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PET tracers for the peripheral benzodiazepine receptor and uses thereof

Pernilla J Schweitzer1, Brian A Fallon, J John Mann

  • 1College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA.

Drug Discovery Today
|August 31, 2010
PubMed

Insights

Peripheral benzodiazepine receptor (PBR) imaging shows promise for diagnosing and monitoring brain diseases. Positron emission tomography (PET) radioligands enable in vivo quantification of PBR, aiding therapeutic evaluation.

Area of Science:

  • Neuroscience
  • Radiochemistry
  • Molecular Imaging

Background:

  • Peripheral benzodiazepine receptor (PBR) is found on activated microglia mitochondria.
  • PBR is involved in central nervous system and peripheral disease pathophysiology.
  • High PBR concentration suggests potential as a biomarker.

Purpose of the Study:

  • Review positron emission tomography (PET) radioligands for PBR imaging.
  • Discuss applications of PBR imaging in living brain.
  • Highlight PBR as a therapeutic target for neuroinflammatory and neuropsychiatric disorders.

Main Methods:

  • Literature review of PET radioligands for PBR.
  • Analysis of PBR imaging applications in preclinical and clinical studies.
  • Discussion of PBR's role in disease and treatment.

Main Results:

  • Several PET radioligands have been developed for PBR imaging.
  • PBR imaging allows in vivo quantification and monitoring of disease.
  • PBR is a viable target for drug development and therapeutic assessment.

Conclusions:

  • PET imaging of PBR offers a valuable tool for neuroscience research.
  • PBR imaging aids in disease diagnosis, progression monitoring, and therapy evaluation.
  • Targeting PBR presents a promising strategy for treating neuroinflammatory and neuropsychiatric conditions.

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