Comparative molecular field analysis of fenoterol derivatives interacting with an agonist-stabilized form of the β 2-adrenergic receptor

A Plazinska, K Pajak, E Rutkowska, L Jimenez…

Index: Plazinska, Anita; Pajak, Karolina; Rutkowska, Ewelina; Jimenez, Lucita; Kozocas, Joseph; Koolpe, Gary; Tanga, Mary; Toll, Lawrence; Wainer, Irving W.; Jozwiak, Krzysztof Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 1 p. 234 - 246

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Citation Number: 7

Abstract

Abstract The β 2-adrenergic receptor (β 2-AR) agonist [3 H]-(R, R′)-methoxyfenoterol was employed as the marker ligand in displacement studies measuring the binding affinities (K i values) of the stereoisomers of a series of 4′-methoxyfenoterol analogs in which the length of the alkyl substituent at α′ position was varied from 0 to 3 carbon atoms. The binding affinities of the compounds were additionally determined using the inverse agonist [3 H]- ...