國家衛生研究院 NHRI:Item 3990099045/15995
English  |  正體中文  |  简体中文  |  全文笔数/总笔数 : 12145/12927 (94%)
造访人次 : 907033      在线人数 : 827
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
搜寻范围 查询小技巧：
  • 您可在西文检索词汇前后加上"双引号"，以获取较精准的检索结果
  • 若欲以作者姓名搜寻，建议至进阶搜寻限定作者字段，可获得较完整数据
    •  进阶搜寻
    主页 ‧ 登入 ‧ 上传 ‧ 说明 ‧ 关于NHRI ‧ 管理 到手机版


    jsp.display-item.identifier=請使用永久網址來引用或連結此文件: http://ir.nhri.org.tw/handle/3990099045/15995


    题名: Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia
    作者: Huang, YH;Lin, SY;Ou, LC;Huang, WC;Chao, PK;Chang, YC;Chang, HF;Lee, PT;Yeh, TK;Kuo, YH;Tien, YW;Xi, JH;Tao, PL;Chen, PY;Chuang, JY;Shih, C;Chen, CT;Tung, CW;Loh, HH;Ueng, SH;Yeh, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Center for Neuropsychiatric Research;NHRI Graduate Student Program
    摘要: Morphinan antagonists, which block opioid effects at mu-opioid receptors, have been studied for their analgesic potential. Previous studies have suggested that these antagonists elicit analgesia with fewer adverse effects in the presence of the mutant mu-opioid receptor (MOR; S196A). However, introducing a mutant receptor for medical applications represents significant challenges. We hypothesize that binding a chemical compound to the MOR may elicit a comparable effect to the S196A mutation. Through high-throughput screening and structure-activity relationship studies, we identified a modulator, 4-(2-(4-fluorophenyl)-4-oxothiazolidin-3-yl)-3-methylbenzoic acid (BPRMU191), which confers agonistic properties to small-molecule morphinan antagonists, which induce G protein-dependent MOR activation. Co-application of BPRMU191 and morphinan antagonists resulted in MOR-dependent analgesia with diminished side effects, including gastrointestinal dysfunction, antinociceptive tolerance, and physical and psychological dependence. Combining BPRMU191 and morphinan antagonists could serve as a potential therapeutic strategy for severe pain with reduced adverse effects and provide an avenue for studying G protein-coupled receptor modulation.
    日期: 2024-07-17
    關聯: Cell Chemical Biology. 2024 Jul 17;Article in Press.
    Link to: http://dx.doi.org/10.1016/j.chembiol.2024.06.013
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=2451-9448&DestApp=IC2JCR
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85200421803
    显示于类别:[葉修華] 期刊論文
    [翁紹華] 期刊論文
    [童俊維] 期刊論文
    [陳炯東] 期刊論文
    [石全(2014-2017)] 期刊論文
    [葉燈光] 期刊論文
    [陶寶綠] 期刊論文
    [其他] 期刊論文
    [林書玉] 期刊論文

    文件中的档案:

    档案 描述 大小格式浏览次数
    PUB39025070.pdf5908KbAdobe PDF41检视/开启


    在NHRI中所有的数据项都受到原著作权保护.

    TAIR相关文章

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - 回馈