کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1377927 | 981991 | 2006 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Endomorphin-2 (EM-2) and morphiceptin are the same class of putative μ-opioid receptor ligands. To investigate the effectiveness of phenylglycine (Phg, l or d) and homophenylalanine (Hfe) as the surrogates of phenylalanine in the position 3 and/or 4 of them, a series of their analogues were synthesized. Opioid receptor binding affinities were determined. Two analogues, [Hfe3]EM-2 and [Phg4] (EM-2/morphiceptin), showed different but potent antinociceptive activity in mouse hot-plate test, the results combined with their half-lives of degradation by mouse brain homogenate could also present some evidence to the in vivo degradative mechanism of EM-2.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 14, 15 July 2006, Pages 3688–3692
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 14, 15 July 2006, Pages 3688–3692
نویسندگان
Yanfeng Gao, Xin Liu, Weixia Liu, Yuanming Qi, Xuefeng Liu, Yifeng Zhou, Rui Wang,