PET tracers for the peripheral benzodiazepine receptor and uses thereof

The peripheral benzodiazepine receptor (PBR) is expressed on the outer mitochondrial membrane of activated microglia and is implicated in the pathophysiology of a variety of central nervous system and peripheral diseases. The abundant receptor concentration makes PBR a potential biomarker and an att...

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Bibliographic Details
Published in:Drug discovery today 2010-11, Vol.15 (21), p.933-942
Main Authors: Schweitzer, Pernilla J., Fallon, Brian A., Mann, J. John, Kumar, J.S. Dileep
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
General pharmacology
Humans
Medical sciences
Microglia - diagnostic imaging
Microglia - metabolism
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Positron-Emission Tomography
Radioisotopes - pharmacokinetics
Radiopharmaceuticals - pharmacokinetics
Rats
Receptors, GABA-A - metabolism
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Description
Summary:The peripheral benzodiazepine receptor (PBR) is expressed on the outer mitochondrial membrane of activated microglia and is implicated in the pathophysiology of a variety of central nervous system and peripheral diseases. The abundant receptor concentration makes PBR a potential biomarker and an attractive target for quantification in vivo using positron emission tomography. PBR can be an important target for monitoring disease progression, for evaluating the effect of therapy, and for investigating new treatment modalities. PBR is also emerging as a potential target in the treatment of neuroinflammatory and neuropsychiatric disorders. Here, we review the positron emission tomography radioligands employed for imaging PBR in living brain and their applications.
ISSN:1359-6446
1878-5832
DOI:10.1016/j.drudis.2010.08.012