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[99mTc(CO)3]+ and [99mTcO2]+ Radiolabeled Cyclic Melanotropin Peptides for Melanoma SPECT Imaging

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The melanoma targeting peptides (Ala-triazol)Ac-Re(Arg11)CCMSH and N4-CO-Re(Arg11)CCMSH were radiolabeled with [99mTc(CO)3]+ and [99mTcO2]+, respectively, and examined for in vitro cell binding, in vivo biodistribution and imaging properties. The (Ala-triazol)Ac-Re(Arg11)CCMSH and N4-CO-Re(Arg11)CCMSH were synthesized as protected peptides on resin followed by rhenium cyclization with [(C6H5)3P]2ReOCl3 in DMF. The peptides were labeled with 99mTc and examined for radiochemical stability and melanoma cell binding. In vivo biodistribution and SPECT/CT imaging studies were performed in B16/F1 melanoma tumor bearing C57 mice. 99mTc(CO)3-(Ala-Triazol)Ac- Re(Arg11)CCMSH and 99mTcO2-N4-CO-Re(Arg11)CCMSH were stable and internalized in B16/F1 melanoma cells upon binding. In vivo biodistribution studies revealed that tumor uptake of 99mTc(CO)3-(Ala-Triazol)Ac-Re(Arg11)CCMSH was 6.08±1.06% ID/g and 7.05±1.48% ID/g at 2 h and 4 h post injection, respectively. Tumor uptake of 99mTcO2-N4-CORe(Arg11)CCMSH was 7.54±1.82% ID/g and 2.28±0.22% ID/g at 1 h and 2 h post injection, respectively. SPECT/CT imaging studies showed that tumor selective uptake of the radiolabeled peptides, which was confirmed by competitive blocking studies.
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Keywords: MC1-R; melanoma; peptide; radioimaging; technetium; tetraamine; tricarbonyl

Document Type: Research Article

Publication date: June 1, 2014

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  • Current Radiopharmaceuticals publishes original research articles, letters, reviews, drug clinical trial studies and guest edited issues on all aspects of research and development of radiolabelled compound preparations. The scope of the journal covers the following areas: radio imaging techniques, therapies; preparation and application of radionuclide compounds including the incorporation of tracer methods used in scientific research and applications.
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