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Development of selective agonists for the morphine-insensitive opioid mu receptor splice variants

Research Project

Project/Area Number 26460152
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Drug development chemistry
Research InstitutionKitasato University

Principal Investigator

Fujii Hideaki  北里大学, 薬学部, 教授 (30458757)

Co-Investigator(Renkei-kenkyūsha) HIRAYAMA Shigeto  北里大学, 薬学部, 助教 (40565842)
SAKURADA Shinobu  東北医科薬科大学, 薬学部, 客員教授 (30075816)
MIZOGUCHI Hirokazu  東北医科薬科大学, 薬学部, 教授 (30360069)
Project Period (FY) 2014-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Keywordsスプライスバリアント / オピオイド / μ受容体 / メサドン / モルヒナン
Outline of Final Research Achievements

To develop nonpeptidic agonists selective for the morphine-insensitive opioid mu receptor splice variants with which peptidic agonist amidino-TAPA can interact, we attempted to identify the pharmacophore for the splice variants. As a designed compound based on the methadone structure did not show any agonistic activities (antinociceptive effects), a working hypothesis that the Phe residue in amidino-TAPA would play an important role in eliciting its activities was not confirmed. The compounds evaluated in in vivo assays must have low or no binding affinities for the kappa receptor. Although we designed and synthesized several morphinan derivatives, only one compound among the synthesized ones fulfilled the criterion. Therefore, we have not yet found selective agonists. To achieve our investigation aims, we think that it is important to newly construct an in vitro assay which can evaluate the binding affinities and/or activities of the tested compounds for the splice variants.

Report

(4 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Research-status Report
  • 2014 Research-status Report
  • Research Products

    (8 results)

All 2017 2016 2015

All Presentation (8 results)

  • [Presentation] モルヒネ非感受性オピオイドμ受容体スプライスバリアント選択的作動薬を志向したモルヒナン誘導体の合成2017

    • Author(s)
      本城綾香、平山重人、唐木文霞、伊藤謙之介、藤井秀明
    • Organizer
      日本薬学会第137年会
    • Place of Presentation
      仙台
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2016

    • Author(s)
      鈴木あずさ、唐木文霞、平山重人、伊藤謙之介、藤井秀明
    • Organizer
      第47回 中部化学関係学協会支部連合秋季大会
    • Place of Presentation
      豊橋
    • Year and Date
      2016-11-05
    • Related Report
      2016 Annual Research Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2016

    • Author(s)
      鈴木あずさ、唐木文霞、平山重人、伊藤謙之介、藤井秀明
    • Organizer
      第60回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2016-09-17
    • Related Report
      2016 Annual Research Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2016

    • Author(s)
      鈴木あずさ、平山重人、唐木文霞、伊藤謙之介、藤井秀明
    • Organizer
      日本薬学会第136年会
    • Place of Presentation
      パシフィコ横浜(横浜)
    • Year and Date
      2016-03-28
    • Related Report
      2015 Research-status Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2015

    • Author(s)
      鈴木 あずさ、平山 重人、伊藤 謙之介、藤井 秀明
    • Organizer
      第70回記念有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      長岡高専(長岡)
    • Year and Date
      2015-11-21
    • Related Report
      2015 Research-status Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2015

    • Author(s)
      鈴木 あずさ、平山 重人、伊藤 謙之介、藤井 秀明
    • Organizer
      第9回北里化学シンポジウム
    • Place of Presentation
      北里大学(東京)
    • Year and Date
      2015-09-26
    • Related Report
      2015 Research-status Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2015

    • Author(s)
      鈴木 あずさ、平山 重人、伊藤 謙之介、藤井 秀明
    • Organizer
      第59回日本薬学会関東支部大会
    • Place of Presentation
      日本大学(船橋)
    • Year and Date
      2015-09-12
    • Related Report
      2015 Research-status Report
  • [Presentation] モルヒネ非感受性スプライスバリアントに選択的な作動薬の創製を志向したメサドン誘導体の合成2015

    • Author(s)
      鈴木あずさ、木浦和哉、平山重人、伊藤謙之介、藤井秀明
    • Organizer
      日本薬学会第135年会
    • Place of Presentation
      兵庫医療大学(神戸)
    • Year and Date
      2015-03-28
    • Related Report
      2014 Research-status Report

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Published: 2014-04-04   Modified: 2018-03-22  

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