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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Córdova, Marco A. Schlumberger, Sébastien Hocking, Henry G. Hartley, Oliver Favreau, Philippe Molgó, Jordi D' Hoedt, Dieter Paolini-bertrand, Marianne Gaertner, Hubert Carlier, Ludovic Leipold, Enrico Boelens, Rolf Stöcklin, Reto Bertrand, Daniel Heinemann, Stefan H. Benoit, Evelyne Tytgat, Jan Markgraf, René |
| Description | Author Affiliation: Favreau P ( Atheris Laboratories, Bernex-Geneva, Switzerland.) |
| Abstract | BACKGROUND AND PURPOSE: The µ-conopeptide family is defined by its ability to block voltage-gated sodium channels (VGSCs), a property that can be used for the development of myorelaxants and analgesics. We characterized the pharmacology of a new µ-conopeptide (µ-CnIIIC) on a range of preparations and molecular targets to assess its potential as a myorelaxant. EXPERIMENTAL APPROACH: µ-CnIIIC was sequenced, synthesized and characterized by its direct block of elicited twitch tension in mouse skeletal muscle and action potentials in mouse sciatic and pike olfactory nerves. µ-CnIIIC was also studied on HEK-293 cells expressing various rodent VGSCs and also on voltage-gated potassium channels and nicotinic acetylcholine receptors (nAChRs) to assess cross-interactions. Nuclear magnetic resonance (NMR) experiments were carried out for structural data. KEY RESULTS: Synthetic µ-CnIIIC decreased twitch tension in mouse hemidiaphragms (IC(50) = 150 nM), and displayed a higher blocking effect in mouse extensor digitorum longus muscles (IC = 46 nM), compared with µ-SIIIA, µ-SmIIIA and µ-PIIIA. µ-CnIIIC blocked Na(V)1.4 (IC(50) = 1.3 nM) and Na(V)1.2 channels in a long-lasting manner. Cardiac Na(V)1.5 and DRG-specific Na(V)1.8 channels were not blocked at 1 µM. µ-CnIIIC also blocked the 3ß2 nAChR subtype (IC(50) = 450 nM) and, to a lesser extent, on the 7 and 4ß2 subtypes. Structure determination of µ-CnIIIC revealed some similarities to -conotoxins acting on nAChRs. CONCLUSION AND IMPLICATIONS: µ-CnIIIC potently blocked VGSCs in skeletal muscle and nerve, and hence is applicable to myorelaxation. Its atypical pharmacological profile suggests some common structural features between VGSCs and nAChR channels. |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 5 |
| Volume Number | 166 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 2012-07-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Conotoxins Pharmacology Conus Snail Nicotinic Antagonists Peptides Sodium Channel Blockers Amino Acid Sequence Animals Chemistry Esocidae HEK293 Cells In Vitro Techniques Mice Molecular Sequence Data Muscle Contraction Drug Effects Muscle, Skeletal Physiology Olfactory Nerve Oocytes Protein Conformation Receptors, Nicotinic Sciatic Nerve Sodium Channels Xenopus Laevis Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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