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Updated: Jul 25, 2025

PET Imaging of Neuroinflammation Using [11C]DPA-713 in a Mouse Model of Ischemic Stroke
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Imidazoline-I2 PET Tracers in Neuroimaging

Christine A Parker1,2, David J Nutt1, Robin J Tyacke1

  • 1Neuropsychopharmacology Unit, Division of Psychiatry, Imperial College London, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK.

International Journal of Molecular Sciences
|June 28, 2023
PubMed

Insights

New PET tracers targeting astrocytes show potential for early detection of neurodegenerative diseases. Clinical data suggests astrogliosis may precede microglial activation, offering new avenues for early intervention.

Area of Science:

  • Neuroscience
  • Molecular Imaging
  • Pharmacology

Background:

  • Neuroinflammation, specifically microglial activation and astrocytosis, is a key target for treating neurodegenerative disorders.
  • Developing cell-type-specific PET imaging tools is crucial for understanding the roles of microglia and astrocytes in human diseases.

Purpose of the Study:

  • To review recent advances in Imidazoline2 binding site (I2BS) PET tracers for targeting astrocytes.
  • To evaluate the potential of I2BS PET tracers as clinical imaging tools for neurodegenerative diseases.

Main Methods:

  • Review of five I2BS PET tracers.
  • Focus on 11C-BU99008, the only GMP-validated tracer for clinical use.
  • Analysis of clinical data from healthy volunteers and patients with Alzheimer's and Parkinson's disease.

Main Results:

  • 11C-BU99008 has been clinically validated and used in human studies.
  • Clinical data suggests astrogliosis may be involved early in neurodegeneration, potentially preceding microglial activation.

Conclusions:

  • I2BS PET tracers, particularly 11C-BU99008, show promise for imaging astrocytes in neurodegenerative conditions.
  • Early detection of astrogliosis could lead to earlier therapeutic interventions in neurodegenerative diseases.
Keywords:
I2BSPETastrogliosisimidazoline binding sites

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