Synthesis of fluorine-18-labeled ciprofloxacin for PET studies in humans
- Author(s)
- Oliver Langer, Markus Mitterhauser, Wolfgang Wadsak, Bernhard X Mayer, Kurt Kletter, Markus Müller
- Abstract
Ciprofloxacin (1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)- quinoline-3-carboxylic acid), a widely-prescribed antibiotic, was labeled with fluorine-18 with the aim to perform positron emission tomography studies in humans for pharmacokinetic measurements. Due to a lack of chemical activation of ciprofloxacin for a direct nucleophilic exchange reaction a novel two-step synthetic approach, which employed an activated 6-fluoro-7-chloro substituted precursor molecule, was developed. The radiosynthesis yielded, starting from 52.5 ‘ 11.3 GBq of [18F]fluoride, 1.3 ‘ 0.6 GBq (n = 13) [18F]ciprofloxacin ready for intravenous administration in about 130 min synthesis time. A series of analytical tests was performed in order to prove the identity of the radiolabeled compound and its suitability for human applications. Œ 2003 Elsevier Science Inc. All rights reserved.
- Organisation(s)
- Department of Inorganic Chemistry
- External organisation(s)
- Austrian Research Centers GmbH (ARC Seibersdorf), Medizinische Universität Wien
- Journal
- Nuclear Medicine and Biology
- Volume
- 30
- Pages
- 285-291
- No. of pages
- 7
- ISSN
- 0969-8051
- Publication date
- 2003
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 3012 Pharmacy, Pharmacology, Toxicology
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/55cb8e20-bd13-4b3e-9f3c-1b051f0c0768