Contribution of binding enthalpy and entropy to affinity of antagonist and agonist binding at human and guinea pig histamine H(1)-receptor.

@article{Wittmann2009ContributionOB,
  title={Contribution of binding enthalpy and entropy to affinity of antagonist and agonist binding at human and guinea pig histamine H(1)-receptor.},
  author={Hans-Joachim Wittmann and Roland Seifert and Andrea Stra\sser},
  journal={Molecular pharmacology},
  year={2009},
  volume={76 1},
  pages={25-37}
}
For several GPCRs, discrimination between agonism and antagonism is possible on the basis of thermodynamics parameters, such as binding enthalpy and entropy. In this study, we analyze whether agonists and antagonists can also be discriminated thermodynamically at the histamine H(1) receptor (H(1)R). Because previous studies revealed species differences in pharmacology between human H(1)R (hH(1)R) and guinea pig H(1)R (gpH(1)R), we analyzed a broad spectrum of H(1)R antagonists and agonists at… CONTINUE READING

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