Synthesis and Radiobiological Evaluation of a new 99mTc-Labeled small Peptide:99mTc-YGGSLAK as Imaging Agent

De, Kakali and Chandra, Susmita and Ganguly, Santanu and Sarkar, Bhart and Misra, Mridula (2011) Synthesis and Radiobiological Evaluation of a new 99mTc-Labeled small Peptide:99mTc-YGGSLAK as Imaging Agent. Journal of Labelled Compounds Radiopharmaceuticals, 54. pp. 374-381.

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    Abstract

    Peptides are known as receptor-specific molecules that play an important role not only in diagnosis and therapy of neoplastic diseases, but also in the pathogenesis of other diseases. In an effort to develop a peptide-based radiopharmaceutical for scintigraphic studies, a small peptide Tyr-Gly-Gly-Ser-Leu-Ala-Lys (YGGSLAK) was synthesized by Fmoc solid-phase peptide synthesis using an automated synthesizer. This peptide was analyzed by TLC, HPLC and mass spectroscopy. Then, we investigated its analytical and pharmacokinetic study after radiolabeling with technetium-99m (99mTc) using SnCl2. The radiochemical purity of the complex was over 95% and log p value was 1.46. In vivo biodistribution studies in rat showed that most activity of this injected radiolabeled peptide (99mTc-YGGSLAK) was accumulated in the liver and followed by gallbladder, intestines and kidney. Scintigraphy studies on rabbits also showed very high uptake and retention in the liver and gallbladder, and after 1 h slowly excreted through the hepatobiliary system and a little amount was also excreted through the renal system. The radiochemical and in vitro and in vivo characterization indicates that 99mTc-YGGSLAK has certain favorable properties and it might be used as a new radiopharmaceutical for hepatobiliary scintigraphy.

    Item Type: Article
    URI: http://www.eprints.iicb.res.in/id/eprint/114
    Subjects: Infectious Diseases and Immunology
    Divisions: Indian Institute of Chemical Biology
    Depositing User: Ms Sutapa Ganguly
    Date Deposited: 29 Sep 2011 14:52
    Last Modified: 20 Jan 2012 12:59
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