Paper Information

Journal:   IRANIAN JOURNAL OF NUCLEAR MEDICINE   WINTER 2015 , Volume 23 , Number 1 (SERIAL NUMBER 43); Page(s) 36 To 43.
 
Paper: 

PREPARATION AND PRELIMINARY BIOLOGICAL EVALUATION OF [153SM] SAMARIUM AMD3100, TOWARDS A POSSIBLE THERAPEUTIC CHEMOKINE RECEPTOR CXCR4 TARGETING COMPLEX

 
 
Author(s):  AGHANEJAD AYUOB, JALILIAN AMIR REZA*, BAHRAMI SAMANI ALI, BEIKI DAVOOD, MAUS STEPHAN, KHALAJ ALI
 
* NUCLEAR SCIENCE RESEARCH SCHOOL, NUCLEAR SCIENCE AND TECHNOLOGY RESEARCH INSTITUTE, TEHRAN, IRAN
 
Abstract: 

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 50oC 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 oC (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.

 
Keyword(s): AMD3100, TARGETED RADIOTHERAPY, RADIOLABELING, BIODISTRIBUTION, SM-153
 
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