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  Synthetic μO-conotoxin MrVIB blocks TTX-resistant sodium channel Na(V)1.8 and has a long-lasting analgesic activity

Bulaj, G., Zhang, M.-M., Green, B. R., Fiedler, B., Layer, R. T., Wei, S., et al. (2006). Synthetic μO-conotoxin MrVIB blocks TTX-resistant sodium channel Na(V)1.8 and has a long-lasting analgesic activity. Biochemistry, 45(23), 7404-7414.

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 Creators:
Bulaj, Gregorz, Author
Zhang, Min-Min, Author
Green, Brad R., Author
Fiedler, Brian, Author
Layer, Richard T., Author
Wei, Sue, Author
Nielsen, Jacob S., Author
Low, Scott J., Author
Klein, Brian D., Author
Wagstaff, John D., Author
Chicoine, Linda, Author
Harty, T. Patrick, Author
Terlau, Heinrich1, Author              
Yoshikami, Doju, Author
Olivera, Baldomero M., Author
Affiliations:
1Molecular and cellular neuropharmacology, Max Planck Institute of Experimental Medicine, Max Planck Society, ou_2173655              

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Free keywords: NEURONAL NA+ CHANNELS; ROOT GANGLION NEURONS; DELTA-CONOTOXIN; NEUROPATHIC PAIN; SENSORY NEURONS; CONUS-MARMOREUS; RECEPTOR-SITE; VENOM; CURRENTS; PEPTIDE
 Abstract: mu O-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 Na(V)1.8 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.

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Language(s): eng - English
 Dates: 2006-06
 Publication Status: Published in print
 Pages: -
 Publishing info: -
 Table of Contents: -
 Rev. Type: Peer
 Identifiers: eDoc: 292180
ISI: 000238047600040
ISI: 000238047600040
 Degree: -

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Title: Biochemistry
  Alternative Title : Biochemistry
Source Genre: Journal
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Pages: - Volume / Issue: 45 (23) Sequence Number: - Start / End Page: 7404 - 7414 Identifier: ISSN: 0006-2960