Home | My Profile | Contact Us
Research Trends Products  |   order gateway  |   author gateway  |   editor gateway  
Register | Forgot Password

Author Resources
 Author Gateway
 Article submission guidelines

Editor Resources
 Editor/Referee Gateway

 Regional Subscription Agents/Distributors
Current Topics in Pharmacology   Volumes    Volume 23 
Single-dose extended-toxicity preclinical study on novel radiotracer formulations for use in the diagnosis of neuroendocrine tumor and neurodegenerative disorders
Domenico Tricarico, Nunzio Denora, Antonietta Mele, Angela Curci, Fatima Maqoud, Rosa Scala, Giuliamaria Camerino, Nicola Zizzo, Angela Assunta Lopedota, Annalisa Cutrignelli, Valentino Laquintana, Massimo Franco, Vincenzo Dimiccoli, Anna Tolomeo, Antonio Scilimati
Pages: 1 - 22
Number of pages: 22
Current Topics in Pharmacology
Volume 23 

Copyright © 2019 Research Trends. All rights reserved

The use of [18F]F-DOPA as an imaging agent for positron emission tomography (PET) studies of neurodegeneration and tumor detection is hindered by the chemical instability in its injectate formulation, which is also accompanied by injection-site reactions. Here we investigated novel F-DOPA lactate-based formulations that minimize formulation toxicity without compromising chemical stability. In vivo tolerability study on ND2 (lactate/Na2EDTA/F-DOPA) and ND3 (acetic acid/F-DOPA) formulations in rats (i.v./i.m. 0.025-5 mg/kg) and mice (i.v. 50 mg/kg) was performed. Single-dose extended-toxicity study was performed in rats and mice in order to evaluate the acute and long-lasting response of the animals to the novel formulations. Toxicity related to ionizing radiation was not investigated because the stable isotope [19F]F-DOPA was used instead of [18F]F-DOPA which is the fluorine radioisotope that decays by b+ emission. The i.m. injection of ND3 (5 mg/kg) and ND3-vehicle to rats caused a local reaction characterized by up-regulation of the autophagic Lc3 and Bnip3, apoptotic Caspase 3, 8 and 9, mitochondrial Pgc1α, and inflammatory Mapk3, Cgrp, TNFα  genes. Mapk3 and Pgc1α were also up-regulated in the ND2 (5 mg/kg)-treated muscles. The i.v. injection of ND3 (5 mg/kg) caused a reduction of body weight in rats, after 14 days of follow-up; the ND3 (50 mg/kg) and the ND3-vehicle caused a loss of body weight of -17.8 ± 1% and -12.3 ± 2% vs controls, respectively, in mice. No effects were observed following the administration of ND2 and the ND2-vehicle in rats and mice. The F-DOPA lactate/Na2EDTA-based formulation is better tolerated than the acetic acid-based formulation.
View Full Article  


Buy this article
Buy this volume
Subscribe to this title
Shopping Cart

Quick Links
Search Products
Browse in Alphabetical Order : Journals
Browse by Subject Classification : Journals

Ordering Information Ordering Information
Downloadable forms Downloadable Forms