DPA-713

DPA-713

DPA-713 is a radiopharmaceutical compound used in PET imaging. It is a derivative of the isoquinoline family and is primarily used to image glial cells in the brain. DPA-713 binds to the translocator protein (TSPO), which is upregulated in activated glial cells. This makes it a valuable tool in the study of neuroinflammation and neurodegenerative diseases.

Chemistry

DPA-713 is a pyrazolo[1,5-a]pyrimidine-acetamide derivative. It is structurally similar to other TSPO ligands such as PK11195 and PBR28, but has been shown to have a higher binding affinity and better pharmacokinetic properties. The chemical structure of DPA-713 allows it to cross the blood-brain barrier, making it suitable for imaging the brain.

Applications

DPA-713 is used in PET imaging to visualize and quantify the distribution of TSPO in the brain. This is particularly useful in the study of diseases that involve neuroinflammation, such as Alzheimer's disease, Parkinson's disease, and multiple sclerosis. By imaging the distribution of TSPO, researchers can gain insights into the role of glial cells in these diseases.

In addition to its use in neuroimaging, DPA-713 has also been used in preclinical studies to investigate the role of TSPO in peripheral tissues. For example, it has been used to image inflammation in models of rheumatoid arthritis and cardiovascular disease.

Limitations

While DPA-713 has many advantages over other TSPO ligands, it is not without limitations. One of the main challenges is the variability in TSPO binding affinity among individuals due to a polymorphism in the TSPO gene. This can affect the quantification of TSPO distribution and may require personalized dosing strategies.

See also

• Positron Emission Tomography
• Translocator protein
• Neuroinflammation
• Neurodegenerative diseases

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