Drug intelligence / Profile preview

fluornitrazene

Development stage
Preclinical
Lead developer
National Institute on Drug Abuse
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous, Parenteral
01

Overview

Fluornitrazene (FNZ), also known as fluetonitazene or 2-fluoroetonitazene, is a novel synthetic fluorinated etonitazene analog and benzimidazole opioid developed by researchers at the National Institute on Drug Abuse (NIDA). It acts as a highly potent and selective mu-opioid receptor (MOR) agonist. Initially investigated as a potential PET radiotracer (when labeled with fluorine-18 or carbon-11) for in vivo target engagement studies, fluornitrazene rapidly enters the brain and accumulates in MOR-rich areas. It is metabolized in vivo into its active metabolite, N-desethyl-fluornitrazene (DFNZ), which exhibits impaired brain penetrance and a favorable safety profile with reduced respiratory depression and abuse liability.

Other names
2-fluoroetonitazeneF-etonitazenefluetonitazeneFNZ
02

Targets

MOR (Mu opioid receptor)

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