Potent and specific inhibition of mMate1-mediated efflux of type I organic cations in the liver and kidney by pyrimethamine.

@article{Ito2010PotentAS,
  title={Potent and specific inhibition of mMate1-mediated efflux of type I organic cations in the liver and kidney by pyrimethamine.},
  author={Sumito Ito and Hiroyuki Kusuhara and Yushun Kuroiwa and Chungyong Wu and Yoshinori Moriyama and Katsuhisa Inoue and Tsunenori Kondo and Hiroaki Yuasa and Hideki Nakayama and Shigeru Horita and Yuichi Sugiyama},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2010},
  volume={333 1},
  pages={341-50}
}
This report describes a potent and selective inhibitor of multidrug and toxin extrusion (MATE) protein, pyrimethamine (PYR), and examines its effect on the urinary and biliary excretion of typical Mate1 substrates in mice. In vitro inhibition studies demonstrated that PYR is a potent inhibitor of mouse (m)Mate1 (K(i) = 145 nM) among renal organic cation transporters mOctn1 and mOctn2 (K(i) > 30 microM), mOct1 (K(i) = 3.6 microM), and mOct2 (K(i) = 6.0 microM). PYR inhibited the uptake of… CONTINUE READING
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