Interaction of Fenoterol Stereoisomers with β2-adrenoceptor-G Sα Fusion Proteins: Antagonist and Agonist Competition Binding

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 2015 Feb 1

PMID 25637582

Citations 3

Authors

Michael T Reinartz

Solveig Kalble

Irving W Wainer

Roland Seifert

Affiliations

Soon will be listed here.

Abstract

The specific interaction between G-protein-coupled receptors and ligand is the starting point for downstream signaling. Fenoterol stereoisomers were successfully used to probe ligand-specific activation (functional selectivity) of the β2-adrenoceptor (β2AR) (Reinartz et al. 2015). In the present study, we extended the pharmacological profile of fenoterol stereoisomers using β2AR-Gsα fusion proteins in agonist and antagonist competition binding assays. Dissociations between binding affinities and effector potencies were found for (R,S')- and (S,S')-isomers of 4'-methoxy-1-naphthyl-fenoterol. Our data corroborate former studies on the importance of the aminoalkyl moiety of fenoterol derivatives for functional selectivity.

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