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Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain

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dc.contributor.authorKim, Younghee-
dc.contributor.authorSon, Jiwon-
dc.contributor.authorKim, Juhyeon-
dc.contributor.authorBaek, Du-Jong-
dc.contributor.authorLee, Yong Sup-
dc.contributor.authorLim, Eun Jeong-
dc.contributor.authorLee, Jae Kyun-
dc.contributor.authorPae, Ae Nim-
dc.contributor.authorMin, Sun-Joon-
dc.contributor.authorCho, Yong Seo-
dc.date.accessioned2021-06-22T23:22:49Z-
dc.date.available2021-06-22T23:22:49Z-
dc.date.created2021-01-21-
dc.date.issued2014-06-
dc.identifier.issn0009-2363-
dc.identifier.urihttps://scholarworks.bwise.kr/erica/handle/2021.sw.erica/22823-
dc.description.abstractA series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 mu m against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia.-
dc.language영어-
dc.language.isoen-
dc.publisherPharmaceutical Society of Japan-
dc.titleSynthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain-
dc.typeArticle-
dc.contributor.affiliatedAuthorMin, Sun-Joon-
dc.identifier.doi10.1248/cpb.c13-00945-
dc.identifier.scopusid2-s2.0-84903395807-
dc.identifier.wosid000336559100002-
dc.identifier.bibliographicCitationChemical and Pharmaceutical Bulletin, v.62, no.6, pp.508 - 518-
dc.relation.isPartOfChemical and Pharmaceutical Bulletin-
dc.citation.titleChemical and Pharmaceutical Bulletin-
dc.citation.volume62-
dc.citation.number6-
dc.citation.startPage508-
dc.citation.endPage518-
dc.type.rimsART-
dc.type.docTypeArticle-
dc.description.journalClass1-
dc.description.isOpenAccessN-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Multidisciplinary-
dc.relation.journalWebOfScienceCategoryPharmacology & Pharmacy-
dc.subject.keywordPlusMETABOTROPIC GLUTAMATE RECEPTORS-
dc.subject.keywordPlusGLUTAMATE-RECEPTOR-1 ANTAGONISTS-
dc.subject.keywordPlusPHARMACOLOGICAL CHARACTERIZATION-
dc.subject.keywordPlusIN-VITRO-
dc.subject.keywordPlusDERIVATIVES-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusMICE-
dc.subject.keywordPlusPROFILES-
dc.subject.keywordPlusLY456236-
dc.subject.keywordPlusEFFICACY-
dc.subject.keywordAuthorglutamate-
dc.subject.keywordAuthormetabotropic glutamate receptor (mGluR)-
dc.subject.keywordAuthorquinoline-
dc.subject.keywordAuthorneuropathic pain-
dc.subject.keywordAuthorspinal nerve ligation (SNL) model-
dc.identifier.urlhttps://www.jstage.jst.go.jp/article/cpb/62/6/62_c13-00945/_article-
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