Compounds > dpa 714
Page last updated: 2024-11-13

dpa 714

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID24895172
CHEMBL ID512306
SCHEMBL ID2513934
MeSH IDM0523097

Synonyms (25)

Synonym
bdbm50243007
2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)-n,n-diethylacetamide
n,n-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide
CHEMBL512306 ,
[18f]d
SCHEMBL2513934
958233-07-3
pyrazolo(1,5-a)pyrimidine-3-acetamide, n,n-diethyl-2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethyl-
n,n-diethyl-2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidine-3-acetamide
Y1H4D2VKZD ,
2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo(1,5-a)pyrimidin-3-yl)-n,n-diethylacetamide
dpa-714 ,
J2.865.885K ,
unii-y1h4d2vkzd
FLZZFWBNYJNHMY-UHFFFAOYSA-N
n,n-diethyl-2-{2-[4-(2-fluoro-ethoxy)-phenyl]-5,7-dimethyl-pyrazolo[1,5-a]pyrimidin-3-yl}-acetamide
EX-A3761
HY-122607
n,n-diethyl-2-[2-[4-(2-fluoroethoxy)phenyl]-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl]acetamide
CS-0087451
MS-26740
pyrazolo[1,5-a]pyrimidine-3-acetamide, n,n-diethyl-2-[4-(2-fluoroethoxy)phenyl]-5,7-dimethyl-
DTXSID801121798
dpa 714
AKOS040741666
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Translocator proteinRattus norvegicus (Norway rat)Ki0.00840.00010.65108.9300AID368146; AID733339
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1215788Drug metabolism in human liver microsomes assessed as N-ethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1076467Displacement of [3H]PK11195 from TSPO in rat heart membrane homogenates2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Preparation and evaluation of novel pyrazolo[1,5-a]pyrimidine acetamides, closely related to DPA-714, as potent ligands for imaging the TSPO 18kDa with PET.
AID1337783Intrinsic clearance in Sprague-Dawley rat hepatic microsomes assessed per mg protein up to 30 mins in presence of NADPH by UPLC-MS method
AID1337780Displacement of [3H]flunitrazepam from CBR in rat cerebral cortex membranes at 1 uM relative to control
AID344346Displacement of [3H]PK11195 from peripheral benzodiazepine receptor in rat kidney membrane2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
AID516405Displacement of [3H]PK11195 from TSPO in rat kidney2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
AID1337782Intrinsic clearance in human hepatic microsomes assessed per mg protein up to 30 mins in presence of NADPH by UPLC-MS method
AID1337781n-Octanol-buffer partition coefficient, log D of the compound at pH 7.4 by HPLC method
AID1215838Drug metabolism in baboon liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-7-(hydroxymethyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID733339Displacement of [3H]-PK 11195 from TSPO in rat C6 cell lysates after 2 hrs by scintillation counting analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging.
AID1337779Displacement of [3H]PK11195 from TSPO in rat heart membranes after 15 mins by scintillation counting method
AID1215795Induction of human CYP3A4-mediated drug metabolism expressed in baculovirus-infected insect cell microsomes assessed as N,N-diethyl-2-(2-(4-hydroxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide formation at 50 uM after 30 mins by LC-UV/MS ana2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215789Drug metabolism in human liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-7-(hydroxymethyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215793Induction of human CYP3A4-mediated drug metabolism expressed in baculovirus-infected insect cell microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-7-(hydroxymethyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide formation at 50 uM after 2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID344348Displacement of [3H]flumazenil from central benzodiazepine receptor in rat brain cortex membrane2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
AID1215831Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-6-hydroxy-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID344347Displacement of [3H]Ro 5-4864 from peripheral benzodiazepine receptor in rat kidney membrane2008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
AID1215834Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N,N-diethyl-2-(2-(4-hydroxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215787Drug metabolism in baboon liver microsomes assessed as N,N-diethyl-2-(2-(4-hydroxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215833Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-7-(hydroxymethyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215830Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5-(hydroxymethyl)-7-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID516406Displacement of [3H]Ro151788 from CBR in rat kidney2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
AID1076468Octanol-buffer partition coefficient, log D of the compound at pH 7.4 by HPLC method2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Preparation and evaluation of novel pyrazolo[1,5-a]pyrimidine acetamides, closely related to DPA-714, as potent ligands for imaging the TSPO 18kDa with PET.
AID344345Lipophilicity, log p at pH 7.52008Journal of medicinal chemistry, Jul-10, Volume: 51, Issue:13
Synthesis and biological evaluation of substituted [18F]imidazo[1,2-a]pyridines and [18F]pyrazolo[1,5-a]pyrimidines for the study of the peripheral benzodiazepine receptor using positron emission tomography.
AID1215832Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N-ethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID368146Displacement of [3H]PK11195 from TSPO in rat cortex2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID1215836Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N-ethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5-(hydroxymethyl)-7-methylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215796Induction of human CYP2D6-mediated drug metabolism expressed in baculovirus-infected insect cell microsomes assessed as N,N-diethyl-2-(2-(4-hydroxyphenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide formation at 50 uM after 30 mins by LC-UV/MS ana2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1215794Induction of human CYP3A4-mediated drug metabolism expressed in baculovirus-infected insect cell microsomes assessed as N-ethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide formation at 50 uM after 30 mins by LC-UV/M2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
AID1076466Displacement of [3H]flunitrazepam from CBR in rat cerebral cortex membrane homogenates2014Bioorganic & medicinal chemistry letters, Mar-15, Volume: 24, Issue:6
Preparation and evaluation of novel pyrazolo[1,5-a]pyrimidine acetamides, closely related to DPA-714, as potent ligands for imaging the TSPO 18kDa with PET.
AID368144Displacement of [3H]PK11195 from TSPO in rat kidney membrane2009Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3
The translocator protein (18 kDa): central nervous system disease and drug design.
AID1337784Intrinsic clearance in CD1 mouse hepatic microsomes assessed per mg protein up to 30 mins in presence of NADPH by UPLC-MS method
AID733338Lipophilicity, log P of the compound at pH 7.5 by reversed phase HPLC analysis2013Journal of medicinal chemistry, Apr-25, Volume: 56, Issue:8
Synthesis and structure-activity relationships of 5,6,7-substituted pyrazolopyrimidines: discovery of a novel TSPO PET ligand for cancer imaging.
AID1215835Drug metabolism in Sprague-Dawley rat liver microsomes assessed as N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-bis(hydroxymethyl)pyrazolo[1,5-a]pyrimidin-3-yl)acetamide level after 15 to 60 mins by LC-MS/MS analysis2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (28.57)29.6817
2010's5 (71.43)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.05

