| Inhibition of nicotinic cholinoceptor mediated current in vagal motor neurons by local anesthetics. | |
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MedLine Citation:
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PMID: 9028586 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The effects of local anesthetics on ligand-gated cation channel currents were examined in rat brainstem vagal motoneurons. Etidocaine (0.1-20 microM) blocked nicotinic cholinoceptor gated currents in cells voltage-clamped at -60 mV in a concentration-dependent manner, but at concentrations up to 100 microM did not inhibit glutamate receptor currents induced by (+/-)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate (AMPA), N-methyl-D-aspartate (NMDA), or glutamate. Relative to etidocaine, procaine displayed about 10-fold lower potency in antagonizing acetylcholine and its inhibitory effect, unlike that of etidocaine, was rapidly reversed by washout. Ketamine (10 microM) caused a 2-fold larger decrease in NMDA current than acetylcholine current, but did not affect AMPA current. In conclusion, (i) etidocaine and procaine possess a moderately potent blocking activity at nicotinic cholinoceptor gated channels in brainstem vagal motoneurons and (ii) in contrast with ketamine, both agents showed similar selectivity in that neither inhibited glutamate receptor gated channels at concentrations up to 0.1 mM. |
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Authors:
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W Y Lu; D Bieger |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Canadian journal of physiology and pharmacology Volume: 74 ISSN: 0008-4212 ISO Abbreviation: Can. J. Physiol. Pharmacol. Publication Date: 1996 Nov |
Date Detail:
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Created Date: 1997-04-15 Completed Date: 1997-04-15 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0372712 Medline TA: Can J Physiol Pharmacol Country: CANADA |
Other Details:
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Languages: eng Pagination: 1265-9 Citation Subset: IM |
Affiliation:
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Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Canada. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Anesthetics, Local
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pharmacology* Animals Etidocaine / pharmacology Ion Channel Gating / drug effects* Ketamine / pharmacology Male Motor Neurons / drug effects* N-Methylaspartate / pharmacology Nicotinic Antagonists / pharmacology* Patch-Clamp Techniques Procaine / pharmacology Rats Vagus Nerve / drug effects* |
| Chemical | |
Reg. No./Substance:
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0/Anesthetics, Local; 0/Nicotinic Antagonists; 36637-18-0/Etidocaine; 59-46-1/Procaine; 6384-92-5/N-Methylaspartate; 6740-88-1/Ketamine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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