Page last updated: 2024-11-10

panadiplon

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

Description

panadiplon: structure given in first source; RN from Toxlit [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3033821
CHEMBL ID279867
SCHEMBL ID123304
MeSH IDM0189526

Synonyms (34)

Synonym
bdbm50048837
3-(5-cyclopropyl-[1,2,4]oxadiazol-3-yl)-5-isopropyl-5h-imidazo[1,5-a]quinoxalin-4-one
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-isopropylimidazo(1,5-a)quinoxalin-4(5h)-one
imidazo(1,5-a)quinoxalin-4(5h)-one, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)-
panadiplon [usan:inn]
fg 10571
panadiplonum [inn-latin]
panadiplone [inn-french]
u-78875
panadiplon
fg-10571
124423-84-3
panadiplon (usan/inn)
D05346
CHEMBL279867 ,
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-propan-2-ylimidazo[1,5-a]quinoxalin-4-one
panadiplone
unii-v4pw0s7zp7
panadiplonum
v4pw0s7zp7 ,
AKOS015904452
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)-imidazo(1,5-a)quinoxalin-4(5h)-one
panadiplon [inn]
panadiplon [usan]
SCHEMBL123304
J-523865
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(propan-2-yl)imidazo[1,5-a]quinoxalin-4(5h)-one
DTXSID40869698
panadiplon (u-78875)
3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-isopropylimidazo[1,5-a]quinoxalin-4(5h)-one
Q7129767
imidazo[1,5-a]quinoxalin-4(5h)-one, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-5-(1-methylethyl)-
HY-106851
CS-0026726

Research Excerpts

Treatment

ExcerptReferenceRelevance
"Panadiplon pretreatment resulted in leftward shifts in the pentobarbital dose-response function but predominantly rightward shifts of the triazolam dose-response function."( Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys.
Rowlett, JK; Woolverton, WL, 2001
)
1.31

Toxicity

ExcerptReferenceRelevance
" Investigational toxicology methods, using appropriate models and hypotheses, can often resolve problems, identify toxic chemical substituents and salvage therapeutic discovery programs."( Cultured hepatocytes as investigational models for hepatic toxicity: practical applications in drug discovery and development.
Bacon, JA; Cramer, CT; Peng, GW; Petrella, DK; Stryd, RP; Sun, EL; Ulrich, RG, 1995
)
0.29
" Idiosyncratic toxic responses are often not detected during this phase in development due to their relative rarity in incidence and differences in species sensitivity."( Metabolic, idiosyncratic toxicity of drugs: overview of the hepatic toxicity induced by the anxiolytic, panadiplon.
Bacon, JA; Brass, EP; Cramer, CT; Petrella, DK; Sun, EL; Ulrich, RG, 2001
)
0.53

Bioavailability

ExcerptReferenceRelevance
" Pharmacokinetic analysis of several compounds indicated excellent oral bioavailability and a reasonable half-life in rats."( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999
)
0.3

Dosage Studied

ExcerptRelevanceReference
" Uniquely, a number of these analogues were found to have a bell-shaped dose-response profile in the alpha1 beta2 gamma2 subtype as determined by whole cell patch-clamp technique, where in vitro efficacy was found to decrease with increasing drug concentration."( Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
Belonga, KL; Carter, DB; Im, HK; Im, WB; Jacobsen, EJ; Mickelson, JW; Petke, JD; Sethy, VH; Stelzer, LS; Tang, AH; TenBrink, RE; VonVoigtlander, PF; Zhong, WZ, 1999
)
0.3
" Panadiplon pretreatment resulted in leftward shifts in the pentobarbital dose-response function but predominantly rightward shifts of the triazolam dose-response function."( Discriminative stimulus effects of panadiplon (U-78875), a partial agonist at the benzodiazepine site, in pentobarbital-trained rhesus monkeys.
Rowlett, JK; Woolverton, WL, 2001
)
1.5
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (23)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)Ki0.00350.00000.21085.6234AID72906
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)Ki0.20410.00000.18819.0000AID72906; AID73226; AID73539
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Ki0.10180.00020.561410.0000AID39930; AID39931; AID40672; AID72136; AID73072
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.00160.00010.739610.0000AID40672
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Ki0.00160.00020.635210.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki0.00160.00020.621710.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Ki0.00160.00020.675810.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Ki0.00160.00020.646910.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Ki0.10180.00020.671210.0000AID39930; AID39931; AID40672; AID72136; AID73072
Gamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)Ki0.00570.00010.25155.6234AID73226
Gamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)Ki0.20410.00000.28325.6234AID72906; AID73226; AID73539
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Ki0.00160.00020.557710.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Ki0.00160.00020.640310.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.10180.00020.570810.0000AID39930; AID39931; AID40672; AID72136; AID73072
Gamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)Ki0.60300.00020.41199.0000AID73539
Beta-2 adrenergic receptor Bos taurus (cattle)Ki0.00160.00160.09040.1400AID40672
GABA theta subunitRattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Ki0.00160.00020.656110.0000AID39930; AID39931; AID40672; AID72136
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
post-embryonic developmentGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
adult behaviorGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inner ear receptor cell developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
innervationGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cellular response to histamineGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cochlea developmentGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
regulation of membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
signal transductionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
gamma-aminobutyric acid signaling pathwayGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synaptic transmission, GABAergicGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride transmembrane transportGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
inhibitory synapse assemblyGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
receptor-mediated endocytosisBeta-2 adrenergic receptor Bos taurus (cattle)
regulation of smooth muscle contractionBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of MAPK cascadeBeta-2 adrenergic receptor Bos taurus (cattle)
negative regulation of G protein-coupled receptor signaling pathwayBeta-2 adrenergic receptor Bos taurus (cattle)
adenylate cyclase-activating adrenergic receptor signaling pathwayBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of autophagosome maturationBeta-2 adrenergic receptor Bos taurus (cattle)
positive regulation of lipophagyBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (11)

