Evaluation of New 99mTc(CO)3 + Radiolabeled Glycylglycine In Vivo

Author(s): Ahmet M. Şenışık*, Çiğdem İçhedef, Ayfer Y. Kılçar, Eser Uçar, Kadir Arı, Yasemin Parlak, Elvan S. Bilgin, Serap Teksöz*.

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 19 , Issue 11 , 2019

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Graphical Abstract:


Abstract:

Background: Peptide-based agents are used in molecular imaging due to their unique properties, such as rapid clearance from the circulation, high affinity and target selectivity. Many of the radiolabeled peptides have been clinically experienced with diagnostic accuracy. The aim of this study was to investigate in vivo biological behavior of [99mTc(CO)3(H2O)3]+ radiolabeled glycylglycine (GlyGly).

Methods: Glycylglycine was radiolabeled with a high radiolabeling yield of 94.69±2%, and quality control of the radiolabeling process was performed by thin layer radiochromatography (TLRC) and High-Performance Liquid Radiochromatography (HPLRC). Lipophilicity study for radiolabeled complex (99mTc(CO)3-Gly-Gly) was carried out using solvent extraction. The in vivo evaluation was performed by both biodistribution and SPECT imaging.

Results: The high radiolabelling yield of 99mTc(CO)3-GlyGly was obtained and verified by TLRC and HPLRC as well. According to the in vivo results, SPECT images and biodistribution data are in good accordance. The excretion route from the body was both hepatobiliary and renal.

Conclusion: This study shows that 99mTc(CO)3-GlyGly has the potential to be used as a peptide-based imaging agent. Further studies, 99mTc(CO)3-GlyGly can be performed on tumor-bearing animals.

Keywords: Technetium tricarbonyl core, radiolabeling, glycylglycine, in vivo, SPECT imaging, biodistribution studies.

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Article Details

VOLUME: 19
ISSUE: 11
Year: 2019
Page: [1382 - 1387]
Pages: 6
DOI: 10.2174/1871520619666190404154723
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