Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique.

@article{Yamazaki1994TransportMO,
  title={Transport mechanism of an H1-antagonist at the blood-brain barrier: transport mechanism of mepyramine using the carotid injection technique.},
  author={Mayako Yamazaki and Hidenori Fukuoka and Osamu Nagata and Hiroharu Kato and Yoshio Ito and Tetsuya Terasaki and Akira Tsuji},
  journal={Biological & pharmaceutical bulletin},
  year={1994},
  volume={17 5},
  pages={676-9}
}
The blood-brain barrier (BBB) permeability of mepyramine was measured by the carotid injection technique to elucidate the transport mechanism of an H1-antagonist in the central nervous system. Mepyramine was found to enter the brain by saturable and carrier-mediated transport. The in vivo kinetic parameters were estimated as follows: the maximum uptake rate (Jmax) was 7.12 +/- 1.37 mumol/min/g of brain, the Michaelis constant (Kt) was 4.40 +/- 2.00 mM, and the nonsaturable first order rate (Kd… CONTINUE READING
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