Affinity and Selectivity of &bgr;‐Adrenoceptor Antagonists In Vitro

  title={Affinity and Selectivity of \&bgr;‐Adrenoceptor Antagonists In Vitro},
  author={Anton Wellstein and Dieter Palm and Gustav Georg Belz},
  journal={Journal of Cardiovascular Pharmacology},
&NA; The potency order of the catecholamines (‐)isoprenaline (Iso), ( ‐ )‐noradrenaline (NA), and ( ‐ )‐adrenaline (Adr) in competition for radiolabelled sites is used for their pharmacological classification. It is shown that the radioligand 3H‐CGP 12177 exclusively labels &bgr;1‐adrenoceptors in rat salivary gland membranes (Iso > NA > Adr), and &bgr;2‐adrenoceptors in rat reticulocytes (Iso > Adr ≥ NA). These models are then used to derive the subtype‐selectivity of the classical &bgr… 
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Bucindolol exerts agonistic activity on the propranolol-insensitive state of beta1-adrenoceptors in human myocardium.
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β- and α2-Adrenoceptor Control of Vascular Tension and Catecholamine Release in Female Normotensive and Spontaneously Hypertensive Rats
  • T. Berg
  • Biology, Medicine
    Front. Neurol.
  • 2017
In these female rats, α2/β1+2AR reciprocally controlled catecholamine release, with a particular negative β1AR-influence on α2AR-auto-inhibition of epinephrine secretion in SHR, is analyzed.
The pharmacogenetics of β-adrenergic receptor antagonists in the treatment of hypertension and heart failure
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