864866-10-4Relevant academic research and scientific papers
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.
Discovery and biological profile of 4-(1-aryltriazol-4-yl)-tetrahydropyridines as an orally active new class of metabotropic glutamate receptor 1 antagonist
Ito, Satoru,Satoh, Atsushi,Nagatomi, Yasushi,Hirata, Yukari,Suzuki, Gentaroh,Kimura, Toshifumi,Satow, Akio,Maehara, Shunsuke,Hikichi, Hirohiko,Hata, Mikiko,Kawamoto, Hiroshi,Ohta, Hisashi
experimental part, p. 9817 - 9829 (2009/04/11)
We describe here the discovery and the structure-activity relationship (SAR) of a series of 4-(1-Aryltriazol-4-yl)-tetrahydropyridines as novel mGluR1 antagonists. Our extensive chemical modification of lead compound 2 successfully led to fluoropyridine a
BIARYL DERIVATIVES
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Page/Page column 33-34, (2010/11/26)
The present invention relates to a compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, whrein: R 1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R 2 is halogen atom, a lower alkyl group, etc.; Q 1 is carbon atom or nitrogen atom; Q 2 is carbon atom which may be substituted with oxo group; the formula (III) : is a single bond or a double bond; A is a group selected from the group consisting of the substituent group ±; and R 5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.
DIARYL-SUBSTITUTED FIVE-MEMBERED HETEROCYCLE DERIVATIVE
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Page/Page column 146, (2010/11/24)
The present invention provides the compounds represented by formula (I): (I) or pharmaceutical salts thereof, wherein: X 1 represents oxygen atoms and the like, X 2 represents nitrogen atoms and the like, X 3 represents nitrogen atoms and the like, X 4 represents nitrogen atoms and the like, R 1 represents formula (II-1): wherein X 5 represents sulfur atoms and the like, A 1 represents carbon atoms and the like, A 2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being usefull for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.
