Drug intelligence / Profile preview

[18F]flumazenil

Development stage
Unknown
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

[18F]flumazenil is a radiolabeled analog of flumazenil used as a positron emission tomography (PET) imaging agent. It specifically binds to the benzodiazepine site of the gamma-aminobutyric acid type A (GABA_A) receptor in the brain. The compound is labeled with fluorine-18 (^18F), which provides a longer half-life than carbon-11-labeled flumazenil and allows for broader clinical use. Its primary application is in neuroimaging to assess GABA_A receptor distribution and density, particularly for localizing epileptogenic zones in drug-resistant temporal lobe epilepsy and evaluating cortical damage in conditions such as stroke, alcoholism, and Alzheimer’s disease[2][3][4][6][9]. Unlike therapeutic flumazenil (used as an antidote for benzodiazepine overdose), [18F]flumazenil serves exclusively as a diagnostic radiopharmaceutical.

Other names
18F-flumazenilfluorine-18 flumazenilfluorine18 flumazenilfluorine 18 flumazenilFMZ PET tracer
02

Targets

BZD site (GABA-A receptor benzodiazepine site)

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