國家衛生研究院 NHRI:Item 3990099045/10299
English  |  正體中文  |  简体中文  |  全文笔数/总笔数 : 12145/12927 (94%)
造访人次 : 909322      在线人数 : 790
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/3990099045/10299


    题名: 1-(2,4-Dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one: A novel opioid receptor agonist with less accompanying gastrointestinal dysfunction than morphine
    作者: Chao, PK;Ueng, SH;Ou, LC;Yeh, TK;Chang, WT;Chang, HF;Chen, SC;Tao, PL;Law, PY;Loh, HH;Cheng, MF;Chuang, JY;Chen, CT;Shih, C;Yeh, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Center for Neuropsychiatric Research
    摘要: BACKGROUND: The authors investigated the pharmacology and signaling pathways of the opioid receptors modulated by compound 1, 1-(2,4-dibromophenyl)-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one. METHODS: In vitro studies of compound 1 were assessed by using a radioligand-binding assay (n = 3), a cyclic adenosine monophosphate assay (n = 3), a beta-arrestin assay (n = 3), an internalization assay (n = 3), and an immunohistochemistry (n = 8). In vivo studies of compound 1 were characterized using a tail-flick test (n = 5 to 6), tail-clip test (n = 7), von Frey hair test (n = 5), and charcoal meal test (n = 5). RESULTS: Compound 1 elicited robust effects in mu-opioid (mean +/- SD; binding affinity: 15 +/- 2 nM; cyclic adenosine monophosphate assay: 24 +/- 6 nM), delta-opioid (82 +/- 7 nM; 1.9 +/- 0.1 muM), and kappa-opioid (76 +/- 9 nM; 1.4 +/- 0.5 muM) receptor-expressing cells. Compound 1 acts as a full agonist of beta-arrestin-2 recruitment in mu-opioid (1.1 +/- 0.3 muM) and delta-opioid (9.7 +/- 1.9 muM) receptor-expressing cells. Compound 1 caused less gastrointestinal dysfunction (charcoal meal test: morphine: 82 +/- 5%; compound 1: 42 +/- 5%) as well as better antinociception in mechanical pain hypersensitivity (tail-clip test: morphine: 10 +/- 3 s; compound 1: 19 +/- 1 s) and in cancer-induced pain (von Frey hair test: morphine: 0.1 +/- 0.1 g; compound 1: 0.3 +/- 0.1 g) than morphine at equi-antinociceptive doses. CONCLUSIONS: Compound 1 produced antinociception with less gastrointestinal dysfunction than morphine.
    日期: 2017-05
    關聯: Anesthesiology. 2017 May;126(5):952-966.
    Link to: http://dx.doi.org/10.1097/aln.0000000000001568
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0003-3022&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000402746000021
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85013127588
    显示于类别:[翁紹華] 期刊論文
    [葉燈光] 期刊論文
    [陳炯東] 期刊論文
    [石全(2014-2017)] 期刊論文
    [葉修華] 期刊論文
    [陶寶綠] 期刊論文

    文件中的档案:

    档案 描述 大小格式浏览次数
    PUB28212204.pdf2810KbAdobe PDF494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