Tracers / [18F]FPEB

[18F]FPEB

Also written as [18F]FPEB; [F-18]FPEB; F-18 FPEB; F-18-FPEB; FPEB
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
Stage
Syntheses indexed
8

What it is

Compound class
3-fluoro-5-(pyridinylethynyl)benzonitrile derivative (mGluR5 PET ligand)
Target / mechanism
Metabotropic glutamate receptor 5 (mGluR5) ligand PMID 32098347
Clinical application
PET imaging of mGluR5 in the central nervous system, including in Alzheimer's disease research PMID 32098347
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
Manual synthesis3
yes
chloro-precursor (1)32098347
2020 Molecules
a maximum 3% RCC was observed by manual synthesis at 200 ℃ from a 10 min reaction. In light of the low radiofluorination conversion, this precursor was not considered for automated radiosynthesis — a maximum 3% RCC was observed by manual synthesis at 200 ℃ from a 10 min reaction
TRACERlab FX2 N
GE HealthCare
HPLC+SPE4
yes
nitro-precursor (2)
ABX
32098347
2020 Molecules
For automated radiosyntheses, a GE TRACERlab™ FX2 N module with 2 and the SPI5 auxiliary SCIDY precursor (5) were performed as previously reported — upon automation and isolation, the highest RCY was only 4% (Table 2, Entry II)
TRACERlab FX2 N
GE HealthCare
HPLC+SPE25 ± 2
yes
SCIDY SPI5 precursor (5)32098347
2020 Molecules
[18F]FPEB synthesis via the SCIDY SPI5 auxiliary precursor was conducted on a GE TRACERlab™ FX2 N automated synthesis module. — resulted in a RCY of 25% ± 2%, with a molar activity (Am) of = 37 ± 13 GBq/µmol (n = 3)
TRACERlab FX2 N
GE HealthCare
HPLC+SPE24
yes
SCIDY SPIAd precursor (7)32098347
2020 Molecules
These automated reaction conditions were then applied to a novel SCIDY precursor for [18F]FPEB radiosynthesis, bearing an adamantyl-based auxiliary (SPIAd). — The SPIAd precursor (compound 7) also resulted in a 24% RCY for [18F]FPEB, and is similar to that of the SPI5 precursor (Table 2, Entry IV).
TRACERlab FX2 N
GE HealthCare
HPLC+SPE36 ± 6
yes
sulfonium salt precursor (6)32098347
2020 Molecules
we adapted the radiochemistry precursor and methodology for automated radiofluorination with the GE TRACERlab™ FX2 N synthesis module. — the sulfonium salt precursor produced [18F]FPEB with a RCY of 36% ± 6% and Am = 77 ± 35 GBq/µmol (n = 3).
TRACERlab FX FN
GE HealthCare
custom manifoldHPLC+SPE2.6%>98%3-nitro-5-[(pyridine-2-yl)ethynyl]benzonitrile
In-house / non-commercial (various)
25305528
2014 Appl Radiat Isot
Synthesis of [18F]FPEB was carried out with a TRACERLab™ FXF-N module from GE Healthcare (Milwaukee, WI). — we have produced over 100 batches of [18F]FPEB with an average radiochemical yield of 2.6% and a highest yield of 9.2%
TRACERlab FX FN
GE HealthCare
SPE15-25%
no
≥99%spirocyclic iodonium(III) ylide precursor 125655630
2015 J Nucl Med
GE medical systems commercial TRACERlab™ FXFN radiosynthesis module — 18F-FPEB was synthesized in 15 – 25% (n = 3) uncorrected radiochemical yields relative to 18F-fluoride
aryl-chloro precursor38369901
2024 J Labelled Comp Radiopharm

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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); 4 article(s) with F-18.