QUINACRINE IS MAINLY METABOLIZED TO MONO-DESETHYL QUINACRINE BY CYP3A4/5 AND ITS BRAIN ACCUMULATION IS LIMITED BY P-GLYCOPROTEIN

@article{Huang2006QUINACRINEIM,
  title={QUINACRINE IS MAINLY METABOLIZED TO MONO-DESETHYL QUINACRINE BY CYP3A4/5 AND ITS BRAIN ACCUMULATION IS LIMITED BY P-GLYCOPROTEIN},
  author={Yong Huang and Hideaki Okochi and Barnaby C. H. May and Giuseppe Legname and Stanley B. Prusiner and Leslie Z. Benet and B. Joseph Guglielmo and Emil T. Lin},
  journal={Drug Metabolism and Disposition},
  year={2006},
  volume={34},
  pages={1136 - 1144}
}
Quinacrine (QA), an antimalarial drug used for over seven decades, has been found to have potent antiprion activity in vitro. To determine whether QA can be used to treat prion diseases, we investigated its metabolism and ability to traverse the blood-brain barrier in mice. In vitro and in vivo, we identified by liquid chromatography-tandem mass spectrometry the major metabolic pathway of QA as N-desethylation and compared our results with an authentic reference compound. The major human… 
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