Summary
β-Adrenoceptors of lung (75% β2) and heart (95% β1) of calf were labelled with 3H-(−)-propranolol. The stereoisomers of 10 ligands were used to inhibit the binding of 3H-(−)-propranolol to membrane particles. The affinity ratio of sereoisomers is consistently greater for β1-adrenoceptors than for β2-adrenoceptors, regardless of whether the ligands are agonists, partial agonists or antagonists. The β1-adrenoceptor appears to possess stricter steric requirements than the β2-adrenoceptor. This property may prove helpful in differentiating the β-adrenoceptor subtypes during receptor solubilization and purification.
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Morris, T.H., Kaumann, A.J. Different steric characteristics of β1- and β2-adrenoceptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 327, 176–179 (1984). https://doi.org/10.1007/BF00500913
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DOI: https://doi.org/10.1007/BF00500913