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dc.contributor.author
Monczor, Federico
dc.contributor.author
Fernández, Natalia Brenda
dc.contributor.author
Fitzsimons, Carlos
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Shayo, Carina Claudia
dc.contributor.author
Davio, Carlos Alberto
dc.date.available
2016-07-19T19:15:26Z
dc.date.issued
2013-09
dc.identifier.citation
Monczor, Federico; Fernández, Natalia Brenda; Fitzsimons, Carlos; Shayo, Carina Claudia; Davio, Carlos Alberto; Antihistaminergics and inverse agonism. Potential therapeutic applications; Elsevier; European Journal of Pharmacology; 715; 9-2013; 26-32
dc.identifier.issn
0014-2999
dc.identifier.uri
http://hdl.handle.net/11336/6591
dc.description.abstract
The accurate characterization of the molecular mechanisms involved in the action of receptor ligands is important for their appropriate therapeutic use and safety. It is well established that ligands acting at the histamine system currently used in the clinic exert their actions by specifically antagonizing G-protein coupled H1 and H2 receptors. However, most of these ligands, assumed to be neutral antagonists, behave as inverse agonists displaying negative efficacy in experimental systems. This suggests that their therapeutic actions may involve not only receptor blockade, but also the decrease of spontaneous receptor activity. The mechanisms whereby inverse agonists achieve negative efficacy are diverse. Theoretical models predict at least three possible mechanisms, all of which are supported by experimental observations. Depending on the mechanism of action engaged, the inverse agonist could interfere specifically with signaling events triggered by unrelated receptors. This possibility opens up new venues to explain the therapeutic actions of inverse agonists of the histamine receptor and perhaps new therapeutic applications.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Elsevier
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.subject
Histamine Receptors
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Antihistaminergics
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Inverse Agonism
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Adverse Effects
dc.subject.classification
Farmacología y Farmacia
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Medicina Básica
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CIENCIAS MÉDICAS Y DE LA SALUD
dc.title
Antihistaminergics and inverse agonism. Potential therapeutic applications
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2016-05-10T13:46:55Z
dc.journal.volume
715
dc.journal.pagination
26-32
dc.journal.pais
Países Bajos
dc.journal.ciudad
Amsterdam
dc.description.fil
Fil: Monczor, Federico. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
dc.description.fil
Fil: Fernández, Natalia Brenda. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
dc.description.fil
Fil: Fitzsimons, Carlos. University Of Amsterdam; Países Bajos
dc.description.fil
Fil: Shayo, Carina Claudia. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental (i); Argentina
dc.description.fil
Fil: Davio, Carlos Alberto. Universidad de Buenos Aires. Facultad de Farmacia y Bioquímica. Departamento de Farmacología. Cátedra de Química Medicinal; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Oficina de Coordinación Administrativa Houssay; Argentina
dc.journal.title
European Journal of Pharmacology
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0014299913004962
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejphar.2013.06.027
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.ejphar.2013.06.027


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