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The selectivity of β‐adrenoceptor agonists at human β 1 ‐, β 2 ‐ and β 3 ‐adrenoceptors
Author(s) -
Baker Jillian G
Publication year - 2010
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.2010.00754.x
Subject(s) - intrinsic activity , isoprenaline , agonist , chemistry , partial agonist , ligand (biochemistry) , formoterol , receptor , pharmacology , radioligand , chinese hamster ovary cell , endocrinology , biology , biochemistry , stimulation , budesonide , corticosteroid
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 beta-adrenoceptor agonists at the three human beta-adrenoceptors to determine whether the current agonists are subtype selective because of affinity or intrinsic efficacy.