Tariquidar Is an Inhibitor and Not a Substrate of Human and Mouse P-glycoprotein.

@article{Weidner2016TariquidarIA,
  title={Tariquidar Is an Inhibitor and Not a Substrate of Human and Mouse P-glycoprotein.},
  author={Lora Deuitch Weidner and King Leung Fung and Pavitra Kannan and Janna K. Moen and Jeyan S. Kumar and Jan Mulder and Robert B. Innis and Michael M. Gottesman and Matthew D. Hall},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2016},
  volume={44 2},
  pages={275-82}
}
Since its development, tariquidar (TQR; XR9576; N-[2-[[4-[2-(6,7-Dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]-4,5-dimethoxyphenyl]quinoline-3-carboxamide) has been widely regarded as one of the more potent inhibitors of P-glycoprotein (P-gp), an efflux transporter of the ATP-binding cassette (ABC) transporter family. A third-generation inhibitor, TQR exhibits high affinity for P-gp, although it is also a substrate of another ABC transporter, breast cancer resistance protein… CONTINUE READING
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Tariquidar Analogues: Synthesis by CuI-Catalysed N/O–Aryl Coupling and Inhibitory Activity against the ABCB1 Transporter

  • M Egger, X Li, C Muller, G Bernhardt, A Buschauer, B Konig
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