DPA-714 (original) (raw)
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.
| Property | Value |
|---|---|
| dbo:abstract | 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. (en) |
| dbo:casNumber | 958233-07-3 |
| dbo:chEMBL | 512306 |
| dbo:fdaUniiCode | Y1H4D2VKZD |
| dbo:thumbnail | wiki-commons:Special:FilePath/DPA-714_Structure.svg?width=300 |
| dbo:wikiPageID | 36064475 (xsd:integer) |
| dbo:wikiPageLength | 4828 (xsd:nonNegativeInteger) |
| dbo:wikiPageRevisionID | 1002398061 (xsd:integer) |
| dbo:wikiPageWikiLink | dbr:Quinolinic_acid dbc:Fluoroethyl_ethers dbr:Binding_affinity dbr:Neurodegeneration dbr:Radiopharmaceutical dbr:DPA-713 dbc:TSPO_ligands dbc:Pyrazolopyrimidines dbr:Positron_emission_tomography dbr:Excitotoxic dbr:Translocator_protein |
| dbp:c | 22 (xsd:integer) |
| dbp:casNumber | 958233 (xsd:integer) |
| dbp:chembl | 512306 (xsd:integer) |
| dbp:chemspiderid | 23328478 (xsd:integer) |
| dbp:f | 1 (xsd:integer) |
| dbp:h | 27 (xsd:integer) |
| dbp:iupacName | N,N-diethyl-2-[4-phenyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-acetamide (en) |
| dbp:n | 4 (xsd:integer) |
| dbp:o | 2 (xsd:integer) |
| dbp:smiles | CCNCCc1cc3cccOCCF (en) |
| dbp:stdinchi | 1 (xsd:integer) |
| dbp:stdinchikey | FLZZFWBNYJNHMY-UHFFFAOYSA-N (en) |
| dbp:unii | Y1H4D2VKZD (en) |
| dbp:wikiPageUsesTemplate | dbt:Drugbox dbt:Reflist dbt:Fdacite |
| dcterms:subject | dbc:Fluoroethyl_ethers dbc:TSPO_ligands dbc:Pyrazolopyrimidines |
| gold:hypernym | dbr:Ligand |
| rdf:type | owl:Thing dul:ChemicalObject dbo:ChemicalSubstance wikidata:Q8386 dbo:Drug |
| rdfs:comment | 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. (en) |
| rdfs:label | DPA-714 (en) |
| owl:sameAs | freebase:DPA-714 yago-res:DPA-714 wikidata:DPA-714 https://global.dbpedia.org/id/4iqwm |
| prov:wasDerivedFrom | wikipedia-en:DPA-714?oldid=1002398061&ns=0 |
| foaf:depiction | wiki-commons:Special:FilePath/DPA-714_Structure.svg |
| foaf:isPrimaryTopicOf | wikipedia-en:DPA-714 |
| is dbo:wikiPageWikiLink of | dbr:DPA-713 dbr:C22H27FN4O2 dbr:Translocator_protein |
| is foaf:primaryTopic of | wikipedia-en:DPA-714 |
