Blood-brain barrier penetration abolished by N-methyl quaternization of nicotine.

@article{Oldendorf1993BloodbrainBP,
  title={Blood-brain barrier penetration abolished by N-methyl quaternization of nicotine.},
  author={William H. Oldendorf and Bob Stoller and Finis L. Harris},
  journal={Proceedings of the National Academy of Sciences of the United States of America},
  year={1993},
  volume={90 1},
  pages={307-11}
}
The present study determined the effect of organically quaternizing either of the two tertiary nitrogen sites of nicotine to assess the in vivo effects of the permanently ionized states of the synthesized N-[14C]methylnicotines on brain uptake in rat after intracarotid injection. Male Sprague-Dawley rats were used to measure the brain uptake index (BUI) by single-pass clearance in brain after rapid injection at pH 7.4 into the left common carotid artery (expressed as a percentage) relative to… CONTINUE READING