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HYP-1, a novel diamide compound, relieves inflammatory and neuropathic pain in rats
- HYP-1, a novel diamide compound, relieves inflammatory and neuropathic pain in rats
- 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
- 정준모; 박혜영; 김화정
- SCOPUS Author ID
- 정준모; 박혜영; 김화정
- Issue Date
- Journal Title
- Pharmacology Biochemistry and Behavior
- vol. 103, no. 1, pp. 33 - 42
- SCI; SCIE; SCOPUS
- 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.
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