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
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آنالیزی یا شیمی تجزیه
پیش نمایش صفحه اول مقاله
A rapid vesicle electrokinetic chromatography method for the in vitro prediction of non-specific binding for potential PET ligands
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
نویسندگان
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