thalamus, cerebral cortex, and medulla oblongata, which showed dose-dependent decreases by administration with multi-dose of unlabeled1.
