کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2485382 | 1114353 | 2013 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Chlorothiazide is a Substrate for the Human Uptake Transporters OAT1 and OAT3
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Chlorothiazide is a Substrate for the Human Uptake Transporters OAT1 and OAT3 Chlorothiazide is a Substrate for the Human Uptake Transporters OAT1 and OAT3](/preview/png/2485382.png)
چکیده انگلیسی
The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, because of the poor passive permeability of the drug, it is likely that uptake transporters on the basolateral membrane are also involved to facilitate vectorial transport in the renal proximal tubule. Two suggested candidate transporters for this role are the human organic anion transporters, OAT1 and OAT3. By using mammalian cells stably expressing these transporters, we have demonstrated OAT1- and OAT3-dependent uptake of chlorothiazide with Michaelis constant values of 14.5 and 37.6 µM, respectively. Furthermore, we have found that probenecid, furosemide, and diclofenac inhibit chlorothiazide transport by OAT1 and OAT3, of which the probenecide-mediated inhibition may be of clinical importance. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:1683-1687, 2013
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 5, May 2013, Pages 1683-1687
Journal: Journal of Pharmaceutical Sciences - Volume 102, Issue 5, May 2013, Pages 1683-1687
نویسندگان
Viktória Juhász, Erzsébet Beéry, Zoltán Nagy, Annamária Bui, Ãva Molnár, Joseph Krisjanis Zolnerciks, Rémi Magnan, Márton Jani, Peter Krajcsi,