Biochemical Pharmacology volume 79, issue 11, P1610-1615 2010 DOI: 10.1016/j.bcp.2010.01.035 View full text
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Krzysztof Jozwiak, Lawrence Toll, Lucita Jimenez, Anthony Yiu-Ho Woo, Rui-Ping Xiao, Irving W. Wainer

Abstract: The binding thermodynamics of the stereoisomers of fenoterol, (R,R')-, (S,S')- , (R,S')-, and (S,R')-fenoterol, to the β2-adrenergic receptor (β2-AR) have been determined. The experiments utilized membranes obtained from HEK cells stably transfected with cDNA encoding human β2-AR. Competitive displacement studies using [3H]CGP-12177 as the marker ligand were conducted at 4°, 15°, 25°, 30° and 37°C, the binding affinities calculated and the standard enthalpic (ΔH°) and standard entropic (ΔS°) contribution to t…

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