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dc.contributor.author Monczor, Federico
dc.contributor.author Fernández, Natalia Brenda
dc.contributor.author Fitzsimons, Carlos
dc.contributor.author 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
dc.subject Antihistaminergics
dc.subject Inverse agonism
dc.subject Adverse effects
dc.subject.classification Farmacología y Farmacia
dc.subject.classification Medicina Básica
dc.subject.classification 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/http://dx.doi.org/10.1016/j.ejphar.2013.06.027
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/10.1016/j.ejphar.2013.06.027


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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Atribución-NoComercial-SinDerivadas 2.5 Argentina (CC BY-NC-ND 2.5 AR)