Synthesis and Evaluation of (4-Chlorobenzhydryl) Piperazine Amides as Sodium Channel Nav1.7 Inhibitors
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Back, Seung Keun | - |
dc.contributor.author | Kam, Yoo Lim | - |
dc.contributor.author | Oh, Jung Ae | - |
dc.contributor.author | Na, Heung Sik | - |
dc.contributor.author | Ih, Uhtaek | - |
dc.contributor.author | Choo, Hea-Young Park | - |
dc.date.accessioned | 2021-09-04T13:02:26Z | - |
dc.date.available | 2021-09-04T13:02:26Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2015-09 | - |
dc.identifier.issn | 0253-2964 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/92592 | - |
dc.description.abstract | Blockage of voltage-gated sodium channels is used to treat neuropathic pain which is chronic and can become debilitating. Sodium channels Nav1.7-1.9 are especially attractive targets for drug discovery because of the broad therapeutic potential of their modulation. For a neuropathic pain therapy, anticonvulsant like lamotrigine, carbamazepine and a topical anesthetic such as Lidocaine are used. A growing number of clinical reports suggest that selective inhibitors of Nav1.7 are likely to be the powerful analgesics for treating a broad range of pain conditions. Therefore we evaluated 108 amide derivatives synthesized on human Nav1.7 (hNav1.7) by VIPR (voltage/ion probe reader), a fluorescence image plate reader (FLIPR) assay that used voltage-sensor fluorescence dye and stable HEK-293 cell lines expressing hNaV1.7. Ten compounds demonstrated inhibitory activity, and the two most active compounds (5 and 6) had IC50 values of 8-10 mu M. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.subject | PHASE COMBINATORIAL SYNTHESIS | - |
dc.subject | NEUROPATHIC PAIN | - |
dc.subject | NA(V)1.7 | - |
dc.subject | MECHANISMS | - |
dc.subject | BRADYKININ | - |
dc.subject | MUTATIONS | - |
dc.subject | NEURONS | - |
dc.subject | BLOCKER | - |
dc.title | Synthesis and Evaluation of (4-Chlorobenzhydryl) Piperazine Amides as Sodium Channel Nav1.7 Inhibitors | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Na, Heung Sik | - |
dc.identifier.doi | 10.1002/bkcs.10446 | - |
dc.identifier.scopusid | 2-s2.0-84940901251 | - |
dc.identifier.wosid | 000360918600020 | - |
dc.identifier.bibliographicCitation | BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.36, no.9, pp.2290 - 2297 | - |
dc.relation.isPartOf | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.title | BULLETIN OF THE KOREAN CHEMICAL SOCIETY | - |
dc.citation.volume | 36 | - |
dc.citation.number | 9 | - |
dc.citation.startPage | 2290 | - |
dc.citation.endPage | 2297 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.identifier.kciid | ART002028690 | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.subject.keywordPlus | PHASE COMBINATORIAL SYNTHESIS | - |
dc.subject.keywordPlus | NEUROPATHIC PAIN | - |
dc.subject.keywordPlus | NA(V)1.7 | - |
dc.subject.keywordPlus | MECHANISMS | - |
dc.subject.keywordPlus | BRADYKININ | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | NEURONS | - |
dc.subject.keywordPlus | BLOCKER | - |
dc.subject.keywordAuthor | Nav1.7 | - |
dc.subject.keywordAuthor | Voltage Ion Probe Reader assay | - |
dc.subject.keywordAuthor | Formalin test | - |
dc.subject.keywordAuthor | Neuropathic pain | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
(02841) 서울특별시 성북구 안암로 14502-3290-1114
COPYRIGHT © 2021 Korea University. All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.