Functional characterization of adenosine transport across the BBB in mice

Hideyasu Murakami, Airi Ohkura, Hitomi Takanaga, Hirotami Matsuo, Noriko Koyabu, Mikihiko Naito, Takashi Tsuruo, Hisakazu Ohtani, Yasufumi Sawada

Research output: Contribution to journalArticlepeer-review

15 Citations (Scopus)


We investigated transport characteristics of adenosine across the blood-brain barrier (BBB) in mice. Uptake clearance across the BBB was measured by using an in situ mouse brain perfusion technique and cultured mouse brain capillary endothelial cell line (MBEC4 cells). Nucleoside transporter was cloned by RT-PCR and expressed on Xenopus laevis oocyte. Both in situ and in vitro studies revealed that the adenosine uptake is concentration-dependent, Na +-independent and S-(p-nitrobenzyl)-6-thioinosine (NBMPR)-sensitive. The Kt values of in situ and in vitro studies were 31.7 ± 13.8 μM and 11.9 ± 2.84 μM, respectively. A good correlation was found for the inhibitory effects of nucleoside analogs to adenosine uptake between in situ and in vitro studies. RT-PCR revealed the expression of RNA of mouse equilibrative nucleoside transporter (mENT1) in mouse brain capillary and MBEC4 cells. In mENT1 expressed on X. laevis oocyte, Kt value of adenosine transport was 6.9 ± 2.7 μM (and comparable to those in situ and in vitro studies). In conclusion, we characterized the adenosine transport across the BBB in mice by using in situ brain perfusion technique and MBEC4 cells and found that these transports share common characteristics with mENT1-mediated transport. Transport of adenosine across the BBB in mice may be attributable to mENT1.

Original languageEnglish
Pages (from-to)37-44
Number of pages8
JournalInternational Journal of Pharmaceutics
Issue number1-2
Publication statusPublished - 2005 Feb 16
Externally publishedYes


  • Adenosine
  • Blood-brain barrier
  • Equilibrative nucleoside transporter

ASJC Scopus subject areas

  • Pharmaceutical Science


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