In vivo and in vitro evidence of blood-brain barrier transport of a novel cationic arginine-vasopressin fragment 4-9 analog.

@article{Tanabe1999InVA,
  title={In vivo and in vitro evidence of blood-brain barrier transport of a novel cationic arginine-vasopressin fragment 4-9 analog.},
  author={Serabi Tanabe and Yasuyuki Shimohigashi and Yasuhide Nakayama and Toshiyuki Makino and Tetsuro Fujita and Takeru Nose and Gozoh Tsujimoto and Teruo Yokokura and Mikihiko Naito and Takashi Tsuruo and Tetsuya Terasaki},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={1999},
  volume={290 2},
  pages={561-8}
}
The blood-brain barrier (BBB) transport and metabolism of a novel arginine-vasopressin fragment 4-9 [AVP(4-9), isoelectric point; (pI) = 9.2] analog, that is, cationic AVP(4-9) (C-AVP(4-9), PI = 9.8), were examined in vivo and in vitro. At 45 min after an i.v. administration to mice, the cerebrum-to-plasma concentration ratios of (35)S-labeled AVP(4-9) and (125)I-labeled C-AVP(4-9) were 0.103 and 0.330 ml/g cerebrum, respectively, and the BBB permeation clearances were 1.47 x 10(-4) and 3.10 x… CONTINUE READING
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