864863-72-9Relevant articles and documents
Synthesis and evaluation of 6-[1-(2-[18F]fluoro-3-pyridyl)-5- methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain
Fujinaga, Masayuki,Yamasaki, Tomoteru,Kawamura, Kazunori,Kumata, Katsushi,Hatori, Akiko,Yui, Joji,Yanamoto, Kazuhiko,Yoshida, Yuichiro,Ogawa, Masanao,Nengaki, Nobuki,Maeda, Jun,Fukumura, Toshimitsu,Zhang, Ming-Rong
experimental part, p. 102 - 110 (2011/03/18)
The purpose of this study was to synthesize 6-[1-(2-[18F]fluoro- 3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline ([18F]FPTQ, [18F]7a) and to evaluate its potential as a positron emission tomography ligand for imaging metabotropic glutamate receptor type 1 (mGluR1) in the rat brain. Compound [18F]7a was synthesized by [ 18F]fluorination of 6-[1-(2-bromo-3-pyridyl)-5-methyl-1H-1,2,3- triazol-4-yl]quinoline (7b) with potassium [18F]fluoride. At the end of synthesis, 1280-1830 MBq (n = 8) of [18F]7a was obtained with >98% radiochemical purity and 118-237 GBq/μmol specific activity using 3300-4000 MBq of [18F]F-. In vitro autoradiography showed that [18F]7a had high specific binding with mGluR1 in the rat brain. Biodistribution study using a dissection method and small-animal PET showed that [18F]7a had high uptake in the rat brain. The uptake of radioactivity in the cerebellum was reduced by unlabeled 7a and mGluR1-selective ligand JNJ-16259685 (2), indicating that [18F]7a had in vivo specific binding with mGluR1. Because of a low amount of radiolabeled metabolite present in the brain, [18F]7a may have a limiting potential for the in vivo imaging of mGluR1 by PET.
