کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9917666 | 1556307 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Biphasic accumulation kinetics of [99mTc]-hexakis-2-methoxyisobutyl isonitrile in tumour cells and its modulation by lipophilic P-glycoprotein ligands
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کلمات کلیدی
CCCPSPET99mTc-MIBIMRP1R12318FDGPGPMDR2-[18F]fluoro-2-deoxy-d-glucose - 2- [18F] fluoro-2-deoxy-d-glycoseP-glycoprotein - P-گلیکوپروتئینCSA - ایالات مؤتلفهٔ آمریکاsingle photon emission computed tomography - توموگرافی کامپیوتری انتشار اتمی فوتونPositron emission tomography - توموگرافی گسیل پوزیترونRhodamine 123 - رودامین 123cyclosporin A - سیکلوسپورین AVer - مشاهده کنیدMultidrug resistance - مقاومت چند داروییVerapamil - وراپامیلPET - پتmultidrug resistance-associated protein - پروتئین مرتبط با مقاومت چند داروییcarbonyl cyanide m-chlorophenylhydrazone - کربنیل سیانید m-chlorophenylhydrazone
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
To study the accumulation and washout kinetics of [99mTc]-hexakis-2-methoxyisobutyl isonitrile (99mTc-MIBI) in MDR positive and MDR negative tumour cells and how this is modified by lipophilic P-glycoprotein ligands. Methods: The tumour cells were incubated in the presence and absence of the ligands and the uptakes of 99mTc-MIBI, rhodamine 123 and 2-[18F]fluoro-2-deoxy-d-glucose (18FDG) were measured. Results: The accumulation of 99mTc-MIBI in the tumour cells followed biphasic kinetics. Verapamil and cyclosporin A increased the membrane fluidity and significantly enhanced the 99mTc-MIBI uptake of the MDR negative cells, while the rhodamine 123 uptake was not affected. Verapamil significantly increased the uptake of rhodamine 123 and 18FDG but did not modify that of 99mTc-MIBI in the MDR positive cells. Cyclosporin A significantly increased the 18FDG uptake of the MDR positive and negative tumour cells; these effects were ouabain-sensitive. Depolarization of the cytoplasmic membrane, acidification of the extracellular medium and the administration of CCCP decreased the accumulation of 99mTc-MIBI and rhodamine 123 uptake in the tumour cells. Conclusions: Lipophilic P-glycoprotein ligands modified the biphasic accumulation kinetics of the 99mTc-MIBI uptakes of MDR negative and positive tumour cells in different and complex ways and could therefore mask the P-glycoprotein pump-dependent changes in tracer accumulation.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 25, Issues 2â3, June 2005, Pages 201-209
Journal: European Journal of Pharmaceutical Sciences - Volume 25, Issues 2â3, June 2005, Pages 201-209
نویسندگان
Teréz Márián, László Balkay, Gábor Szabó, Zoárd T. Krasznai, Zoltán Hernádi, László Galuska, Judit Szabó-Péli, Olga Ãsik, Lajos Trón, Zoltán Krasznai,