title: A99mTc-tricine-HYNIC-labeled Peptide Targeting the Melanocortin-1 Receptor for Melanoma Imaging.
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 with99mTc 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 with99mTc 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.
authors.affiliation: Department of Radiopharmacy, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Danial
authors.initials: D
authors.lastname: Shamshirian
authors.affiliation: Radiation Application Research School, Nuclear Science and Technology Research Institute (NSTRI), Tehran, Iran.
authors.forename: Mostafa
authors.initials: M
authors.lastname: Erfani
authors.affiliation: Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Davood
authors.initials: D
authors.lastname: Beiki
authors.affiliation: Department of Radiopharmacy, School of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Maliheh
authors.initials: M
authors.lastname: Hajiramazanali
authors.affiliation: Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran.
authors.forename: Babak
authors.initials: B
authors.lastname: Fallahi
keywords: 99mTc; HYNIC; Radiopeptide; Tricine; α-MSH