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dc.contributor.authorLee, Jee Youn-
dc.contributor.authorKam, Yoo Lim-
dc.contributor.authorOh, Jungae-
dc.contributor.authorKim, Dong Hyun-
dc.contributor.authorChoi, Jin-Sung-
dc.contributor.authorChoi, Hae Young-
dc.contributor.authorHan, Sungmin-
dc.contributor.authorYoun, Inchan-
dc.contributor.authorChoo, Hea-Young Park-
dc.contributor.authorYune, Tae Young-
dc.date.accessioned2024-01-20T02:30:17Z-
dc.date.available2024-01-20T02:30:17Z-
dc.date.created2021-09-01-
dc.date.issued2017-02-
dc.identifier.issn0091-3057-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/123133-
dc.description.abstractClinical and experimental studies suggest that voltage-gated sodium channels (VGSCs) play a key role in the pathogenesis of neuropathic pain and that blocking agents against these channels can be potentially therapeutic. In the current study, we investigated whether a novel compound, (-)-2-Amino-1-(4-( (4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)-propan-1-one(HYP-17), binds to VGSCs and evaluated its inhibitory effect on Na+ currents of the rat dorsal root ganglia (DRG) sensory neurons and its analgesic effect on inflammatory and neuropathic pain. HYP-17 (10 mu M) reduced both the tetrodotoxin-sensitive (TTX-S) and the TTX-resistant (TTX-R) currents in DRG sensory neurons. However, neither the voltage-dependent activation curves nor the steady-state inactivation curves for TTX-S and TTX-R currents were changed by HYP-17. In rats injected with 5% formalin under the plantar surface of the hind paw, HYP-17 (10 mu g) significantly reduced both the early and late phase spontaneous pain behaviors. Systemic injection with HYP-17 (60 mg/kg, i.p.) also significantly relieved the mechanical, cold, and warm allodynia induced by rat tail nerve injury. Furthermore, HYP-17 (60 mg/kg, i.p.) significantly relieved the central neuropathic pain induced by spinal cord injury (SCI), and inhibited c-Fos expression in lumbar (L) 4-L5 spinal segments. Electrophysiological study showed that HYP-17 significantly attenuated the hyper-responsiveness of lumbar dorsal horn neurons. In addition, HYP-17 significantly reduced the levels of pp38MAPK and p-JNK in microglia and astrocytes, respectively, in the L4-L5 spinal dorsal horn. Therefore, our results indicate that HYP-17 has potential analgesic activities against nociceptive, inflammatory and neuropathic pain. (C) 2016 Published by Elsevier Inc.-
dc.languageEnglish-
dc.publisherPERGAMON-ELSEVIER SCIENCE LTD-
dc.subjectSPINAL-CORD-INJURY-
dc.subjectTETRODOTOXIN-RESISTANT SODIUM-
dc.subjectPRIMARY SENSORY NEURONS-
dc.subjectROOT GANGLION NEURONS-
dc.subjectTERMINAL KINASE JNK-
dc.subjectC-FOS EXPRESSION-
dc.subjectDORSAL-HORN-
dc.subjectSUBCUTANEOUS FORMALIN-
dc.subjectTACTILE ALLODYNIA-
dc.subjectBMK IT2-
dc.titleHYP-17, a novel voltage-gated sodium channel blocker, relieves inflammatory and neuropathic pain in rats-
dc.typeArticle-
dc.identifier.doi10.1016/j.pbb.2016.12.013-
dc.description.journalClass1-
dc.identifier.bibliographicCitationPHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR, v.153, pp.116 - 129-
dc.citation.titlePHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR-
dc.citation.volume153-
dc.citation.startPage116-
dc.citation.endPage129-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000393248100012-
dc.identifier.scopusid2-s2.0-85007425419-
dc.relation.journalWebOfScienceCategoryBehavioral Sciences-
dc.relation.journalWebOfScienceCategoryNeurosciences-
dc.relation.journalWebOfScienceCategoryPharmacology & Pharmacy-
dc.relation.journalResearchAreaBehavioral Sciences-
dc.relation.journalResearchAreaNeurosciences & Neurology-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.type.docTypeArticle-
dc.subject.keywordPlusSPINAL-CORD-INJURY-
dc.subject.keywordPlusTETRODOTOXIN-RESISTANT SODIUM-
dc.subject.keywordPlusPRIMARY SENSORY NEURONS-
dc.subject.keywordPlusROOT GANGLION NEURONS-
dc.subject.keywordPlusTERMINAL KINASE JNK-
dc.subject.keywordPlusC-FOS EXPRESSION-
dc.subject.keywordPlusDORSAL-HORN-
dc.subject.keywordPlusSUBCUTANEOUS FORMALIN-
dc.subject.keywordPlusTACTILE ALLODYNIA-
dc.subject.keywordPlusBMK IT2-
dc.subject.keywordAuthorSodium channel inhibitor-
dc.subject.keywordAuthorSpinal cord injury-
dc.subject.keywordAuthorTail nerve injury-
dc.subject.keywordAuthorNeuropathic pain-
dc.subject.keywordAuthorMicroglia-
dc.subject.keywordAuthorAstrocyte-
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KIST Article > 2017
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