NDLI: Distribution, elimination, and renal handling of (99m)technetium-Demogastrin 1.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Trejtnar, Frantisek Laznickova, Alice Laznicek, Milan Novy, Zbynek Maina, Theodosia Nock, Berthold A. Behe, Martin
Description	Country affiliation: Czech Republic Author Affiliation: Trejtnar F ( Faculty of Pharmacy, Charles University in Prague, Hradec Kralove, Czech Republic. trejtnarf@faf.cuni.cz)
Abstract	Radiolabeled cholecystokinin/gastrin (CCK) receptor-targeting peptides are promising compounds for radiodiagnosis and radiotherapy of certain malignancies. This study evaluated the pharmacokinetic profile of a CCK-2 receptor-specific peptide, Demogastrin 1, labeled with technetium-99m ((99m)Tc-Demogastrin 1), in rats. To investigate the fate of (99m)Tc-Demogastrin 1 in the rat, biodistribution and elimination studies in vivo were performed, and elimination parameters in perfused rat liver and kidney were determined. Biodistribution studies showed that (99m)Tc-Demogastrin 1 was rapidly cleared from the blood and most organs. A significant amount of radioactivity was detected in the CCK-2 receptor-rich organs, such as the stomach. Low radioactivity was found in the CCK-1 receptor-rich organs. Radioactivity in bowels and stomach declined relatively slowly. High and long-term retention of radioactivity in the kidneys was observed. Elimination of (99m)Tc-Demogastrin 1 via the bile was negligible. A high and rapid renal excretion was observed in elimination experiments in vivo. In the perfused kidney, glomerular filtration was found to be the main renal excretion mechanism of (99m)Tc-Demogastrin 1. Demogastrin 1 was distributed preferentially to the organs expressing CCK-2 receptors. The decisive elimination route of (99m)Tc-Demogastrin 1 in rats was urinary excretion. A high and prolonged renal retention may limit potential clinical use of the compound.
File Format	HTM / HTML
ISSN	10849785
Issue Number	2
Volume Number	27
e-ISSN	15578852
Journal	Cancer Biotherapy & Radiopharmaceuticals
Language	English
Publisher	Mary Ann Liebert, Inc.
Publisher Date	2012-03-01
Publisher Place	United States
Access Restriction	Subscribed
Subject Keyword	Discipline Pharmacology Discipline Oncology Gastrins Pharmacokinetics Radiopharmaceuticals Technetium Animals Isotope Labeling Methods Kidney Metabolism Liver Male Rats Rats, Wistar Receptor, Cholecystokinin B Tissue Distribution Journal Article Research Support, Non-u.s. Gov't
Content Type	Text
Resource Type	Article
Subject	Radiology, Nuclear Medicine and Imaging Cancer Research Pharmacology Oncology

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