Huwentoxin-IV (HWTX-IV), a peptide with 35 amino acid residues, was discovered in the venom of spider
Ornithoctonus huwena. The peptide had an inhibitory effect on a tetrodotoxin-sensitive (TTX-S) sodium channel with
highly sensitive to Nav1.7, an attractive target for pain release therapy. In this study we further demonstrated the analgesic
effects of HWTX-IV using mouse and rat as an inflammatory pain model and/or a neuropathic pain models. In the both
cases, the analgesic effects of the peptide were dose-dependent, and statistically significant. In the inflammatory model,
100 µg/kg of HWTX-IV produced an efficient reversal of hyperalgesia up to 63.6% after injection of formalin in rats with
the efficiency equivalent to that of morphine at 50 µg/kg, and 200 µg/kg of HWTX-IV produced protective effect up to
55.6% after injection of acetic acid with the efficiency equivalent to that of morphine at 100 µg/kg. In the spinal nerve
model, the peptide produced the longer and higher reversal effect on allodynia than Mexiletine. These results
demonstrated that HWTX-IV released efficiently the acute inflammatory pain and chronic neuropathic pain in these
animals, suggesting that HWTX-IV was a potential and efficient candidate for further clinical drug development against
inflammatory and neuropathic pain.
Keywords: Analgesic, huwentoxin-IV, inflammatory pain, neurotoxin, neuropathic pain.
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