KMID : 1148920110450040248
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Nuclear Medicine and Molecular Imaging 2011 Volume.45 No. 4 p.248 ~ p.254
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Radiosynthesis of 99mTc(CO)3-Clinafloxacin Dithiocarbamate and Its Biological Evaluation as a Potential Staphylococcus aureus Infection Radiotracer
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Shah Syed Qaiser
Khan Mohammad Rafiullah Ali Syed Mohammad
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Abstract
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Background: Clinafloxacin dithiocarbamate (CNND) was radiolabeled with technetium-99m (99mTc) using [99mTc(CO)3(H2O)3]+ and assessed for its radiochemical stability in saline and serum, its in vitro binding with methicillin-resistant Staphylococcus aureus (MRSA) and biodistribution in female nude mice (FNM) artificially infected with live and heat-killed MRSA.
Methods: In normal saline (NS) the 99mTc(CO)3-clinafloxacin dithiocarbamate (99mTc(CO)3-CNND) showed radiochemical stability with a maximum value of 99.10?¡¾?0.20% and remained stable up to 4 h (92.65?¡¾?0.18%).
Results: In human serum at 37¡ÆC within 16 h of incubation, 14.85% side products as a result of de-tagging developed. Incubation with MRSA gave saturated binding with a maximum value of 72.75?¡¾?1.20%. Almost six-fold higher uptake was seen in the infected muscle of the FNM as compared to the inflamed and normal muscle. The 99mTc(CO)3-CNND complex showed a normal route of excretion from the body of the FNM model.
Conclusion: The higher stability in NS, HS, saturated in vitro binding with a live strain of MRSA and six-fold higher uptake in the target organ showed the 99mTc(CO)3-CNND complex to be a potential MRSA infection radiotracer.
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KEYWORD
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99mTc(CO)3-Clinafloxacin dithiocarbamate complex, MRSA, Infection radiotracer
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