DPA-714

DPA-714

DPA-714 is a fluorine-18 radiolabeled compound that is used in Positron Emission Tomography (PET) imaging. It is a derivative of the PK11195 compound and is used to visualize and quantify the 18 kDa translocator protein (TSPO) in the brain. TSPO is a mitochondrial protein that is upregulated in the brain during neuroinflammation, making DPA-714 a valuable tool in the study of neuroinflammatory diseases such as Alzheimer's disease, Parkinson's disease, and multiple sclerosis.

Chemistry

DPA-714 is a pyrazolopyrimidine derivative, similar to its predecessor PK11195, but with a higher affinity for TSPO. The compound is radiolabeled with fluorine-18, a positron-emitting isotope, which allows it to be detected by PET imaging.

Use in PET Imaging

In PET imaging, DPA-714 is injected into the patient's bloodstream, where it crosses the blood-brain barrier and binds to TSPO in the brain. The fluorine-18 in the compound emits positrons, which are detected by the PET scanner to create a three-dimensional image of the brain. The amount of DPA-714 binding correlates with the level of TSPO expression, providing a measure of neuroinflammation in the brain.

Clinical Applications

DPA-714 has been used in research studies to investigate the role of neuroinflammation in various neurological diseases. Studies have shown increased DPA-714 binding in the brains of patients with Alzheimer's disease, Parkinson's disease, and multiple sclerosis, suggesting that these diseases are associated with an upregulation of TSPO and increased neuroinflammation.

Safety and Side Effects

As a radiolabeled compound, DPA-714 exposes patients to a small amount of radiation. However, the risk is considered minimal and is outweighed by the benefits of the information gained from the PET scan. Side effects are rare and typically mild, including possible allergic reactions to the compound.