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

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Title Synthesis and Radiobiological Evaluation of a new 99mTc-Labeled small Peptide:99mTc-YGGSLAK as Imaging Agent
 
Creator De, Kakali
Chandra, Susmita
Ganguly, Santanu
Sarkar, Bhart
Misra, Mridula
 
Subject Infectious Diseases and Immunology
 
Description 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.
 
Date 2011
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/114/1/JOURNAL_OF_CELLULAR_PHYSIOLOGY%2C226(1)%2C158%2D164%2C2011[112].pdf
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.
 
Relation http://www.eprints.iicb.res.in/114/