| Literature DB >> 15013496 |
Markus Mitterhauser1, Wolfgang Wadsak, Leila Wabnegger, Leonhard-Key Mien, Stefan Tögel, Oliver Langer, Werner Sieghart, Helmut Viernstein, Kurt Kletter, Robert Dudczak.
Abstract
[(11)C]Flumazenil, a highly selective benzodiazepine antagonist is the most extensively used GABA(A) ligand for PET so far. To overcome half life disadvantages of (11)C a [(18)F]-labeled flumazenil derivative, 2'-[(18)F]fluoroflumazenil (FFMZ) was developed and biologically evaluated with respect to the GABA(A) 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 [(3)H]flumazenil binding from membrane GABA(A) receptors with an IC(50)value (3.5 nM) comparable to that of Flumazenil (2.8 nM). The presented data confirm the potential of [(18)F]FFMZ for PET imaging of the GABA-ergic system.Entities:
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Year: 2004 PMID： 15013496 DOI： 10.1016/j.nucmedbio.2003.09.003
Source DB: PubMed Journal: Nucl Med Biol ISSN： 0969-8051 Impact factor: 2.408