biostudies-literatureUnknown355(2)Littmann T<h4>Unlabelled</h4>Beyond canonical signaling via Gαs and cAMP, the concept of functional selectivity at β2-adrenoceptors (β2ARs) describes the ability of adrenergic drugs to stabilize ligand-specific receptor conformations to initiate further signaling cascades comprising additional G-protein classes or β-arrestins (βarr). A set of 65 adrenergic ligands including 40 agonists and 25 antagonists in either racemic or enantiopure forms was used for βarr recruitment experiments based on a split-luciferase assay in a cellular system expressing β2AR. Many agonists showed only (weak) partial agonism regarding βarr recruitment. Potencies and/or efficacies increased depending on the number of chirality centers in (R) configuration; no (S)-configured distomer was more effective at inducing βarr recrThe Journal of pharmacology and experimental therapeutics183-90https://www.ebi.ac.uk/biostudies/studies/S-EPMC4631950biostudies-literatureRecruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.PMC4631950Littmann TGottle MSeifert RReinartz MTWainer IWOzawa TKalble SfalseRecruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.<h4>Unlabelled</h4>Beyond canonical signaling via Gαs and cAMP, the concept of functional selectivity at β2-adrenoceptors (β2ARs) describes the ability of adrenergic drugs to stabilize ligand-specific receptor conformations to initiate further signaling cascades comprising additional G-protein classes or β-arrestins (βarr). A set of 65 adrenergic ligands including 40 agonists and 25 antagonists in either racemic or enantiopure forms was used for βarr recruitment experiments based on a split-luciferase assay in a cellular system expressing β2AR. Many agonists showed only (weak) partial agonism regarding βarr recruitment. Potencies and/or efficacies increased depending on the number of chirality centers in (R) configuration; no (S)-configured distomer was more effective at inducing βarr recr2015-01-01T00:00:00Z2015 Nov2026-05-09T15:48:22.369Z2019-03-27T02:01:16ZS-EPMC46319502630676410.1124/jpet.115.227959