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dc.contributor.author Lemos Legnazzi, Bibiana
dc.contributor.author Shayo, Carina Claudia
dc.contributor.author Monczor, Federico
dc.contributor.author Martín, María E.
dc.contributor.author Fernández, Natalia Brenda
dc.contributor.author Brodsky, Andres
dc.contributor.author Baldi, Alberto
dc.contributor.author Davio, Carlos Alberto
dc.date.available 2017-12-22T00:21:42Z
dc.date.issued 2000-07-15
dc.identifier.citation Davio, Carlos Alberto; Baldi, Alberto; Brodsky, Andres; Fernández, Natalia Brenda; Martín, María E.; Monczor, Federico; et al.; Rapid desensitization and slow recovery of the cyclic AMP response mediated by histamine H2 receptors in the U937 cell line; Pergamon-Elsevier Science Ltd.; Biochemical Pharmacology; 60; 2; 15-7-2000; 159-166
dc.identifier.issn 0006-2952
dc.identifier.uri http://hdl.handle.net/11336/31323
dc.description.abstract The present study focused on the desensitization process of the H(2) receptor in U937 cells and the recovery of the cyclic AMP (cAMP) response. Treatment of U937 leukemic cells with the H(2) histamine receptor agonists (+/-)-N(1)-[3-(3, 4-difluorophenyl)-3-(pyridin-2-yl)propyl]-N(2)-[3-(1H-imidazol-4-yl)p ropyl]guanidine (BU-E-75) and amthamine produced a rapid desensitization characterized by decreased cAMP production (T(1/2) = 20 min). Pretreatment with 10 microM BU-E-75 did not induce modifications in the responses to prostaglandin E(2), isoproterenol, or forskolin. H(2) receptor desensitization was not affected by protein kinase A and C inhibitors, but was reduced drastically by Zn(2+) and heparin, known to act as inhibitors of G protein-coupled receptor kinases. Recovery studies of the cAMP response showed that cAMP levels reached 50% of the initial values within 5 hr. Furthermore, desensitization produced an important decrease in the basal level of this cyclic nucleotide. The minimal value was observed 12 hr later, and corresponded to approximately 1.3% of the initial basal level (7.5 vs 0.1 pmol/10(6) cells). This result could be explained by an increase in phosphodiesterase activity following 10 microM BU-E-75 treatment. When cells were exposed for 2 hr to an H(2) agonist, binding assays showed no modification in the number of H(2) receptors; internalization began just after 8 hr. Although the initial desensitization seems to involve G protein-coupled receptor kinases, results indicate that additional mechanisms of regulation were triggered by the H(2) agonists.
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 HOMOLOGOUS DESENSITATION
dc.subject G PROTEIN-COUPLED RECEPTOR KINASES
dc.subject PHOSPHORODIESTERASES
dc.subject [3H]TIOTIDINE BINDING
dc.subject CELL DIFFERENTIATION
dc.subject.classification Bioquímica y Biología Molecular
dc.subject.classification Medicina Básica
dc.subject.classification CIENCIAS MÉDICAS Y DE LA SALUD
dc.subject.classification Farmacología y Farmacia
dc.subject.classification Medicina Básica
dc.subject.classification CIENCIAS MÉDICAS Y DE LA SALUD
dc.title Rapid desensitization and slow recovery of the cyclic AMP response mediated by histamine H2 receptors in the U937 cell line
dc.type info:eu-repo/semantics/article
dc.type info:ar-repo/semantics/artículo
dc.type info:eu-repo/semantics/publishedVersion
dc.date.updated 2017-12-04T17:54:48Z
dc.identifier.eissn 1873-2968
dc.journal.volume 60
dc.journal.number 2
dc.journal.pagination 159-166
dc.journal.pais Estados Unidos
dc.description.fil Fil: Lemos Legnazzi, Bibiana. Universidad de Buenos Aires. Facultad de Medicina. Hospital de Clínicas General San Martín; Argentina
dc.description.fil Fil: Shayo, Carina Claudia. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina
dc.description.fil Fil: Monczor, Federico. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad de Buenos Aires. Facultad de Medicina. Hospital de Clínicas General San Martín; Argentina
dc.description.fil Fil: Martín, María E.. Universidad de Buenos Aires. Facultad de Medicina. Hospital de Clínicas General San Martín; Argentina
dc.description.fil Fil: Fernández, Natalia Brenda. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina
dc.description.fil Fil: Brodsky, Andres. Universidad de Buenos Aires. Facultad de Medicina. Hospital de Clínicas General San Martín; Argentina
dc.description.fil Fil: Baldi, Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Instituto de Biología y Medicina Experimental. Fundación de Instituto de Biología y Medicina Experimental. Instituto de Biología y Medicina Experimental; Argentina
dc.description.fil Fil: Davio, Carlos Alberto. Universidad de Buenos Aires. Facultad de Medicina. Hospital de Clínicas General San Martín; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
dc.journal.title Biochemical Pharmacology
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0006295200002951?via%3Dihub
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/S0006-2952(00)00295-1
dc.relation.alternativeid info:eu-repo/semantics/altIdentifier/pmid/http://europepmc.org/abstract/med/10825460


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