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Elucidation of neural GABA transporter function by developing novel subtype-selective inhibitors

Research Project

Project/Area Number 15K14960
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeMulti-year Fund
Research Field Pharmacology in pharmacy
Research InstitutionHokkaido University

Principal Investigator

MINAMI Masabumi  北海道大学, 薬学研究院, 教授 (20243040)

Co-Investigator(Renkei-kenkyūsha) SHUTO Satoshi  北海道大学, 大学院薬学研究院, 教授 (70241346)
Project Period (FY) 2015-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywords脳・神経 / 薬理学 / 有機化学 / GABA / トランスポーター / 創薬
Outline of Final Research Achievements

Compound B, a candidate of the selective inhibitor for the BGT-1 subtype of the GABA transporters, showed an antidepressant effect in the tail suspension test. This compound showed high binding affinity and agonistic activity on GABAA receptors. It did not bind to GABAB receptors. These results suggested that the antidepressant effect of the compound B is due to the inhibition of BGT-1 or the combined action of BGT-1 inhibition and GABAA receptor activation. In order to obtain a compound which does not act on GABA receptors but inhibits BGT-1 selectively, four compounds were newly synthesized. However, none of them showed BGT-1 inhibitory effect.

Report

(3 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • Research Products

    (4 results)

All 2016 Other

All Presentation (2 results) Remarks (2 results)

  • [Presentation] 新規GABAトランスポーター阻害薬候補化合物の薬理活性評価2016

    • Author(s)
      佐藤孝行、井川ありさ、圓山智嘉史、末政亮大、小林嵩明、有澤光弘、井手聡一郎、周東智、南雅文
    • Organizer
      日本薬学会薬理系薬学部会 次世代を担う創薬・医療薬理シンポジウム2016
    • Place of Presentation
      東北大学(宮城県・仙台市)
    • Year and Date
      2016-08-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] GABAトランスポーターサブタイプ特異的な新規阻害薬候補化合物の薬理活性評価2016

    • Author(s)
      佐藤孝行、井川ありさ、圓山智嘉史、末政亮大、小林嵩明、有澤光弘、井手聡一郎、周東智、南雅文
    • Organizer
      日本薬学会第136年会
    • Place of Presentation
      パシフィコ横浜(神奈川県・横浜市)
    • Year and Date
      2016-03-26
    • Related Report
      2015 Research-status Report
  • [Remarks] 北海道大学大学院薬学研究院 医療薬学部門 医療薬学分野 薬理学研究室

    • URL

      http://www.pharm.hokudai.ac.jp/yakuri/index.html

    • Related Report
      2016 Annual Research Report
  • [Remarks] 北海道大学大学院薬学研究院 医療薬学部門 医療薬学分野 薬理学研究室

    • URL

      http://www.pharm.hokudai.ac.jp/yakuri/

    • Related Report
      2015 Research-status Report

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Published: 2015-04-16   Modified: 2018-03-22  

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