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HYP-1, a novel diamide compound, relieves inflammatory and neuropathic pain in rats

Title
HYP-1, a novel diamide compound, relieves inflammatory and neuropathic pain in rats
Authors
Kam Y.L.Back S.K.Kang B.Kim Y.-Y.Kim H.-J.Rhim H.Nah S.-Y.Chung J.-M.Kim D.H.Choi J.-S.Na H.S.Choo H.-Y.P.
Ewha Authors
정준모박혜영김화정
SCOPUS Author ID
정준모scopus; 박혜영scopus; 김화정scopus
Issue Date
2012
Journal Title
Pharmacology Biochemistry and Behavior
ISSN
0091-3057JCR Link
Citation
vol. 103, no. 1, pp. 33 - 42
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
In the present study, we investigated whether a novel compound, 2-(2-(4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-oxoethylamino)-N-(3,4, 5-trimethoxybenzyl)acetamide (HYP-1), is capable of binding to voltage-gated sodium channels (VGSCs) and evaluated both its inhibitory effect on Na + currents of the rat dorsal root ganglia (DRG) sensory neuron and its in vivo analgesic activity using rat models of inflammatory and neuropathic pain. HYP-1 showed not only high affinity for rat sodium channel (site 2), but also potent inhibitory activity against the TTX-R Na+ currents of the rat DRG sensory neuron. HYP-1 co-injected with formalin (5%, 50 μl) under the plantar surface of rat hind paw dose-dependently reduced spontaneous pain behaviors during both the early and late phases. This result was confirmed by c-Fos immunofluorescence in the L4-5 spinal segments. A large number of c-Fos-positive neurons were observed in rat injected with a mixture of formalin and vehicle, but not in rat treated with a mixture of formalin and HYP-1. In addition, the effectiveness of HYP-1 (6 and 60 mg/kg, i.p.) in suppression of neuropathic pain, such as mechanical, cold and warm allodynia, induced by rat tail nerve injury was investigated. HYP-1 showed limited selectivity over hERG, N-type and T-type channels. Our present results indicate that HYP-1, as a VGSC blocker, has potential analgesic activities against nociceptive, inflammatory and neuropathic pain. © 2012 Elsevier Inc.
DOI
10.1016/j.pbb.2012.07.010
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자연과학대학 > 생명과학전공 > Journal papers
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