Journal
NUCLEAR MEDICINE AND BIOLOGY
Volume 31, Issue 2, Pages 291-295Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.nucmedbio.2003.09.003
Keywords
FFMZ; flumazenil; fluoroflumazenil; GABA; PET
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[C-11]Flumazenil, a highly selective benzodiazepine, antagonist is the most extensively used GABA(A) ligand for PET so far. To overcome half life disadvantages of C-11 a [F-18]-labeled flumazenil derivative, 2'-[F-18]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 [H-3]flumazenil binding from membrane GABA(A) receptors with an IC50 value (3.5 nM) comparable to that of Flumazenil (2.8 nM). The presented data confirm the potential of [F-18]FFMZ for PET imaging of the GABA-ergic system. (C) 2004 Elsevier Inc. All rights reserved.
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