國家衛生研究院 NHRI:Item 3990099045/14521
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    题名: Benzo[b]thiophene-2-carboxamides as novel opioid receptor agonists with potent analgesic effect and reduced constipation
    作者: Kuppusamy, R;Hsu, YT;Ke, YY;Chang, PW;Chang, YC;Chang, HF;Wang, PC;Lin, YH;Huang, YC;Yeh, TK;Chuang, JY;Loh, HH;Shih, C;Chen, CT;Yeh, SH;Ueng, SH
    贡献者: Institute of Biotechnology and Pharmaceutical Research;NHRI Graduate Student Program
    摘要: Currently, there is a significant unmet need for novel analgesics with fewer side effects. In this study, we carried out structural modification of a hit compound previously identified in an artificial-intelligence (AI) virtual screening and discovered the potent analgesic, benzo[b]thiophene-2-carboxamide analog (compound 25) with new structural scaffold. We investigated the signaling pathways of opioid receptors mediated by compound 25, and found this racemic compound activated mu-opioid receptor through the cyclic adenosine monophosphate (cAMP) and β-arrestin-2-mediated pathways with strong potency and efficacy, and accompanying nociceptin-orphanin FQ opioid peptide and delta-opioid receptors through the cAMP pathway with weak potencies. Compound 25 elicited potent antinociception in thermal-stimulated pain (ED50 value of 127.1 ± 34.65 μg/kg) and inflammatory-induced allodynia models with less gastrointestinal transit inhibition and antinociceptive tolerance than morphine. Overall, this study revealed a novel analgesic with reduced risks of side effects.
    日期: 2022-12-05
    關聯: European Journal of Medicinal Chemistry. 2022 Dec 5;243:Article number 114728.
    Link to: http://dx.doi.org/10.1016/j.ejmech.2022.114728
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0223-5234&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000906679200004
    Cited Times(Scopus): https://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=85137302073
    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
    [葉燈光] 期刊論文

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