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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4
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
نویسندگان
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