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dc.contributor.author Garcia, Daniel Asmed
dc.contributor.author Bujons, Jordi
dc.contributor.author Vale, Carmen
dc.contributor.author Suñol, Cristina
dc.date.available 2018-08-29T20:21:40Z
dc.date.issued 2006-01
dc.identifier.citation Garcia, Daniel Asmed; Bujons, Jordi; Vale, Carmen; Suñol, Cristina; Allosteric positive interaction of thymol with the GABA-A receptor in primary cultures of mouse cortical neurons; Pergamon-Elsevier Science Ltd; Neuropharmacology; 50; 1; 1-2006; 25-35
dc.identifier.issn 0028-3908
dc.identifier.uri http://hdl.handle.net/11336/57589
dc.description.abstract Thymol is a naturally occurring phenolic monoterpene known for its anti-microbial and anti-oxidant properties. It is used in dental practice and in anaesthetic halothane preparations. Recent studies have reported enhanced GABAA receptor-operated chloride channel activity and increased binding affinity of [3H]flunitrazepam in the presence of thymol. In the present work, we more closely examined the pharmacological action of thymol on the native GABAA receptor by using primary cultures of cortical neurons. Thymol enhanced GABA-induced (5 μM) chloride influx at concentrations lower than those exhibiting direct activity in the absence of GABA (EC50 = 12 μM and 135 μM, respectively). This direct effect was inhibited by competitive and non-competitive GABAA receptor antagonists. Thymol increased [3H]flunitrazepam binding (EC50 = 131 μM) and showed a tendency to increase [ 3H]muscimol binding. These results confirm that thymol is a positive allosteric modulator of the GABAA receptor. The thymol structural analogues menthol and cymene, which lack an aromatic ring or a hydroxyl group, did not affect [3H]flunitrazepam binding. Using a pharmacophoric model that includes a hydrogen bond donor group as well as an aromatic ring with two aliphatic substituents, we propose to demonstrate the molecular essential features of these compounds to interact with GABAA receptors. Thymol (0-1 mM) did not affect cellular viability.
dc.format application/pdf
dc.language.iso eng
dc.publisher Pergamon-Elsevier Science Ltd
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject CELL VIABILITY
dc.subject CULTURED CORTICAL NEURONS
dc.subject GABAA RECEPTOR
dc.subject PHARMACOPHORE MODEL
dc.subject RECEPTOR BINDING AND CHLORIDE FLUX
dc.subject THYMOL
dc.subject.classification Otras Ciencias Biológicas
dc.subject.classification Ciencias Biológicas
dc.subject.classification CIENCIAS NATURALES Y EXACTAS
dc.title Allosteric positive interaction of thymol with the GABA-A receptor in primary cultures of mouse cortical neurons
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2018-08-13T17:05:38Z
dc.journal.volume 50
dc.journal.number 1
dc.journal.pagination 25-35
dc.journal.pais Estados Unidos
dc.journal.ciudad Nueva York
dc.description.fil Fil: Garcia, Daniel Asmed. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Instituto de Investigaciones Biológicas y Tecnológicas. Universidad Nacional de Córdoba. Facultad de Ciencias Exactas, Físicas y Naturales. Instituto de Investigaciones Biológicas y Tecnológicas; Argentina. Consejo Superior de Investigaciones Científicas; España. Institut d'Investigacions Biomèdiques de Barcelona; España
dc.description.fil Fil: Bujons, Jordi. Consejo Superior de Investigaciones Científica; España. Institut d'Investigacions Químiques i Ambientals de Barcelona; España
dc.description.fil Fil: Vale, Carmen. Consejo Superior de Investigaciones Científicas; España. Institut d'Investigacions Biomèdiques de Barcelona; España. Universidad de Santiago de Compostela; España
dc.description.fil Fil: Suñol, Cristina. Consejo Superior de Investigaciones Científicas; España. Institut d'Investigacions Biomèdiques de Barcelona; España
dc.journal.title Neuropharmacology
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0028390805002716
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.neuropharm.2005.07.009
dc.conicet.fuente individual


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info:eu-repo/semantics/restrictedAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)