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| Favreau, Philippe; Benoit, Evelyne; Hocking, Henry G.; Carlier, Ludovic; D'Hoedt, Dieter; Leipold, Enrico; Markgraf, Rene; Schlumberger, Sebastien; Cordova, Marco A.; Gaertner, Hubert; Paolini-bertrand, Marianne; Hartley, Oliver; Tytgat, Jan; Heinemann, Stefan H.; Bertrand, Daniel; Boelens, Rolf; Stoecklin, Reto; Molgo, Jordi. |
| BACKGROUND AND PURPOSE The mu-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 mu-conopeptide (mu-CnIIIC) on a range of preparations and molecular targets to assess its potential as a myorelaxant. EXPERIMENTAL APPROACH mu-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. mu-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... |
| Tipo: Text |
Palavras-chave: Cone snail venom; Mu-conotoxin; Voltage-gated sodium channel; Nicotinic acetylcholine receptor; Myorelaxant; Twitch tension; NMR structure. |
| Ano: 2012 |
URL: https://archimer.ifremer.fr/doc/00467/57830/60132.pdf |
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