Tracers / [11C]PBR28

[11C]PBR28

Also written as [11C]PBR28; [C-11]PBR28; C-11 PBR28; N-(2-[11C]methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide; PBR28
Radionuclide
C-11 t½ 20.36 min
Modality
PET
Production route
Stage
Syntheses indexed
3

What it is

Compound class
TSPO radioligand (acetamide-based, N-(2-methoxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide derivative)
Target / mechanism
Binds translocator protein (TSPO, 18 kDa), a marker of microglial activation PMID 26839827
Clinical application
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
HPLC+SPE45-55%
yes
>99%p-phenol precursor 6 (N-(2-Hydroxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide)26839827
2015 Sci Pharm
we optimized the radiolabeling procedure of [11C]PBR28 in GE-FXC, GE-FXMeI/FXM, and TRASIS AIO modules at the Wake Forest PET Center for clinical trials — The radiochemical yield was ~45–55% and the specific activity ranged from 8000–9500 mCi/μmol (n=15, decay corrected to EOS).
In-house / custom builtcustom manifoldHPLC70-80%
yes
>99%desmethyl-PBR28 (4a), N-(2-hydroxybenzyl)-N-(4-phenoxypyridin-3-yl)acetamide19716298
2009 Bioorg Med Chem Lett
The radiosynthesis was performed in an in-house automated multi-purpose 11C-radiosynthesis module, allowing measurement of specific radioactivity during synthesis.19,20 — produce the corresponding pure radiolabeled compound [11C]4b in 70-80% radiochemical yield, decay corrected to end of bombardment (EOB), based on [11C]CO2
HPLC+SPE3.6%>99%desmethyl-PBR2822503515
2012 Appl Radiat Isot
using a GE TRACERlab FX(C-Pro) — Typical radiochemical yield using the optimized method is 3.6% yield (EOS, n=3)

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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)

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); 3 article(s) with C-11.