Tracers / [18F]GE-179

[18F]GE-179

Also written as [18F]GE-179; [18F]GE179; [F-18]GE-179; [F-18]GE179; F-18 GE-179; GE-179; N-(2-chloro-5-(S-2-[18F]fluoroethyl)thiophenyl)-N'-(3-thiomethylphenyl)-N'-methylguanidine
Radionuclide
F-18 t½ 109.7 min
Modality
PET
Production route
Cyclotron liquid target
Stage
Research
Syntheses indexed
2

What it is

Compound class
Guanidine
Target / mechanism
Open / activated NMDA-receptor ion channel (intra-channel PCP binding site) PMID 34558066 / DOI 10.1111/epi.17074; PMID 31986223 / DOI 10.1002/jlcr.3831
Clinical application
Research PET marker of activated/open NMDA receptor ion channels; investigated for identifying epileptogenic brain areas in treatment-resistant focal epilepsy PMID 34558066 / DOI 10.1111/epi.17074
Theranostic pair

Regulatory status

FDA
No Drugs@FDA / openFDA drug registry — no approved application found; search: https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=BasicSearch.process&searchTerm=GE-179
EMA (centralised)
Other approvals
Brand names

Clinical use

Typical injected activity
~187 MBq (range 173-192 MBq) PMID 25991402 / DOI 10.1136/jnnp-2014-309897; PMID 29892810 / DOI 10.1186/s13550-018-0396-2
Uptake time
90-min dynamic scan started at injection; tracer uptake phase ~first 30 min PMID 25991402 / DOI 10.1136/jnnp-2014-309897

Reported in the literature. Not a dosing recommendation.

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
HPLC7 ± 2%96.5 ± 1%N-(2-chloro-5-thiophenol)-N'-(3-thiomethylphenyl)-N'-methyl guanidine, 831986223
2020 J Labelled Comp Radiopharm
We describe the development of a process using the GE FASTlab™ radiosynthesis platform coupled with HPLC purification. — The crude product was purified by semi-preparative HPLC to give the formulated product in an activity yield (AY) of 7 ± 2% (n = 15) with a total synthesis time of 120 minutes.
12 ± 6%
yes
>95%31026789
2019 Appl Radiat Isot

Precursor

Common precursor
Thiol precursor N-(2-chloro-5-thiophenol)-N'-(3-thiomethylphenyl)-N'-methyl guanidine (8); 2-step: [18F]fluorination of ethylene ditosylate then S-alkylation PMID 31986223 / DOI 10.1002/jlcr.3831
Suppliers seen in the literature
Typical final purification
HPLC

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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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