Tracer library / [18F]DPA-714
Structure of DPA-714 (unlabelled parent compound, from PubChem)
Unlabelled parent compoundPubChem CID 24895172

[18F]DPA-714

Also written as [18F]DPA-714; [18F]DPA714; [F-18]DPA-714; [F-18]DPA714; DPA-714
Radionuclide
F-18 t½ 109.77 min
Modality
PET
Production route
—
Stage
Clinical research
Syntheses indexed
6

What it is

Compound class
Radiolabelled pyrazolo[1,5-a]pyrimidine acetamide (second-generation TSPO ligand)
Target / mechanism
18-kDa translocator protein (TSPO), a marker of activated microglia/macrophages in neuroinflammation PMID 19223401
Clinical application
Neuroinflammation / microglial activation imaging in neurological disorders PMID 34037896
Theranostic pair
—

Published syntheses

ModuleCassettePurificationYield %RCP %Precursor / supplierSource
TRACERlab FX FN
GE HealthCare
—HPLC24 ± 3%—tosylate substrate24615467
2014 Eur J Nucl Med Mol Imaging
Automated synthesis of 18F-DPA-714 was carried out using a slightly modified TRACERLab FX-FN module (GE Medical Systems). - The yield was 24 ± 3% with a specific activity of 41–107 GBq/μmol (n = 8).
Synthera
IBA
vendor cassetteHPLC+SPE24.6 ± 3.8%
not corrected
> 99.9%N,N-Diethyl-2-(2-(4-(2-toluenesulfonyloxyeth…N,N-Diethyl-2-(2-(4-(2-toluenesulfonyloxyethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide
ABX
38461627
2024 Appl Radiat Isot
an automated Synthera® radiosynthesizer (Version 1, IBA Molecular) employing an Integrated Fluidic Processor™ (IFP) cassette - EOS activity yield of 24.6 ± 3.8% and a molar activity of > 18.5 TBq/mmol (500 Ci/mmol)
ELIXYS FLEX/CHEM
Sofie
—HPLC+SPE13.5 ± 3.04%
not corrected
—2-(4-(3-(2-(diethylamino)-2-oxoethyl)-5,7-di…2-(4-(3-(2-(diethylamino)-2-oxoethyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-2-yl)phenoxy)ethyl 4-methylbenzenesulfonate
In-house / non-commercial (various)
34871885
2022 Appl Radiat Isot
Elixys Flex/Chem (Sofie Biosciences \u2013 Dulles, VA) - [18F]DPA-714 was synthesized in a 13.5 ± 3.04% activity yield (EOS)
AllinOne (AiO)
Trasis
custom manifoldHPLC+SPE55-71
decay-corrected
100DPA-714 tosylate
PharmaSynth AS, Tartu, Estonia
34037896
2021 EJNMMI Radiopharm Chem
synthesised using an in-house designed cassette and sequence - [18F]DPA-714 was obtained with consistently high radiochemical yields of 55-71% (n=6)
iMiDEV
PMB-Alcen
vendor cassetteHPLC17 ± 6%
decay-corrected
>99%TsO-DPA-714
PharmaSynth AS, Tartu, Estonia
39692929
2024 EJNMMI Radiopharm Chem
the iMiDEV™ radiosynthesiser - RCYa–17 ± 6%10 ± 1%11%
TRACERlab FX FN
GE HealthCare
—————22104496
2012 Appl Radiat Isot
using a TRACERlab FX-FN synthesizer

Precursor

Common precursor
—
Suppliers seen in the literature
—
Cited suppliers in indexed syntheses
ABX, In-house / non-commercial (various), PharmaSynth AS
Typical final purification
—

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Quality control Preliminary - inferred from compound class

Ph. Eur. monograph
not verified No Ph. Eur. check is recorded for this entry.
USP monograph
not verified No USP check is recorded for this entry.
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. Stage set/updated at stage 39 from PMID 34037896: 'boosting reliability, throughput, and introducing a significant degree of simplicity'.
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