Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers.

@article{Eap2007StereoselectiveBO,
  title={Stereoselective block of hERG channel by (S)-methadone and QT interval prolongation in CYP2B6 slow metabolizers.},
  author={Chin B. Eap and Severine Crettol and J-S Rougier and Juerg Schlaepfer and Liliana Sintra Grilo and J-J D{\'e}glon and J. N. Besson and Marina Croquette-Krokar and P A Carrupt and H. Abriel},
  journal={Clinical pharmacology and therapeutics},
  year={2007},
  volume={81 5},
  pages={719-28}
}
Methadone inhibits the cardiac potassium channel hERG and can cause a prolonged QT interval. Methadone is chiral but its therapeutic activity is mainly due to (R)-methadone. Whole-cell patch-clamp experiments using cells expressing hERG showed that (S)-methadone blocked the hERG current 3.5-fold more potently than (R)-methadone (IC50s (half-maximal inhibitory concentrations) at 37 degrees C: 2 and 7 microM). As CYP2B6 slow metabolizer (SM) status results in a reduced ability to metabolize (S… CONTINUE READING

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