DPA-714 or N,N-diethyl-2-[4-(2-fluoroethoxy)phenyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine-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 of DPA-714 for TSPO is reported as Ki = 7.0 ± 0.4 nM.
[18F]DPA-714 is currently under investigation as a potential radiopharmaceutical for imaging TSPO in living systems using positron emission tomography (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, suggesting potential neuroprotective effects.
There's war in the heavens
Rebellion on high
the son of the morning
Descends from a black sky
Severed and broken
His wings burned to dust
His coverings of diamonds and gold
In a moment in time dissolve to rust
Thunder and lightning
Shatter the night
The dragon of darkness
Appears cursed by the keeper of the light
The dark is chosen
The scroll has been sealed
Hidden in verses of prophets
His face is revealed
Songs of glory
Shout across the land
I can take you there
Child of mine, take my hand
Down through the ages
The story's been told
The daughter of wisdom
Beguiled by the serpent of old
Born into sin in a valley of thorns
Torn from enchantment and
Tossed into the eye of the storm
Heaven's garden
Made by God for man
This is paradise
Child of mine, take my hand
Glory to glory
Sin after sin
The rider of death
Pushes on to the place where
The battle must begin
Songs of glory
Shout across the land
This is paradise
Won't you take my hand
Heaven's garden
Made by God for man
This is paradise
Child of mine, take my hand
Oh, take my hand