Tracers / [18F]FMZ

[18F]FMZ

Also written as [18F]Flumazenil; [18F]FMZ; [F-18]Flumazenil; [F-18]FMZ; Flumazenil
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
Stage
Syntheses indexed
9

What it is

Compound class
Radiolabelled imidazobenzodiazepine (flumazenil derivative)
Target / mechanism
Central benzodiazepine site of the GABA-A receptor PMID 23857513
Clinical application
Localisation of the epileptogenic zone in drug-resistant temporal lobe epilepsy (presurgical evaluation) PMID 23857513
Theranostic pair

Regulatory status

FDA
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
Uptake time

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab MX
GE HealthCare
custom manifold4 %
yes
2-nitroflumazenil27090254
2016 EJNMMI Res
A new synthesis sequence was written for the GE TRACERlab MXFDG. — 18F-flumazenil was successfully obtained in 4 % decay corrected yield
iPHASE FlexLab
iPHASE Technologies
HPLC+SPE22.2 ± 2.7%
yes
>98%stannyl precursor 3 (Ethyl 5-methyl-6-oxo-8-(tributylstannyl)-5,6-dihydro-4H-benzo[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate)
In-house / non-commercial (various)
36144667
2022 Molecules
the iPHASE Flexlab radiochemistry module — affording a 22.2 ± 2.7% (n = 5) decay-corrected yield after 80 min
AllinOne (AiO)
Trasis
vendor cassetteHPLC35 ± 5%
no
[18F]flumazenil > 99%FMZ-BPin
In-house / non-commercial (various)
35306596
2022 EJNMMI Radiopharm Chem
The fully automated synthesis was developed on the Trasis AllinOne (AIO) platform using a single-use cassette. — this method yielded [18F]FMZ in 35 ± 5% n.d.c.
AllinOne (AiO)
Trasis
vendor cassetteHPLC43 ± 2%
no
[18F]flumazenil ≥ 98%FMZ-BPin
In-house / non-commercial (various)
35306596
2022 EJNMMI Radiopharm Chem
The fully automated synthesis was developed on the Trasis AllinOne (AIO) platform using a single-use cassette. — Starting with 300–340 MBq (n = 5, Trasis) of [18F]fluoride this method yielded [18F]FMZ in 43 ± 2% n.d.c.
TRACERlab FX FN
GE HealthCare
HPLC+SPE15-20
yes
>95%nitroflumazenil36986516
2023 Pharmaceuticals (Basel)
All synthesis and purification procedures were performed on a Tracerlab FX-FN automated synthesizer — with a radiochemical yield (RCY) of 15–20% decay, corrected at the end of bombardment (EOB)
20% for [18F]flumazenil22001413
2012 Appl Radiat Isot
The substitutions were carried out in a microfluidic reaction flow cell — 20% for [(18)F]flumazenil
SPE6.4 ± 0.7%
no
>97%29413823
2018 Appl Radiat Isot
All procedures were performed with TRACERlab FX N Pro synthesizer in 53 min. — FMZ was routinely synthesized in 6.4 ± 0.7% RCY at EOS (not decay corrected, n = 8)
24480268
2014 Nucl Med Biol
SPE26±4%>99%nitro-flumazenil precursor19423008
2009 Nucl Med Biol
an automated radiosynthesis system integrating a microwave reactor — The radiochemical yield obtained at the end of synthesis was 26+/-4% (EOB)

Precursor

Common precursor
2-nitroflumazenil PMID 27090254 (DOI 10.1186/s13550-016-0168-9)
Suppliers seen in the literature
Cited suppliers in indexed syntheses
In-house / non-commercial (various)
Typical final purification

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Quality control Preliminary — inferred from compound class

Ph. Eur. monograph
USP monograph
AppearancepHRCP HPLCRCP TLCHPLC UVRadionuclidic (HPGe)Half-lifeActivityEndotoxins (LAL)SterilityFilter integrity
How this set was arrived at. base set per Ph. Eur. general monograph 0125 (rule); organic-phase radiosynthesis assumed from isotope/compound class, no synthesis data confirming it -> GC residual solvents (preliminary); conventional nucleophilic 18F-fluorination assumed from isotope/compound class, no synthesis data confirming K222 use -> Kryptofix test (preliminary)

Tests listed by reference only. Monograph texts are copyrighted and are not reproduced here. How these are derived

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Notes

Added from reverse module search (stage 6); 8 article(s) with F-18.