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.05 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index39.53 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (14.29%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
pk 11195
PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine		3.5520aromatic amide;
isoquinolines;
monocarboxylic acid amide;
monochlorobenzenes		antineoplastic agent
ro 5-4864
4'-chlorodiazepam: selectively binds peripheral benzodiazepine receptor		3.1410
diazepam
Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity.. diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5.		3.14101,4-benzodiazepinone;
organochlorine compound		anticonvulsant;
anxiolytic drug;
environmental contaminant;
sedative;
xenobiotic
n,n-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide
N,N-di-n-hexyl-2-(4-fluorophenyl)indole-3-acetamide: binds with high affinity to glial mitochondrial diazepam binding inhibitor receptors & increases mitochondrial steroidogenesis		3.1410phenylindole
(r)-(11c)1-(2-chlorophenyl)-n-methyl-n-(1-methylpropyl)-3-isoquinolinecarboxamide
[no description available]		2.110
ssr180575
SSR180575: structure in first source		3.1410
dpa-713
[no description available]		3.8530
2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-n,n-diethylacetamide
2-(6-chloro-2-(4-(3-fluoropropoxy)phenyl)imidazo(1,2-a)pyridin-3-yl)-N,N-diethylacetamide: PET radioligand for imaging neuroinflammation; structure in first source		2.0410
ConditionIndicatedRelationship StrengthStudiesTrials
Degenerative Diseases, Central Nervous System
[description not available]		02.9610
Central Nervous System Disease
[description not available]		02.9610
Central Nervous System Diseases
Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.		02.9610
Neurodegenerative Diseases
Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.		02.9610