کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9001450 | 1557916 | 2005 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and antinociceptive activity of cyclic endomorphin-2 and morphiceptin analogs
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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: Synthesis and antinociceptive activity of cyclic endomorphin-2 and morphiceptin analogs Synthesis and antinociceptive activity of cyclic endomorphin-2 and morphiceptin analogs](/preview/png/9001450.png)
چکیده انگلیسی
Cyclic analogs of the opioid peptides endomorphin-2 and morphiceptin of the type Tyr-X-Phe-Phe-Y-NH2 and Tyr-X-Phe-d-Pro-Y-NH2 (X = Lys or Asp and Y = Lys or Asp), respectively, were synthesized in order to test their structure-activity relationships. Antinociceptive activity of the new analogs was assessed in the hot-plate test after intracerebroventricular administration in mice. The strong analgesic effect was observed for the analogs with Asp in position 2, while the analogs with Lys in the second position were inactive. Antinociception caused by Asp2 analogs was dose-dependent and reversed by the concomitant administration of the universal opioid antagonist naloxone and by the selective κ antagonist, nor-BNI. However, receptor binding studies revealed poor affinity of all cyclic analogs at the μ-opioid receptor and no affinity at δ- and κ-opioid receptors. It is most likely that the new cyclic analogs produced their antinociception by the release of dynorphin A, which subsequently acted on the κ-opioid receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 71, Issues 1â2, 19 December 2005, Pages 188-195
Journal: Biochemical Pharmacology - Volume 71, Issues 1â2, 19 December 2005, Pages 188-195
نویسندگان
Anna Janecka, Jakub Fichna, Rafal Kruszynski, Yusuke Sasaki, Akihiro Ambo, Jean Costentin, Jean-Claude do-Rego,