Processvia Protein(s)Taxonomy
GABA receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
protein bindingGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neurotransmitter receptor activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
benzodiazepine receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-gated chloride ion channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel activityGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
beta2-adrenergic receptor activityBeta-2 adrenergic receptor Bos taurus (cattle)
protein homodimerization activityBeta-2 adrenergic receptor Bos taurus (cattle)
norepinephrine bindingBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
GABA receptor complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-1Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
axonGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit gamma-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-3Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
cytoplasmic vesicle membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
extracellular exosomeGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-ergic synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit beta-2Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
cerebellar Golgi cell to granule cell synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynaptic specialization membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
GABA-A receptor complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
chloride channel complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
postsynapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
dendrite membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
transmembrane transporter complexGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
plasma membraneGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
synapseGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
neuron projectionGamma-aminobutyric acid receptor subunit alpha-6Homo sapiens (human)
early endosomeBeta-2 adrenergic receptor Bos taurus (cattle)
Golgi apparatusBeta-2 adrenergic receptor Bos taurus (cattle)
receptor complexBeta-2 adrenergic receptor Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID173445Antagonism of metrazole-induced clonic convulsions in rats after ip injection1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
AID223126Compound was tested for ethanol potentiation expressed as loss of righting reflex (anesthesia)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID35392In vitro efficacy calculated by chlorine current assay on alpha-1-beta-2-gamma-2 (GABA-A) receptor subtype1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID124224In vivo efficacy is evaluated by percent control of cerebellar GMP levels in (drug+stress) treated mice/mice under stress1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID39931Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
AID73539Displacement of [3H]-Ro-15-4513 from GABA-A receptor alpha-6-beta-2-gamma-2 subunits expressed in Sf9 cells1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID196345Inhibition of [35S]TBPS binding to GABA-A Benzodiazepine receptor of rat brain membranes1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID112327Ethanol potentiation was measured against LORR1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID196364In vitro [36Cl]-uptake in rat cerebrocortical synaptoneurosomes1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID72906Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID72136Inhibition of [3H]flunitrazepam binding to GABA-A receptor of rat cortical membranes1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID177961Antagonistic activity against metrazole-induced clonic convulsions in rat after ip injection1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID112191In vivo antagonistic activity against benzodiazepine in mice1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID73226Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID112326Ethanol potentiation activity was measured as loss of traction response in male CF-1 mice after oral administration1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID222344Compound was tested for Acute electroshock physical dependence activity (drug MA50/V122 MA50); No significant activity1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID44593In vitro GABA-mediated chloride current in A293 cells expressing GABA-A benzodiazepine receptor alpha-1-beta-2-gamma-2 subunits at 5 uM1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID72305In vitro inhibition of [35S]TBPS binding in rat brain membranes, activity expressed as [35S]TBPS shift value1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID123132In vivo acute electroshock physical dependence activity in mice; Not active.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID223125Antagonism of benzodiazepine traction in mice1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID72779In vitro efficacy for GABA-A alpha-1-beta-2-gamma-2 subtype expressed in A293 cells in Cl- current assay1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
AID73072Displacement of [3H]-Ro- 15-4513 from alpha-6 beta2 gamma2 subunits of Rat GABA-A receptor expressed in Sf-9 insect cell membranes1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
AID39930Binding affinity against benzodiazepine receptor (BzR) in rat cortical membranes determined by competition experiments with radiolabeled [3H]flunitrazepam (Fnz)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID114819Ability to antagonize the muscle relaxation effect in mice caused by a benzodiazepine full agonist, triazolam.1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID221056Ability to antagonize metrazole-induced seizures (clonic and tonic) in mice after intraperitoneal injection1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID40672Displacement of [3H]flunitrazepam from GABA-A benzodiazepine receptor of rat cortical membranes1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
AID223127Compound was tested for ethanol potentiation expressed as the loss of traction response (muscle relaxation)1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID72594In vitro efficacy by [35S]t-butyl-bicyclophosphorothionate (TBPS) binding to the picrotoxin convulsant site on the GABA-A receptor chloride complex.1996Journal of medicinal chemistry, Sep-13, Volume: 39, Issue:19
3-Phenyl-substituted imidazo[1,5-alpha]quinoxalin-4-ones and imidazo[1,5-alpha]quinoxaline ureas that have high affinity at the GABAA/benzodiazepine receptor complex.
AID108875Acute electroshock physical dependence activity was evaluated; IA=Inactive1996Journal of medicinal chemistry, Jan-05, Volume: 39, Issue:1
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
AID72593Binding to GABA-A receptor complex relative to TBPS binding to picrotoxin convulsant site1996Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23
High-affinity alpha-aminobutyric acid A/benzodiazepine ligands: synthesis and structure-activity relationship studies of a new series of tetracyclic imidazoquinoxalines.
AID177313In vivo efficacy evaluated for ability to antagonize metrazole induced clonic convulsions in rat after ip injection1999Journal of medicinal chemistry, Apr-08, Volume: 42, Issue:7
Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (20)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's18 (90.00)18.2507
2000's2 (10.00)29.6817
2010's0 (0.00)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: 11.12

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index11.12 (24.57)
Research Supply Index3.04 (2.92)
Research Growth Index4.16 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (10.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other18 (90.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]