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
| Module | Cassette | Purification | Yield % | RCP % | Precursor / supplier | Source |
|---|---|---|---|---|---|---|
| — | — | HPLC | 7 ± 2% | 96.5 ± 1% | N-(2-chloro-5-thiophenol)-N'-(3-thiomethylphenyl)-N'-methyl guanidine, 8 | 31986223 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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Get in touchQuality control Preliminary — inferred from compound class
- Ph. Eur. monograph
- —
- USP monograph
- —
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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