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Structure-bias relationships for fenoterol stereoisomers in six molecular and cellular assays at the β2-adrenoceptor.

Reinartz, Michael T. ; Kälble, Solveig ; Littmann, Timo ; Ozawa, Takeaki ; Dove, Stefan ; Kaever, Volkhard ; Wainer, Irving W. ; Seifert, Roland



Abstract

Functional selectivity is well established as an underlying concept of ligand-specific signaling via G protein-coupled receptors (GPCRs). Functionally, selective drugs could show greater therapeutic efficacy and fewer adverse effects. Dual coupling of the β2-adrenoceptor (β2AR) triggers a signal transduction via Gsα and Giα proteins. Here, we examined 12 fenoterol stereoisomers in six molecular ...

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