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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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| HATORI,EIKI; SAKURABA,SHIGEKI; KASHIWAGI,MASANORI; KURIBAYASHI,JUNYA; TSUJITA,MIKI; HOSOKAWA,YUKI; TAKEDA,JUNZO; KUWANA,SHUN-ICHI. |
| Nicotine exposure is a risk factor in several breathing disorders Nicotinic acetylcholine receptors (nAChRs) exist in the ventrolateral medulla, an important site for respiratory control. We examined the effects of nicotinic acetylcholine neurotransmission on central respiratory control by addition of a nAChR agonist or one of various antagonists into superfusion medium in the isolated brainstem-spinal cord from neonatal rats. Ventral C4 neuronal activity was monitored as central respiratory output, and activities of respiratory neurons in the ventrolateral medulla were recorded in whole-cell configuration. RJR-2403 (0.1-10mM), alpha4beta2 nAChR agonist induced dose-dependent increases in respiratory frequency. Non-selective nAChR antagonist mecamylamine... |
| Tipo: Journal article |
Palavras-chave: Brainstem-spinal cord; Neonatal rat; Inspiratory neuron; Preinspiratory neuron; Nicotinic acetylcholine receptor. |
| Ano: 2006 |
URL: http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0716-97602006000200014 |
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