A <sup>99m</sup>Tc-tricine-HYNIC-labeled Peptide Targeting the Melanocortin-1 Receptor for Melanoma Imaging
| Author | Danial Shamshirian | en |
| Author | Mostafa Erfani | en |
| Author | Davood Beiki | en |
| Author | Maliheh Hajiramazanali | en |
| Author | Babak Fallahi | en |
| Issued Date | 2016-07-31 | en |
| Abstract | Melanocortin-1 (MC1) receptor is an attractive melanoma-specific target for the development of α-MSH peptide based imaging and therapeutic agents. In this work a new lactam bridge α-MSH analogue was synthesized and radiolabeled with 99mTc via HYNIC chelator and tricine as co-ligand. Also, stability in human serum, receptor bound internalization and tissue biodistribution in tumor bearing nude mice were thoroughly investigated. Radiolabeling with 99mTc was performed at high specific activities (163MBq/nmol) with an acceptable labeling yield (>98%). The radioligand showed specific internalization into B16/F10 cells (13.35 ± 0.9% at 4 h). In biodistribution studies, a receptor-specific uptake was observed in MC1 receptor positive organ so that after 4 h the tumor uptake was 4.51 ± 0.11 % ID/g. Predominant renal excretion pathway with a highest accumulation of activity in tumor was observed for this radiopeptide. Obtained results show that the new designed labeled peptide conjugate can be a suitable candidate for diagnosis of metastatic melanomas. | en |
| DOI | https://doi.org/10.22037/ijpr.2016.1880 | en |
| Keyword | α-MSH | en |
| Keyword | <sup>99</sup>mTc | en |
| Keyword | Tricine | en |
| Keyword | HYNIC | en |
| Keyword | Radiopeptide | en |
| Publisher | Brieflands | en |
| Title | A <sup>99m</sup>Tc-tricine-HYNIC-labeled Peptide Targeting the Melanocortin-1 Receptor for Melanoma Imaging | en |
| Type | Original Article | en |
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