國家衛生研究院 NHRI:Item 3990099045/14384
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    题名: Selective and antagonist-dependent µ-opioid receptor activation by the combination of 2-{[2-(6-chloro-3,4-dihydro-1(2H)-quinolinyl)-2-oxoethyl]sulfanyl}-5-phenyl-4,6-(1H,5H)-pyrimidinedione and naloxone/naltrexone
    作者: Lin, SY;Tien, YW;Ke, YY;Chang, YC;Chang, HF;Ou, LC;Law, PY;Xi, JH;Tao, PL;Loh, HH;Chao, YS;Shih, C;Chen, CT;Yeh, SH;Ueng, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research;Center for Neuropsychiatric Research
    摘要: We identified, via high-throughput screening using a FLIPR® calcium assay, compound 1, which incorporated a dihydroquinolinyl-2-oxoethylsulfanyl-(1H,5H)-pyrimidinedione core and activated the μ-opioid receptor (MOR) in the presence of naloxone or naltrexone. A structure-activity relationship study of the analogs of 1 led to the design of compound 21, which activated MOR in the presence of naloxone with an EC(50) of 3.3 ± 0.2 μM. MOR activation by the compound 21-antagonist pair was antagonist-dependent. Compound 21 did not affect the potency of the orthosteric agonist, morphine, toward MOR, indicating that it affected the function of MOR antagonists rather than that of the agonists. Computer modeling of the compound 21-MOR-naloxone complex revealed major interactions between compound 21 and MOR, including hydrogen bonding with Ser196, π-π stacking with Tyr149, and sulfur-aromatic interaction with Trp192. This study may pave the way for developing agents capable of safe and effective MOR modulation.
    日期: 2022-11
    關聯: Bioorganic Chemistry. 2022 Nov;128:Article number 105905.
    Link to: http://dx.doi.org/10.1016/j.bioorg.2022.105905
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0045-2068&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000859336700001
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85132836559
    显示于类别:[翁紹華] 期刊論文
    [葉修華] 期刊論文
    [陳炯東] 期刊論文
    [石全(2014-2017)] 期刊論文
    [趙宇生(2002-2013)] 期刊論文
    [陶寶綠] 期刊論文
    [林書玉] 期刊論文

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