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Discovery and biological evaluation of tetrahydrothieno[2,3-c]pyridine derivatives as selective metabotropic glutamate receptor 1 antagonists for the potential treatment of neuropathic pain
- Authors
- Nam, Mina; Kim, TaeHun; Kwak, Jinsook; Seo, Seon Hee; Ko, Min Kyung; Lim, Eun Jeong; Min, Sun-Joon; Cho, Yong Seo; Keum, Gyochang; Baek, Du-Jong; Lee, Jiyoun; Pae, Ae Nim
- Issue Date
- Jun-2015
- Publisher
- Elsevier BV
- Keywords
- mGluR1 antagonist; Metabotropic glutamate receptor; Neuropathic pain; Thiophene derivatives
- Citation
- European Journal of Medicinal Chemistry, v.97, pp 245 - 258
- Pages
- 14
- Indexed
- SCI
SCIE
SCOPUS
- Journal Title
- European Journal of Medicinal Chemistry
- Volume
- 97
- Start Page
- 245
- End Page
- 258
- ISSN
- 0223-5234
1768-3254
- Abstract
- Metabotropic glutamate receptor 1 (mGluR1) has been a prime target for drug discovery due to its heavy involvement in various brain disorders. Recent studies suggested that mGluR1 is associated with chronic pain and can serve as a promising target for the treatment of neuropathic pain. In an effort to develop a novel mGluR1 antagonist, we designed and synthesized a library of compounds with tetrahydrothieno [2,3-c]pyridine scaffold. Among these compounds, compound 9b and 10b showed excellent antagonistic activity in vitro and demonstrated pain-suppressing activity in animal models of pain. Both compounds were orally active, and compound 9b exhibited a favorable pharmacokinetic profile in rats. We believe that these compounds can provide a promising lead compound that is suitable for the potential treatment of neuropathic pain. (C) 2015 Elsevier Masson SAS. All rights reserved.
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Related Researcher
- Min, Sun Joon
- ERICA 공학대학 (ERICA 에너지바이오학과)