The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.

ABSTRACT:

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 beta-adrenoceptor agonists at the three human beta-adrenoceptors to determine whether the current agonists are subtype selective because of affinity or intrinsic efficacy.

Experimental approach

Stable clonal CHO-K1 cell lines, transfected with either the human beta(1),

SUBMITTER: Baker JG 

PROVIDER: S-EPMC2936015 | biostudies-literature | 2010 Jul

REPOSITORIES: biostudies-literature