Synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ targeting metabotropic glutamate receptor 5 (mGluR5)

Ji Young Kim, Myung Hee Son, Kihang Choi, Du Jong Baek, Min Kyung Ko, Eun Jeong Lim, Ae Nim Pae, Gyochang Keum, Jae Kyun Lee, Yong Seo Cho, Hyunah Choo, Youn Woo Lee, Byung Seok Moon, Byung Cheol Lee, Ho Young Lee, Sun Joon Min

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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 [11C]MPEQ 3 proved that accumulation of [ 11C]MPEQ 3 in rat brain was correlated to the localization of the mGluR5.

Original languageEnglish
Pages (from-to)2304-2310
Number of pages7
JournalBulletin of the Korean Chemical Society
Volume35
Issue number8
DOIs
Publication statusPublished - 2014 Aug 20

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Metabotropic Glutamate 5 Receptor
Rats
Brain
Analgesics
Animals
quinoline
Imaging techniques

ASJC Scopus subject areas

  • Chemistry(all)

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Synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ targeting metabotropic glutamate receptor 5 (mGluR5). / 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.

In: Bulletin of the Korean Chemical Society, Vol. 35, No. 8, 20.08.2014, p. 2304-2310.

Research output: Contribution to journalArticle

Kim, JY, Son, MH, Choi, K, Baek, DJ, Ko, MK, Lim, EJ, Pae, AN, Keum, G, Lee, JK, Cho, YS, Choo, H, Lee, YW, Moon, BS, Lee, BC, Lee, HY & Min, SJ 2014, 'Synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ targeting metabotropic glutamate receptor 5 (mGluR5)', Bulletin of the Korean Chemical Society, vol. 35, no. 8, pp. 2304-2310. https://doi.org/10.5012/bkcs.2014.35.8.2304
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. / Synthesis and in vivo evaluation of 5-methoxy-2-(phenylethynyl)quinoline (MPEQ) and [11C]MPEQ targeting metabotropic glutamate receptor 5 (mGluR5). In: Bulletin of the Korean Chemical Society. 2014 ; Vol. 35, No. 8. pp. 2304-2310.
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