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
- 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
- 남민아; 김태훈; 곽진숙; 서선희; 고민경; 임은정; 민선준; 조용서; 금교창; 백두종; 이지연; 배애님
- mGluR1; Metabotropic glutamate receptor; Neuropathic pain; Thiophene derivatives
- Issue Date
- European journal of medicinal chemistry
- VOL 97, 245-258
- 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.
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