Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 박혜영 | - |
dc.date.accessioned | 2017-02-15T08:02:56Z | - |
dc.date.available | 2017-02-15T08:02:56Z | - |
dc.date.issued | 2017 | - |
dc.identifier.issn | 0091-3057 | - |
dc.identifier.other | OAK-20043 | - |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/234475 | - |
dc.description.abstract | Clinical 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.language | English | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | Sodium channel inhibitor | - |
dc.subject | Spinal cord injury | - |
dc.subject | Tail nerve injury | - |
dc.subject | Neuropathic pain | - |
dc.subject | Microglia | - |
dc.subject | Astrocyte | - |
dc.title | HYP-17, a novel voltage-gated sodium channel blocker, relieves inflammatory and neuropathic pain in rats | - |
dc.type | Article | - |
dc.relation.volume | 153 | - |
dc.relation.index | SCIE | - |
dc.relation.index | SCOPUS | - |
dc.relation.startpage | 116 | - |
dc.relation.lastpage | 129 | - |
dc.relation.journaltitle | PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR | - |
dc.identifier.doi | 10.1016/j.pbb.2016.12.013 | - |
dc.identifier.wosid | WOS:000393248100012 | - |
dc.identifier.scopusid | 2-s2.0-85007425419 | - |
dc.author.google | Lee, Jee Youn | - |
dc.author.google | Kam, Yoo Lim | - |
dc.author.google | Oh, Jungae | - |
dc.author.google | Kim, Dong Hyun | - |
dc.author.google | Choi, Jin-Sung | - |
dc.author.google | Choi, Hae Young | - |
dc.author.google | Han, Sungmin | - |
dc.author.google | Youn, Inchan | - |
dc.author.google | Choo, Hea-Young Park | - |
dc.author.google | Yune, Tae Young | - |
dc.contributor.scopusid | 박혜영(34972649500;57200273796) | - |
dc.date.modifydate | 20230411110509 | - |