Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H20N2O3 |
Molecular Weight | 348.3951 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(CN(C(C)=O)C2=CC=C(OC3=CC=CC=C3)N=C2)C=CC=C1
InChI
InChIKey=SLJDUPUOYWPBAB-UHFFFAOYSA-N
InChI=1S/C21H20N2O3/c1-16(24)23(15-17-8-6-7-11-20(17)25-2)18-12-13-21(22-14-18)26-19-9-4-3-5-10-19/h3-14H,15H2,1-2H3
PBR28 or PBR-28, a chemical substance that binds to translocator protein TSPO, also known as Peripheral-type benzodiazepine receptor (PBR). TSPO located within the cells such as macrophages reaches high levels of expression in inflammatory conditions and thus can be a biomarker of neuroinflammation. When radioactivity in the form of carbon-11 is tagged to PBR 28 and is administered, its uptake in the inflammatory body regions can be measured using positron emission tomography (PET). PBR28 now is involved in a clinical trial to evaluate the specificity of its binding in the joints of patients with inflammatory joint disease, like rheumatoid and psoriatic arthritis.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P30536 Gene ID: 706.0 Gene Symbol: TSPO Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/18024084 |
0.59 nM [Ki] |
PubMed
Title | Date | PubMed |
---|---|---|
Radiation dosimetry and biodistribution in monkey and man of 11C-PBR28: a PET radioligand to image inflammation. | 2007 Dec |
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Brain and whole-body imaging in nonhuman primates of [11C]PBR28, a promising PET radioligand for peripheral benzodiazepine receptors. | 2008 Feb 1 |
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Increased in vivo glial activation in patients with amyotrophic lateral sclerosis: assessed with [(11)C]-PBR28. | 2015 |
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Assessment of neuroinflammation in a mouse model of obesity and β-amyloidosis using PET. | 2016 Aug 31 |
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Tracking Macrophage Infiltration in a Mouse Model of Pancreatic Cancer with the Positron Emission Tomography Tracer [11C]PBR28. | 2018 Dec |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18006619
Whole-body peripheral benzodiazepine receptor (PBR) images were acquired after intravenous bolus administration of (11)C-PBR28 in 7 healthy humans (651 +/- 111 MBq)
Route of Administration:
Intravenous
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