The selectivity of β‐adrenoceptor agonists at human β1‐, β2‐ and β3‐adrenoceptors

Background and purpose:  There are two important properties of receptor–ligand interactions: affinity (the ability of the ligand to bind to the receptor) and efficacy (the ability of the receptor–ligand complex to induce a response). Ligands are classified as agonists or antagonists depending on whether or not they have efficacy. In theory, it is possible to develop selective agonists based on selective affinity, selective intrinsic efficacy or both. This study examined the affinity and intrinsic efficacy of 31 β‐adrenoceptor agonists at the three human β‐adrenoceptors to determine whether the current agonists are subtype selective because of affinity or intrinsic efficacy.

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