DPA-713
DPA-713 is a radioligand used in positron emission tomography (PET) imaging to study the translocator protein (TSPO), which is associated with neuroinflammation and other neurological disorders. DPA-713 is a member of the second generation of TSPO ligands, which are characterized by their high affinity and selectivity for the TSPO.
Chemical Properties[edit | edit source]
DPA-713, chemically known as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)thiazol-4-yl)acetamide, is a small molecule that binds to the TSPO with high affinity. The presence of the fluoroethoxy group allows for the incorporation of the radioactive isotope fluorine-18 (18F), making it suitable for PET imaging.
Mechanism of Action[edit | edit source]
DPA-713 binds to the TSPO, a protein located on the outer mitochondrial membrane. TSPO is involved in the transport of cholesterol and other molecules into mitochondria, and its expression is upregulated in response to cellular stress and inflammation. By binding to TSPO, DPA-713 allows for the visualization and quantification of TSPO expression in the brain and other tissues using PET imaging.
Applications in Research[edit | edit source]
DPA-713 is used primarily in research settings to study neuroinflammation in various neurological disorders, including Alzheimer's disease, Parkinson's disease, multiple sclerosis, and traumatic brain injury. It is also used to investigate the role of TSPO in psychiatric disorders such as depression and schizophrenia.
Advantages[edit | edit source]
Compared to first-generation TSPO ligands, DPA-713 has several advantages:
- Higher affinity and selectivity for TSPO
- Improved signal-to-noise ratio in PET imaging
- Reduced non-specific binding
Limitations[edit | edit source]
Despite its advantages, DPA-713 has some limitations:
- Variability in TSPO expression among individuals, which can affect the interpretation of PET imaging results
- Potential for off-target effects, although these are minimized compared to first-generation ligands
Related Pages[edit | edit source]
- Positron emission tomography
- Translocator protein
- Neuroinflammation
- Alzheimer's disease
- Parkinson's disease
- Multiple sclerosis
- Traumatic brain injury
- Depression
- Schizophrenia
See Also[edit | edit source]
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