國家衛生研究院 NHRI:Item 3990099045/16241
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    題名: DBPR116, a prodrug of BPRMU191, in combination with naltrexone as a safer opioid analgesic than morphine via peripheral administration
    作者: Lin, SY;Chang, YC;Tien, YW;Kuo, YH;Chang, HF;Ou, LC;Chen, YP;Chang, KH;Hsu, YT;Huang, YC;Yang, CM;Law, PY;Xi, JH;Tao, PL;Loh, HH;Yeh, TK;Zhuang, H;Hsieh, HP;Shih, C;Chen, CT;Yeh, SH;Ueng, SH
    貢獻者: Institute of Biotechnology and Pharmaceutical Research;Center for Neuropsychiatric Research
    摘要: The development of opioid analgesics with reduced adverse effects is an unmet need. In a previous study, we discovered a unique combination of BPRMU191 and morphinan antagonists that produced potent antinociception with reduced adverse effects after central administration (intrathecal or intracerebroventricular). BPRMU191/naltrexone exhibits notable in vitro and in vivo pharmacological properties. However, the poor blood-brain barrier penetrative ability of BPRMU191 restricts its clinical application. In this study, we utilized a prodrug strategy to deliver sufficient brain concentrations of BPRMU191 and selected compound 2 (DBPR116) with the best physicochemical and pharmacological properties among other in vivo active prodrugs. The in vivo pharmacological studies of compound 2/naltrexone, including thermally stimulated pain, cancer pain, constipation, sedation, psychological dependence, heart rate, and respiratory frequency measurements, demonstrated that it was a safer opioid analgesic than morphine in pain control.
    日期: 2024-10-29
    關聯: Journal of Medicinal Chemistry. 2024 Oct 29;Article in Press.
    Link to: http://dx.doi.org/10.1021/acs.jmedchem.4c02107
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
    顯示於類別:[葉修華] 期刊論文
    [翁紹華] 期刊論文
    [林書玉] 期刊論文
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    [莊宏] 期刊論文
    [謝興邦] 期刊論文
    [石全(2014-2017)] 期刊論文
    [陳炯東] 期刊論文
    [陶寶綠] 期刊論文

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