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2022 Fiscal Year Final Research Report

Development of Poten Analgesics without Drug Dependence

Research Project

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Project/Area Number 20K06943
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
Research InstitutionKitasato University

Principal Investigator

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

Project Period (FY) 2020-04-01 – 2023-03-31
Keywordsオピオイド / μ受容体 / スプライスバリアント
Outline of Final Research Achievements

We attempted to develop agonists for the morphine-insensitive mu opioid receptor splice variants (MRP-insensitive SV), which amidino-TAPA interact with, as potent analgesics without drug dependence. At first, we attempted to develop an in vitro functional assay system for the MRP-insensitive SV but the attempt is not complete at present. Therefore, we conducted to develop the binding assay system for the MRP-insensitive SV as an alternative to the functional assay. The attempt to optimize the assay conditions revealed the critical factors to improve the assay system.
Based on the lead compound SYK-823, we designed and synthesized several morphinan derivatives with the substituent bearing phenyl group at the 4, 5, or 6-position to find four potential compounds.

Free Research Field

創薬科学

Academic Significance and Societal Importance of the Research Achievements

薬物依存性等の副作用の無い強力鎮痛薬の開発は医療上の重要な課題である。また、オピオイド鎮痛薬の過剰摂取による死亡例の急増(オピオイド・クライシスと称される)が、欧米をはじめ世界的に社会問題化している。よって本研究課題の解決は、重篤な疼痛に苦しむ患者はもとより医療従事者にも福音をもたらすばかりでなく、オピオイド・クライシスと称される社会問題に対する解決につながることが期待できる。
また、本研究の標的タンパク質は、通常7回膜貫通型であるGタンパク共役受容体(GPCR)にもかかわらず6回膜貫通型のものを含んでおり、研究がほとんど進んでいない6回膜貫通型GPCRの研究に光を当てるものである。

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Published: 2024-01-30  

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