In silico and in vivo study of radio-iodinated nefiracetam as a radiotracer for brain imaging in mice
Author:
Sanad M. H.1, Farag A. B.2, Rizvi S. F. A.3
Affiliation:
1. Labeled Compounds Department , Hot Laboratories Center, Egyptian Atomic Energy Authority , P.O. Box 13759 , Cairo , Egypt 2. Pharmaceutical Chemistry Department , Faculty of Pharmacy, Ahram Canadian University , Giza , Egypt 3. College of Chemistry and Chemical Engineering, Lanzhou University , Lanzhou 730000 , Gansu , PR China
Abstract
Abstract
This study presents development and characterization of a radiotracer, [125I]iodonefiracetam ([125I]iodoNEF). Labeling with high yield and radiochemical purity was achieved through the formation of a [125I]iodoNEF radiotracer after investigating many factors like oxidizing agent content (chloramines-T (Ch-T)), substrate amount (Nefiracetam (NEF)), pH of reaction mixture, reaction time and temperature. Nefiracetam (NEF) is known as nootropic agent, acting as N-methyl-d-aspartic acid receptor ligand (NMDA). The radiolabeled compound was stable, and exhibited the logarithm of the partition coefficient (log p) value of [125I]iodonefiracetam as 1.85 (lipophilic). Biodistribution studies in normal mice confirmed the suitability of the [125I]iodoNEF radiotracer as a novel tracer for brain imaging. High uptake of 8.61 ± 0.14 percent injected dose/g organ was observed in mice
Publisher
Walter de Gruyter GmbH
Subject
Physical and Theoretical Chemistry
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