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Toxins 2014, 6(8), 2363-2378; doi:10.3390/toxins6082363
Article

Synthesis and Analgesic Effects of μ-TRTX-Hhn1b on Models of Inflammatory and Neuropathic Pain

1,†
, 2,†
, 3
, 1
, 1
, 1
, 1
, 3,*  and 2,*
1 College of Chemistry and Chemical Engineering, Hunan Institute of Science and Technology, Yueyang 414006, Hunan, China 2 The Second Xiangya Hospital of Central South University, Changsha 410008, Hunan, China 3 College of Life Sciences, Hunan Normal University, Changsha 410081, Hunan, China These authors contributed equally to this work.
* Authors to whom correspondence should be addressed.
Received: 28 March 2014 / Revised: 17 July 2014 / Accepted: 18 July 2014 / Published: 13 August 2014
(This article belongs to the Special Issue Ion Channel Neurotoxins)
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Abstract

μ-TRTX-Hhn1b (HNTX-IV) is a 35-amino acid peptide isolated from the venom of the spider, Ornithoctonus hainana. It inhibits voltage-gated sodium channel Nav1.7, which has been considered as a therapeutic target for pain. The goal of the present study is to elucidate the analgesic effects of synthetic μ-TRTX-Hhn1b on animal models of pain. The peptide was first synthesized and then successfully refolded/oxidized. The synthetic peptide had the same inhibitory effect on human Nav1.7 current transiently expressed in HEK 293 cells as the native toxin. Furthermore, the analgesic potentials of the synthetic peptide were examined on models of inflammatory pain and neuropathic pain. μ-TRTX-Hhn1b produced an efficient reversal of acute nociceptive pain in the abdominal constriction model, and significantly reduced the pain scores over the 40-min period in the formalin model. The efficiency of μ-TRTX-Hhn1b on both models was equivalent to that of morphine. In the spinal nerve model, the reversal effect of μ-TRTX-Hhn1b on allodynia was longer and higher than mexiletine. These results demonstrated that μ-TRTX-Hhn1b efficiently alleviated acute inflammatory pain and chronic neuropathic pain in animals and provided an attractive template for further clinical analgesic drug design.
Keywords: μ-TRTX-Hhn1b; Nav1.7; analgesic; inflammatory pain; neuropathic pain μ-TRTX-Hhn1b; Nav1.7; analgesic; inflammatory pain; neuropathic pain
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Liu, Y.; Tang, J.; Zhang, Y.; Xun, X.; Tang, D.; Peng, D.; Yi, J.; Liu, Z.; Shi, X. Synthesis and Analgesic Effects of μ-TRTX-Hhn1b on Models of Inflammatory and Neuropathic Pain. Toxins 2014, 6, 2363-2378.

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