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• W2969077457 abstract "Los bloqueadores beta son moléculas ampliamente utilizadas y capaces de antagonizar los receptores adrenérgicos (RA) beta, pertenecen a la familia de receptores acoplados a proteínas G y reciben el estímulo de las catecolaminas endógenas. Tras su estimulación, se activan cascadas intracelulares que en última instancia originan la contracción cardiaca o la dilatación vascular, según el subtipo y su ubicación. Se han descrito 3 subtipos, que se expresan de manera diferenciada en el organismo (RA-β1, β2 y β3), y el subtipo β1 es el más abundante en el corazón. Desde su descubrimiento, los RA-β se han convertido en diana para combatir las enfermedades cardiovasculares. Desde su invención por James Black a finales de los años cincuenta, los bloqueadores beta han supuesto una revolución en la terapia cardiovascular. Hasta ahora se dispone de 3 generaciones: los bloqueadores beta no selectivos, los bloqueadores beta cardioselectivos (antagonista selectivo de β1) y los bloqueadores beta vasodilatadores. Estos constituyen la tercera generación y son capaces de bloquear los β1 además de tener actividad vasodilatadora, bien bloqueando los RA-α1 o activando los RA-β3. Los bloqueadores beta todavía se utilizan ampliamente en la clínica tras más de 50 años desde la introducción del propranolol en el mercado por su capacidad para reducir la frecuencia cardiaca y, por lo tanto, la demanda miocárdica de oxígeno en el caso de una angina. Beta-blockers are widely used molecules that are able to antagonize β-adrenergic receptors (ARs), which belong to the G protein-coupled receptor family and receive their stimulus from endogenous catecholamines. Upon β-AR stimulation, numerous intracellular cascades are activated, ultimately leading to cardiac contraction or vascular dilation, depending on the relevant subtype and their location. Three subtypes have been described that are differentially expressed in the body (β1-, β2- and β3-ARs), β1 being the most abundant subtype in the heart. Since their discovery, β-ARs have become an important target to fight cardiovascular disease. In fact, since their discovery by James Black in the late 1950s, β-blockers have revolutionized the field of cardiovascular therapies. To date, 3 generations of drugs have been released: nonselective β-blockers, cardioselective β-blockers (selective β1-antagonists), and a third generation of these drugs able to block β1 together with extra vasodilation activity (also called vasodilating β-blockers) either by blocking α1- or by activating β3-AR. More than 50 years after propranolol was introduced to the market due to its ability to reduce heart rate and consequently myocardial oxygen demand in the event of an angina attack, β-blockers are still widely used in clinics." @default.
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• W2969077457 date "2019-10-01" @default.
• W2969077457 modified "2023-10-17" @default.
• W2969077457 title "Bloqueadores beta: perspectiva histórica y mecanismos de acción" @default.
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• W2969077457 doi "https://doi.org/10.1016/j.recesp.2019.02.023" @default.
• W2969077457 hasPublicationYear "2019" @default.
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