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dc.contributor.author
Gravielle, Maria Clara
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dc.date.available
2019-10-22T21:02:25Z
dc.date.issued
2018-09
dc.identifier.citation
Gravielle, Maria Clara; Regulation of GABAA receptors by prolonged exposure to endogenous and exogenous ligands; Pergamon-Elsevier Science Ltd; Neurochemistry International; 118; 9-2018; 96-104
dc.identifier.issn
0197-0186
dc.identifier.uri
http://hdl.handle.net/11336/87025
dc.description.abstract
GABAA receptors mediate most of the fast inhibitory transmissions in the central nervous system. These receptors are pentameric complexes that exhibit high structural and pharmacological heterogeneity, as they can be constructed from 19 distinct subunits. GABAA receptors are the targets of numerous clinically relevant drugs used to treat various disorders such as anxiety, insomnia and epilepsy. These receptors are also the targets of many volatile anesthetics and drugs of abuse, such as alcohol. This review is focused on the effect of long-term treatment with GABA, and the positive allosteric modulators benzodiazepines, neurosteroids and ethanol on GABAA receptors. Prolonged exposure of GABAA receptors to these compounds triggers several adaptive mechanisms that lead to changes in the structure, function and localization of receptors. These changes include GABAA receptor subunit expression, intracellular trafficking and phosphorylation. These adaptations are relevant to different physiological, pathological and pharmacological conditions and, in most cases, are associated with the development of tolerance. Understanding the molecular mechanisms underlying these regulatory processes will be relevant for therapeutic benefits.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Pergamon-Elsevier Science Ltd
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dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
BENZODIAZEPINE
dc.subject
ETHANOL
dc.subject
GABA
dc.subject
GABAA RECEPTOR
dc.subject
NEUROSTEROID
dc.subject.classification
Otras Ciencias de la Salud
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dc.subject.classification
Ciencias de la Salud
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dc.subject.classification
CIENCIAS MÉDICAS Y DE LA SALUD
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dc.title
Regulation of GABAA receptors by prolonged exposure to endogenous and exogenous ligands
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-10-15T14:13:50Z
dc.journal.volume
118
dc.journal.pagination
96-104
dc.journal.pais
Países Bajos
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dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Gravielle, Maria Clara. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay. Instituto de Investigaciones Farmacológicas. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Instituto de Investigaciones Farmacológicas; Argentina
dc.journal.title
Neurochemistry International
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S0197018618300214
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/https://doi.org/10.1016/j.neuint.2018.05.015
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