Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).

@article{Gillard2002BindingCO,
  title={Binding characteristics of cetirizine and levocetirizine to human H(1) histamine receptors: contribution of Lys(191) and Thr(194).},
  author={Michel Gillard and Christy Van Der Perren and Nicole Moguilevsky and Roy Massingham and Pierre Chatelain},
  journal={Molecular pharmacology},
  year={2002},
  volume={61 2},
  pages={391-9}
}
Competition experiments with [(3)H]mepyramine showed that cetirizine and its enantiomers, levocetirizine and (S)-cetirizine, bound with high affinity and stereoselectivity to human H(1) histamine receptors (K(i) values of 6, 3, and 100 nM, respectively). Cetirizine and levocetirizine were 600-fold more selective for H(1) receptors compared with a panel of receptors and channels. Binding results indicated that the interaction between cetirizine, its enantiomers, and histamine is compatible with… CONTINUE READING
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