{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["355(2)"],"submitter":["Littmann T"],"pubmed_abstract":["<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 recr"],"journal":["The Journal of pharmacology and experimental therapeutics"],"pagination":["183-90"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC4631950"],"repository":["biostudies-literature"],"pubmed_title":["Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands."],"pmcid":["PMC4631950"],"pubmed_authors":["Littmann T","Gottle M","Seifert R","Reinartz MT","Wainer IW","Ozawa T","Kalble S"],"additional_accession":[]},"is_claimable":false,"name":"Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.","description":"<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 recr","dates":{"release":"2015-01-01T00:00:00Z","publication":"2015 Nov","modification":"2026-05-09T15:48:22.369Z","creation":"2019-03-27T02:01:16Z"},"accession":"S-EPMC4631950","cross_references":{"pubmed":["26306764"],"doi":["10.1124/jpet.115.227959"]}}