| A novel agonist effect on the nicotinic acetylcholine receptor exerted by the anticonvulsive drug Lamotrigine. | |
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MedLine Citation:
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PMID: 18621019 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The anticonvulsive drug Lamotrigine (LTG) is found to activate adult muscle nicotinic acetylcholine receptors (AChR). Single-channel patch-clamp recordings showed that LTG (0.05-400 microM) applied alone is able to open AChR channels. [125I]alpha-bungarotoxin-binding studies further indicate that LTG does not bind to the canonical ACh-binding sites. Fluorescence experiments using the probe crystal violet demonstrate that LTG induces the transition from the resting state to the desensitized state of the AChR in the presence of excess alpha-bungarotoxin, that is, when the agonist site is blocked. Allosterically-potentiating ligands or the open-channel blocker QX-314 exhibited a behavior different from that of LTG. We conclude that LTG activates the AChR through a site that is different from those of full agonists/competitive antagonists and allosterically-potentiating ligands, respectively. |
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Authors:
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Ana Sofía Vallés; Ingrid Garbus; Silvia S Antollini; Francisco J Barrantes |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-06-24 |
Journal Detail:
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Title: Biochimica et biophysica acta Volume: 1778 ISSN: 0006-3002 ISO Abbreviation: Biochim. Biophys. Acta Publication Date: 2008 Oct |
Date Detail:
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Created Date: 2008-09-22 Completed Date: 2008-12-16 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0217513 Medline TA: Biochim Biophys Acta Country: Netherlands |
Other Details:
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Languages: eng Pagination: 2395-404 Citation Subset: IM |
Affiliation:
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UNESCO Chair of Biophysics and Molecular Neurobiology and Instituto de Investigaciones Bioquímicas de Bahía Blanca, C.C. 857, B8000FWB Bahía Blanca, Argentina. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anticonvulsants / metabolism* Binding Sites Bungarotoxins / metabolism CHO Cells Cricetinae Cricetulus Nicotinic Antagonists / metabolism Patch-Clamp Techniques Receptors, Nicotinic* / chemistry, metabolism Triazines / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Anticonvulsants; 0/Bungarotoxins; 0/Nicotinic Antagonists; 0/Receptors, Nicotinic; 0/Triazines; 84057-84-1/lamotrigine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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