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

@article{Wellstein1986AffinityAS,
  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},
  year={1986},
  volume={8},
  pages={S36–S40}
}
&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… Expand
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