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首页> 外文期刊>Biochemistry >Synthetic muO-conotoxin MrVIB blocks TTX-resistant sodium channel NaV1.8 and has a long-lasting analgesic activity.
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Synthetic muO-conotoxin MrVIB blocks TTX-resistant sodium channel NaV1.8 and has a long-lasting analgesic activity.

机译：合成的muO-芋螺毒素MrVIB阻断耐TTX的钠通道NaV1.8，并具有持久的镇痛作用。

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摘要

MuO-conotoxin MrVIB is a blocker of voltage-gated sodium channels, including TTX-sensitive and -resistant subtypes. A comprehensive characterization of this peptide has been hampered by the lack of sufficient synthetic material. Here, we describe the successful chemical synthesis and oxidative folding of MrVIB that has made an investigation of the pharmacological properties and therapeutic potential of the peptide feasible. We show for the first time that synthetic MrVIB blocks rat NaV1.8 sodium channels and has potent and long-lasting local anesthetic effects when tested in two pain assays in rats. Furthermore, MrVIB can block propagation of action potentials in A- and C-fibers in sciatic nerve as well as skeletal muscle in isolated preparations from rat. Our work provides the first example of analgesia produced by a conotoxin that blocks sodium channels. The emerging diversity of antinociceptive mechanisms targeted by different classes of conotoxins is discussed.
机译：MuO-conotoxin MrVIB是电压门控钠通道的阻滞剂，包括TTX敏感和耐药亚型。缺乏足够的合成材料阻碍了该肽的全面表征。在这里，我们描述了MrVIB的成功化学合成和氧化折叠，这使得对该肽的药理特性和治疗潜力的研究成为可能。我们首次展示了合成的MrVIB在大鼠的两种疼痛试验中进行测试时能阻断大鼠NaV1.8钠通道，并具有有效而持久的局部麻醉作用。此外，MrVIB可以阻断大鼠分离制剂中坐骨神经A和C纤维以及骨骼肌中动作电位的传播。我们的工作提供了由阻断钠通道的芋螺毒素产生的镇痛作用的第一个例子。讨论了不同类别的芋螺毒素靶向的抗伤害感受机制的新兴多样性。

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