کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5529064 1548828 2017 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Effect of methoxy group position on biological properties of 18F-labeled benzyl triphenylphosphonium cations
ترجمه فارسی عنوان
تأثیر موقعیت گروه متوسوسی بر خواص بیولوژیکی کاتیونهای بنزیل ترفنفیل فسفونیوم بنفش
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی تحقیقات سرطان
چکیده انگلیسی

Introduction18F-labeled phosphonium cations targeting mitochondrial membrane potential would be promising for positron emission tomography (PET) myocardial perfusion imaging (MPI). The purpose of this study was to examine the influence of additional methoxy group and its different positions on myocardium uptake and pharmacokinetics properties of 18F-labeled benzyl triphenylphosphonium cations.MethodIn this study, three novel 18F-labeled phosphonium cations, [18F]4-(fluoromethyl)benzyltris(4-methoxyphenyl) phosphonium cation (1b), [18F]4-(fluoromethyl)benzyltris(2-methoxyphenyl) phosphonium cation (2b) and [18F]4-(fluoromethyl)benzyltris(3-methoxyphenyl) phosphonium cation (3b), were efficiently prepared by a One-Pot method starting from the substitution of non-carried-added fluoride-18. Radiotracers were purified by HPLC. Physicochemical properties, in vitro cell uptake assay, in vivo mice biodistribution and rat micro-PET imaging were investigated.ResultsResults suggested that the position of methoxy group exhibited significant effect on the biological properties of 18F-labeled benzyl triphenylphosphonium cations. The addition of methoxy group on orth- or meta-position of the radiotracers accelerated the radioactivity clearance from liver. The para-radiotracer had the highest uptake in the heart and other non-targeting organs. According to the biodistribution data, 2b (ortho-) displayed the fastest liver clearance and highest heart-to-background ratios. And its rat micro-PET images at 60 min post-injection revealed a good visualization of heart and favorable heart-to-background contrast. Nevertheless, 2b exhibited a lower initial liver uptake and quicker liver clearance compared with 99mTc-sestamibi.ConclusionThe ortho- compound (2b) displayed the most favorable biological properties as a potential MPI agent to acquire high contrast images early after injection.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Nuclear Medicine and Biology - Volume 49, June 2017, Pages 16-23
نویسندگان
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