کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10553542 | 967830 | 2011 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A rapid vesicle electrokinetic chromatography method for the in vitro prediction of non-specific binding for potential PET ligands
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کلمات کلیدی
AOTPoPCEKCNSBLiposome electrokinetic chromatographynon-specific binding - اتصال غیر اختصاصیPositron emission tomography - توموگرافی گسیل پوزیترونBBB - سد خونی مغزیblood brain barrier - سد خونی مغزیImmobilized artificial membrane - غشای مصنوعی ImmobilizedIAM - من هستمPET - پتelectrokinetic chromatography - کروماتوگرافی الکترو کینتیک
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
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چکیده انگلیسی
High non-specific binding (NSB) is one of the most common reasons for candidate failure in potential positron emission tomography (PET) radiotracer development. It is of interest to develop high throughput in vitro methods for predicting non-specific binding prior to radiolabeling, which would help guide radiotracer candidate selection and assist decision making in new radiotracer discovery. We evaluated several electrokinetic chromatographic (EKC) systems to help identify PET ligands with low non-specific binding characteristics by mimicking the ligand-brain tissue interaction. The measured retention factors of tracers in clinical use or terminated candidates within AOT vesicle EKC systems were compared with literature in vitro or in vivo NSB data. We conclude that there is a statistical correlation between the chromatographic retention parameters of tested drugs and their NSB. The AOT vesicle EKC method can provide NSB in vitro trend analysis for a large number of drug candidates early in the novel radiotracer discovery process with minimal resources.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 54, Issue 4, 25 March 2011, Pages 722-729
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 54, Issue 4, 25 March 2011, Pages 722-729
نویسندگان
Zhengjin Jiang, John Reilly, Brian Everatt, Emmanuelle Briard,