Synthesis and biological evaluation of aryl isoxazole derivatives as metabotropic glutamate receptor 1 antagonists: A potential treatment for neuropathic pain

Title
Synthesis and biological evaluation of aryl isoxazole derivatives as metabotropic glutamate receptor 1 antagonists: A potential treatment for neuropathic pain
Authors
조경희김태훈손우승서선희민선준조용서금교창정규성고훈영이지연배애님
Keywords
mGluR1 antagonist; Metabotropic glutamate receptor; Neuropathic pain; Schizophrenia; Aryl isoxazole
Issue Date
2015-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 25, NO 6, 1324-1328
Abstract
Glutamate is the major excitatory neurotransmitter and known to activate the metabotropic and ionotropic glutamate receptors in the brain. Among these glutamate receptors, metabotropic glutamate receptor 1 (mGluR1) has been implicated in various brain disorders including anxiety, schizophrenia and chronic pain. Several studies demonstrated that the blockade of mGluR1 signaling reduced pain responses in animal models, suggesting that mGluR1 is a promising target for the treatment of neuropathic pain. In this study, we have developed mGluR1 antagonists with an aryl isoxazole scaffold, and identify several compounds that are orally active in vivo. We believe that these compounds can serve as a useful tool for the investigation of the role of mGluR1 and a promising lead for the potential treatment of neuropathic pain.
URI
http://pubs.kist.re.kr/handle/201004/49843
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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