The effect of stereochemistry on the thermodynamic characteristics of the binding of fenoterol stereoisomers to the beta(2)-adrenoceptor.

@article{Jzwiak2010TheEO,
  title={The effect of stereochemistry on the thermodynamic characteristics of the binding of fenoterol stereoisomers to the beta(2)-adrenoceptor.},
  author={Krzysztof J{\'o}zwiak and Lawrence Toll and Lucita Jimenez and Anthony Yiu-Ho Woo and Rui-ping Xiao and Irving W Wainer},
  journal={Biochemical pharmacology},
  year={2010},
  volume={79 11},
  pages={1610-5}
}
The binding thermodynamics of the stereoisomers of fenoterol, (R,R')-, (S,S')-, (R,S')-, and (S,R')-fenoterol, to the beta(2)-adrenergic receptor (beta(2)-AR) have been determined. The experiments utilized membranes obtained from HEK cells stably transfected with cDNA encoding human beta(2)-AR. Competitive displacement studies using [(3)H]CGP-12177 as the marker ligand were conducted at 4, 15, 25, 30 and 37 degrees C, the binding affinities calculated and the standard enthalpic (DeltaH degrees… CONTINUE READING

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