Biological evaluation of 2'-[18F]fluoroflumazenil ([ 18F]FFMZ), a potential GABA receptor ligand for PET
- Author(s)
- Markus Mitterhauser, Leila Wabnegger, Leonhard-Key Mien, Stefan Tögel, Oliver Langer, Werner Sieghart, Helmut Viernstein, Kurt Kletter, Robert Dudczak
- Abstract
[11C]Flumazenil, a highly selective benzodiazepine antagonist is the most extensively used GABAA ligand for PET so far. To overcome half life disadvantages of 11C a [18F]-labeled flumazenil derivative, 2'-[18F]fluoroflumazenil (FFMZ) was developed and biologically evaluated with respect to the GABAA receptor. Organ with the highest uptake was the pituitary gland. Brain uptake was high and followed the order cortex>thalamus>cerebellum>rest brain. Fluoroflumazenil displaced [3H]flumazenil binding from membrane GABAA receptors with an IC50value (3.5 nM) comparable to that of Flumazenil (2.8 nM). The presented data confirm the potential of [ 18F]FFMZ for PET imaging of the GABA-ergic system. Π2004 Elsevier Inc. All rights reserved.
- Organisation(s)
- Department of Inorganic Chemistry, Department of Sport and Human Movement Science
- External organisation(s)
- Medizinische Universität Wien, University of Vienna
- Journal
- Nuclear Medicine and Biology
- Volume
- 31
- Pages
- 291-295
- No. of pages
- 5
- ISSN
- 0969-8051
- Publication date
- 2004
- Peer reviewed
- Yes
- Austrian Fields of Science 2012
- 3012 Pharmacy, Pharmacology, Toxicology
- Portal url
- https://ucrisportal.univie.ac.at/en/publications/c12f9c5e-11ba-41bb-ac6e-6c478d9a3b3e