Relaxation of androgens on rat thoracic aorta: testosterone concentration dependent agonist/antagonist L-type Ca2+ channel activity, and 5beta-dihydrotestosterone restricted to L-type Ca2+ channel blockade

Simple item page
dc.contributor.affiliationInstituto de Investigaciones Biomédicas, Departamento de Biología Celular y Fisiología, and Facultad de Medicina, Departamento de Farmacología, México D.F. 04510.es_ES
dc.creatorMontaño, L.M.
dc.creatorCalixto, E.
dc.creatorFigueroa, A.
dc.creatorFlores-Soto, E.
dc.creatorCarbajal, V.
dc.creatorPerusquía, M.
dc.creator.identificador"http://orcid.org/0000-0002-8329-4918">Montaño, Luis M.es_ES
dc.date.accessioned2017-06-29T06:02:44Z
dc.date.accessioned2026-03-27T14:35:46Z
dc.date.available2017-06-29T06:02:44Z
dc.date.issued2008es_ES
dc.date.published2008es_ES
dc.description.abstractotrodiomaAndrogen vasorelaxing action is a subject of recent interest. We investigated the involvement of l-type voltage-operated Ca(2+) channels (L-VOCCs), K(+) channels, intracellular Ca(2+) concentration ([Ca(2+)]i), and cAMP in the vasorelaxing effect of testosterone and 5beta-dihydrotestosterone (5beta-DHT) on rat thoracic aorta. Isolated aortic rings were used to study the vasorelaxing potency of testosterone and 5beta-DHT on KCl- and noradrenaline-induced contractions. Patch-clamp was used to analyze androgen effects on Ca(2+) inward and K(+) outward currents. The fluorescence technique was used to evaluate [Ca(2+)]i in single myocytes; moreover, simultaneous measurements of [Ca(2+)]i and vascular contraction were evaluated. 5beta-DHT was more potent than testosterone to relax KCl-induced contraction, but they were equipotent to relax noradrenaline contraction. l-type Ca(2+) currents were blocked by nifedipine, both androgens, and an estrogen in a concentration-dependent manner, and the order of potency was: testosterone > nifedipine > 5beta-DHT > 17beta-estradiol. We observed that testosterone has different mechanism of action by the concentration range used: at nm concentrations it was a powerful L-VOCCs antagonist, whereas at mum concentrations it was observed that: 1) its Ca(2+) antagonist property is reverted by increasing the l-type inward Ca(2+) currents (Ca(2+) agonist property); and 2) the [Ca(2+)]i and cAMP production was increased. The total K(+) currents were unaffected by testosterone or 5beta-DHT. The data show that 5beta-DHT-induced vasorelaxation is due to its selective blockade on L-VOCCs (from nm to microm concentrations), but testosterone-induced vasorelaxation involves concentration-dependent additional mechanisms: acting as an L-VOCCs antagonist at low concentrations, and increasing [Ca(2+)]i and cAMP production at high concentrations.es_ES
dc.description.monthMayes_ES
dc.identifier557es_ES
dc.identifier.citationAlberto Darío Ramírez Gonzálezes_ES
dc.identifier.doi10.1210/en.2007-1288es_ES
dc.identifier.eissn1945-7170es_ES
dc.identifier.issn0013-7227es_ES
dc.identifier.numero5es_ES
dc.identifier.organizacionInstituto Nacional de Psiquiatría Ramón de la Fuente Muñizes_ES
dc.identifier.paginacion2517-2526es_ES
dc.identifier.placeUnited Stateses_ES
dc.identifier.urihttps://doi.org/10.1210/en.2007-1288es_ES
dc.identifier.urihttps://repositorio.inprf.gob.mx/handle/123456789/5244
dc.identifier.volumen149es_ES
dc.language.isoenges_ES
dc.relation149 (5) 2517-2526 p.es_ES
dc.relationversión del editores_ES
dc.relation.jnabreviadoENDOCRINOLOGYes_ES
dc.relation.journalEndocrinologyes_ES
dc.rightsacceso cerradoes_ES
dc.subject.meshAndrogens-pharmacologyes_ES
dc.subject.meshAnimalses_ES
dc.subject.meshAorta, Thoracic-drug effectses_ES
dc.subject.meshAorta, Thoracic-physiologyes_ES
dc.subject.meshCalcium-metabolismes_ES
dc.subject.meshCalcium Channel Agonists-pharmacologyes_ES
dc.subject.meshCalcium Channel Blockers-pharmacologyes_ES
dc.subject.meshCalcium Channels, L-Type-metabolismes_ES
dc.subject.meshCells, Culturedes_ES
dc.subject.meshDihydrotestosterone-pharmacologyes_ES
dc.subject.meshDose-Response Relationship, Druges_ES
dc.subject.meshMalees_ES
dc.subject.meshMembrane Potentials-drug effectses_ES
dc.subject.meshMuscle Cellses_ES
dc.subject.meshOsmolar Concentrationes_ES
dc.subject.meshPotassium-metabolismes_ES
dc.subject.meshRatses_ES
dc.subject.meshRats, Wistares_ES
dc.subject.meshSubstrate Specificityes_ES
dc.subject.meshTestosterone-pharmacologyes_ES
dc.subject.meshVasodilation-drug effectses_ES
dc.titleRelaxation of androgens on rat thoracic aorta: testosterone concentration dependent agonist/antagonist L-type Ca2+ channel activity, and 5beta-dihydrotestosterone restricted to L-type Ca2+ channel blockadees_ES
dc.typearticlees_ES

Files

Collections

Artículos de revista