Molecular mechanisms of drug influx and efflux transport at the blood-brain barrier

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  • OHTSUKI Sumio
    Graduate School of Pharmaceutical Sciences New Industry Creation Hatchery Center, Tohoku University CREST of the Japan Science and Technology Corporation (JST)
  • HORI Satoko
    Graduate School of Pharmaceutical Sciences New Industry Creation Hatchery Center, Tohoku University CREST of the Japan Science and Technology Corporation (JST)
  • TERASAKI Tetsuya
    Graduate School of Pharmaceutical Sciences New Industry Creation Hatchery Center, Tohoku University CREST of the Japan Science and Technology Corporation (JST)

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Other Title
  • 血液脳関門の薬物透過と排出の分子機構―中枢支援防御システム―
  • ケツエキ ノウ カンモン ノ ヤクブツ トウカ ト ハイシュツ ノ ブンシ キコウ チュウスウ シエン ボウギョ システム
  • −中枢支援防御システム−

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The blood-brain barrier (BBB) segregates the circulating blood from interstitial fluid in the brain and restricts drug permeability into the brain. Recent studies have revealed that the BBB exhibits not only blood-to-brain influx transport for the supply of nutrients, but also brain-to-blood efflux transport to excrete drugs and endogenous compounds. The influx transport system allows drugs to enter the brain. L-DOPA is transported into the brain by the large neutral amino acid transport system, system L. A cationic µ-opioid peptide analogue enters the brain by adsorptive-mediated endocytosis. In contrast, efflux transport limits the distribution of drugs in the brain. The ATP binding cassette transporter B1 (ABCB1) mediates the efflux transport of lipophilic drugs at the BBB by using ATP energy. Furthermore, organic anion transporter 3 (OAT3) is expressed at the BBB and mediates the efflux transport of homovanillic acid, a dopamine metabolite. This efflux transport is also likely to be involved in the transport of anionic drugs such as 6-mercaptopurine and acyclovir. Clarifying the BBB transport could give us important information allowing the development of better CNS drugs and improving our understanding of the relationship between CNS diseases and BBB functions.<br>

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