DPA-714 or ''N'',''N''-diethyl-2- -(2-fluoroethoxy)phenyl5,7-dimethylpyrazolo ,5-''a''yrimidine-3-acetamide is a selective ligand for the translocator protein (TSPO) currently under evaluation for several clinical applications. For this reason, a practical, multigram synthetic route for its preparation has been described. The

binding affinity In biochemistry and pharmacology, a ligand is a substance that forms a complex with a biomolecule to serve a biological purpose. The etymology stems from ''ligare'', which means 'to bind'. In protein-ligand binding, the ligand is usually a mol ...

of DPA-714 for TSPO is reported as ''K''_i = 7.0 ± 0.4 nM. sup>18FPA-714 is currently under investigation as a potential radiopharmaceutical for imaging TSPO in living systems using

positron emission tomography Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in Metabolism, metabolic processes, and in other physiological activities including bl ...

(PET). DPA-714, along with other members of the DPA class of TSPO ligands, has been shown to decrease microglial activation and increase neuronal survival in a quinolinic acid rat model of excitotoxic

neurodegeneration A neurodegenerative disease is caused by the progressive loss of structure or function of neurons, in the process known as neurodegeneration. Such neuronal damage may ultimately involve cell death. Neurodegenerative diseases include amyotrophic ...

, suggesting potential neuroprotective effects.

References

{{Translocator protein modulators Pyrazolopyrimidines TSPO ligands Fluoroethyl ethers

See also

References