Large neutral amino acid transporter enables brain drug delivery via prodrugs.

@article{Gynther2008LargeNA,
  title={Large neutral amino acid transporter enables brain drug delivery via prodrugs.},
  author={Mikko Gynther and Krista Laine and Jarmo Ropponen and Jukka Lepp{\"a}nen and Anne Mannila and Tapio Nevalainen and Jouko Savolainen and Tomi J{\"a}rvinen and Jarkko Rautio},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 4},
  pages={932-6}
}
The blood-brain barrier efficiently controls the entry of drug molecules into the brain. We describe a feasible means to achieve carrier-mediated drug transport into the rat brain via the specific, large neutral amino acid transporter (LAT1) by conjugating a model compound to L-tyrosine. A hydrophilic drug, ketoprofen, that is not a substrate for LAT1 was chosen as a model compound. The mechanism and the kinetics of the brain uptake of the prodrug were determined with an in situ rat brain… CONTINUE READING
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