【文章名】Radiosynthesis and preliminary evaluation of 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1
Radiosynthesis and preliminary evaluation of 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide as a new positron emission tomography ligand for metabotropic glutamate receptor subtype 1
[摘要]：The purpose of this study was to develop 4-[F-18]fluoro-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methylbenzamide ([F-18]FITM, [F-18]4) as a new PET ligand for imaging metabotropic glutamate receptor subtype 1 (mGluR1). [F-18]4 was synthesized by [F-18]fluorination of a novel nitro precursor 3 with [F-18]KF in the presence of Kryptofix 222. At the end of synthesis, 429-936 MBq (n = 8) of [F-18]4 was obtained with > 99% radiochemical purity and 204-559 GBq/mu mol specific activity starting from 6.7 to 13.0 GBq of [F-18]F. The brain distribution of [F-18]4 was determined by the in vitro and ex vivo autoradiography using rat brain sections. The in vitro and in vivo specific binding of [F-18]4 to mGluR1 was detected in the cerebellum, thalamus, hippocampus, and striatum. These results suggest that [F-18]4 is a promising PET ligand for the in vivo evaluation of mGluR1. (C) 2011 Elsevier Ltd. All rights reserved.
