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

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 e...

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Veröffentlicht in:Bulletin of the Korean Chemical Society 2014, Vol.35 (8), p.2304-2310
Hauptverfasser: Kim, Ji Young, Son, Myung-Hee, Choi, Kihang, Baek, Du-Jong, Ko, Min Kyung, Lim, Eun Jeong, Pae, Ae Nim, Keum, Gyochang, Lee, Jae Kyun, Cho, Yong Seo, Choo, Hyunah, Lee, Youn Woo, Moon, Byung Seok, Lee, Byung Cheol, Lee, Ho-Young, Min, Sun-Joon
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Sprache:kor
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Zusammenfassung: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.
ISSN:0253-2964
1229-5949