Journal Article 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).

Fujinaga, Masayuki  ,  Yamasaki, Tomoteru  ,  Nengaki, Nobuki  ,  Ogawa, Masanao  ,  Kumata, Katsushi  ,  Shimoda, Yoko  ,  Yui, Joji  ,  Xie, Lin  ,  Zhang, Yiding  ,  Kawamura, Kazunori  ,  Ming-Rong, Zhang

26 ( 2 )  , pp.370 - 374 , 2016-01 , Elsevier Science Ltd
ISSN:0960-894x
Description
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 [(11)C]1 as a novel positron emission tomography ligand and to evaluate its binding ability for mGluR4. Using stannyl precursor 3, [(11)C]1 was efficiently synthesized by introducing an [(11)C]methyl group into a pyrimidine ring via C-(11)C coupling and deprotection reactions, in 16±6% radiochemical yield (n=10). At the end of synthesis, 0.54-1.10GBq of [(11)C]1 was acquired with >98% radiochemical purity and 90-120GBq/μmol of specific activity. In vitro autoradiography and ex vivo biodistribution study in rat brains showed specific binding of [(11)C]1 in the cerebellum, striatum, thalamus, cerebral cortex, and medulla oblongata, which showed dose-dependent decreases by administration with multi-dose of unlabeled 1.

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