2012 Fiscal Year Final Research Report
Prediction of the human brain distribution for the central nervous system drugs using a novel human immortalized brain capillary endothelial cells
| Project/Area Number |
22590144
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Medical pharmacy
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| Research Institution | Teikyo University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
OKURA Takashi 帝京大学, 薬学部, 准教授 (80326123)
KATO Sayaka 帝京大学, 薬学部, 助教 (70505940)
HIGUCHI Kei 帝京大学, 薬学部, 助教 (10625304)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 血液脳関門 / ヒト細胞株 / トランスポーター / カチオン性薬物 / 脳移行性 / 遺伝子解析 / スケールアップ |
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| Research Abstract |
Prediction of the brain distribution of drugs, based on the transport function of the human blood-brain barrier (BBB), is important for not only development of new central nervous system (CNS)-acting drugs, but also pharmacotherapy for CNS diseases. The purpose of this study is to clarify the functional expression of cation transporters using human brain capillary endothelial cell line hCMEC/D3 (D3), an in vitro model. The study was also investigated whether or not the results of in vitro uptake study using D3 cells can be extrapolated to human BBB. In this study, it was found that cationic transporters (OCTN2, OCTN1, PMAT and H^+/organic cation antiporter) are functionally expr essed in D3 cells. Further, a method can be established for extrapolating brain distribution of theCNS-acting drugs in human from the in vitro data using D3 cells.
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