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http://dx.doi.org/10.5012/bkcs.2014.35.8.2304

Synthesis and In vivo Evaluation of 5-Methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ Targeting Metabotropic Glutamate Receptor 5 (mGluR5)  

Kim, Ji Young (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Son, Myung-Hee (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Choi, Kihang (Department of Chemistry, Korea University)
Baek, Du-Jong (Department of Chemistry, College of Natural Sciences, Sangmyung University)
Ko, Min Kyung (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Lim, Eun Jeong (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Pae, Ae Nim (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Keum, Gyochang (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Lee, Jae Kyun (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Cho, Yong Seo (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Choo, Hyunah (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Lee, Youn Woo (Department of Nuclear Medicine, Seoul National University Bundang Hospital)
Moon, Byung Seok (Department of Nuclear Medicine, Seoul National University Bundang Hospital)
Lee, Byung Cheol (Department of Nuclear Medicine, Seoul National University Bundang Hospital)
Lee, Ho-Young (Department of Nuclear Medicine, Seoul National University Bundang Hospital)
Min, Sun-Joon (Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST))
Publication Information
Bulletin of the Korean Chemical Society / v.35, no.8, 2014 , pp. 2304-2310 More about this Journal
Abstract
The synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) 3 as a potential mGluR5 selective radioligand is described. We have identified MPEQ 3 exhibiting the analgesic effect in the neuropathic pain animal model. The effect of mGluR5 on neuronal activity in rat brain was evaluated through FDG/PET imaging in the presence of MPEQ 3. In addition, the PET study of [$^{11}C$]MPEQ 3 proved that accumulation of [$^{11}C$]MPEQ 3 in rat brain was correlated to the localization of the mGluR5.
Keywords
MPEQ; Metabotropic glutamate receptor 5 (mGluR5); in vivo; PET imaging; Neuropathic pain;
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