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dc.contributor.author
Gravielle, Maria Clara
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dc.date.available
2018-03-15T18:17:51Z
dc.date.issued
2016-07
dc.identifier.citation
Gravielle, Maria Clara; Activation-induced regulation of GABAA receptors: Is there a link with the molecular basis of benzodiazepine tolerance?; Academic Press Ltd - Elsevier Science Ltd; Pharmacological Research; 109; 7-2016; 92-100
dc.identifier.issn
1043-6618
dc.identifier.uri
http://hdl.handle.net/11336/38954
dc.description.abstract
Benzodiazepines have been used clinically for more than 50 years to treat disorders such as insomnia, anxiety, and epilepsy, as well as to aid muscle relaxation and anesthesia. The therapeutic index for benzodiazepines if very high and the toxicity is low. However, their usefulness is limited by the development of either or both tolerance to most of their pharmacological actions and dependence. Tolerance develops at different rates depending on the pharmacological action, suggesting the existence of distinct mechanisms for each behavioral parameter. Alternatively, multiple mechanisms could coexist depending on the subtype of GABAA receptor expressed and the brain region involved. Because most of the pharmacological actions of benzodiazepines are mediated through GABAA receptor binding, adaptive alterations in the number, structure, and/or functions of these receptors may play an important role in the development of tolerance. This review is focused on the regulation of GABAA receptors induced by long-term benzodiazepine exposure and its relationship with the development of tolerance. Understanding the mechanisms behind benzodiazepine tolerance is critical for designing drugs that could maintain their efficacy during long-term treatments.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Academic Press Ltd - 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
Gaba
dc.subject
Gabaa Receptor
dc.subject
Tolerance
dc.subject
Uncoupling
dc.subject.classification
Otras Ciencias Biológicas
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dc.subject.classification
Ciencias Biológicas
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dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
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dc.title
Activation-induced regulation of GABAA receptors: Is there a link with the molecular basis of benzodiazepine tolerance?
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2018-03-14T17:04:22Z
dc.journal.volume
109
dc.journal.pagination
92-100
dc.journal.pais
Estados Unidos
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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
Pharmacological Research
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dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/pii/S1043661815002959
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.phrs.2015.12.030
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