کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9002493 | 1118588 | 2005 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Characterization of antinociceptive activity of novel endomorphin-2 and morphiceptin analogs modified in the third position
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Characterization of antinociceptive activity of novel endomorphin-2 and morphiceptin analogs modified in the third position Characterization of antinociceptive activity of novel endomorphin-2 and morphiceptin analogs modified in the third position](/preview/png/9002493.png)
چکیده انگلیسی
In the present study we investigated and compared the in vivo analgesia of centrally administered endomorphin-2 and morphiceptin, and their analogs modified in position 3. Two series of analogs were synthesized by introducing unnatural aromatic amino acids in the d configuration: 3-(1-naphthyl)-d-alanine (d-1-Nal), 3-(2-naphthyl)-d-alanine (d-2-Nal), 3-(4-chlorophenyl)-d-alanine (d-ClPhe), 3-(3,4-dichlorophenyl)-d-alanine (d-Cl2Phe). Antinociceptive activity of endomorphin-2, morphiceptin, and their analogs was compared in the mouse hot-plate test, performed after i.c.v. administration of the peptides at a dose of 10 μg/animal. The best results were obtained for two morphiceptin analogs, [d-Phe3]morphiceptin and [d-1-Nal3]morphiceptin, which showed greatly improved analgesic activity, as compared to morphiceptin. In the endomorphin-2 series none of the modifications produced analogs more potent than the parent compound, but [d-1-Nal3]endomorphin-2 was the best analog. Antinociception induced by endomorphin-2 was reversed by concomitant i.c.v. administration of [d-Phe3]endomorphin-2, [d-2-Nal3]endomorphin-2, and [d-2-Nal3]morphiceptin, indicating that these analogs were weak μ-opioid antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 69, Issue 1, 1 January 2005, Pages 179-185
Journal: Biochemical Pharmacology - Volume 69, Issue 1, 1 January 2005, Pages 179-185
نویسندگان
Jakub Fichna, Jean-Claude do-Rego, Piotr Kosson, Jean Costentin, Anna Janecka,