کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9012302 | 1124554 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The suitability of iodinated Angiotensin-(1-7) peptides as pharmacological tools
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
Introduction: The heptapeptide Angiotensin-(1-7) [(Ang-(1-7)] is a biologically active component of the Renin-Angiotensin System. Pharmacological studies often involve Ang-(1-7) radioactively labelled with 125I. Given the small size of the original peptide, we investigated whether introduction of a rather bulky iodine label interferes with the biological activity of Ang-(1-7). Methods: Ang-(1-7) was labelled with nonradioactive iodine with the chloramine-T method. The reaction products were separated on HPLC and analysed with mass spectrometry. The products were tested for biological activity in two ways: The ability of labelled Ang-(1-7) to block Ang II-induced contraction in rat aortic rings was tested in an organ bath setup. The affinity of labelled angiotensin for ACE in rat plasma was examined in vitro. Results: Iodination of Angiotensin-(1-7) resulted in two main products: monoiodinated and diiodinated Ang-(1-7) that could be easily separated on HPLC. In an organ bath experiment, monoiodinated Ang-(1-7) blocked Ang II responses identical to the native compound, whereas diiodinated Ang-(1-7) had lost its ability to block Ang II responses. Likewise, monoiodinated Ang-(1-7) had retained its affinity for ACE, while the affinity of diiodinated Ang-(1-7) was greatly reduced. Discussion: Monoiodinated Ang-(1-7) has a biological activity identical to the native compound, whereas this is lost in diiodinated Ang-(1-7). Therefore, only the monoiodinated radioactive form seems suited for pharmacological studies.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmacological and Toxicological Methods - Volume 51, Issue 1, JanuaryâFebruary 2005, Pages 51-55
Journal: Journal of Pharmacological and Toxicological Methods - Volume 51, Issue 1, JanuaryâFebruary 2005, Pages 51-55
نویسندگان
Annemarieke E. Loot, Azuwerus van Buiten, Anton J.M. Roks, Robert H. Henning,