A 99mTc-tricine-HYNIC-labeled Peptide Targeting the Melanocortin-1 Receptor for Melanoma Imaging

Document Type: Research article

Authors

1 Department of Radiopharmacy, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

2 Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran

3 Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran

4 Department of Radiopharmacy, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.

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 hours). In biodistribution studies, a receptor-specific uptake was observed in MC1 receptor positive organ so that after 4 hours 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.

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Iranian Journal of Pharmaceutical Research

Volume 15, Issue 3
Summer 2016
Pages 349-360

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