preparation and preliminary biological evaluation of [153sm] samarium amd3100; towards a possible therapeutic chemokine receptor cxcr4 targeting complex
نویسندگان
چکیده
introduction: in continuation of recent development of possible c-x-c chemokine receptor type 4 (cxcr4) imaging agents, we report the development of a possible cxcr4 targeted therapy agent. methods: [153sm]labeled 1,1′-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo -tetradecane ([153sm]-amd3100) was prepared using [153sm]smcl3 and amd-3100 for 24h at 50°c in acetate buffer.stability tests, partition coefficient determination, toxicity tests and biodistribution studies of the complex in wild-type rats were determined. results: the radiolabeled complex was prepared in high radiochemical purity (>95%; rtlc and >99% hplc) and specific activity of 278 gbq/mmol and demonstrated significant stability up to 48h at 37 °c (in presence of human serum). partition coefficient determination was calculated log p= -1.09.hepatotoxicity experiments demonstrated no distinguishable effect on hepatic enzymes in 10 days post injection.initial complex biodistribution data showed significant liver and kidney accumulation in wild-type rats. conclusion: since lung and spleen are considered as cxcr4 rich organs, the best lung/blood and spleen/blood ratios were achieved 12 and 7 at 24 h post injection. further investigations are needed especially on therapeutic properties of this agent.
منابع مشابه
Preparation and preliminary biological evaluation of [153Sm] samarium AMD3100; towards a possible therapeutic chemokine receptor CXCR4 targeting complex
Introduction: In continuation of recent development of possible C-X-C chemokine receptor type 4 (CXCR4) imaging agents, we report the development of a possible CXCR4 targeted therapy agent. Methods: [153Sm]labeled 1,1′-[1,4-phenylenebis(methylene)] bis-1,4,8,11-tetraazacyclo -tetradecane ([153Sm]-AMD3100) was prepared using [153Sm]SmCl3 and AMD-3100 ...
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عنوان ژورنال:
iranian journal of nuclear medicineناشر: tehran university of medical sciences
ISSN 1681-2824
دوره 23
شماره 1 2014
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