Page last updated: 2024-11-10

2-(2-benzofuranyl)-2-imidazoline

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

Description

2-(2-benzofuranyl)-2-imidazoline: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3080926
CHEMBL ID404505
CHEBI ID103964
SCHEMBL ID563160
MeSH IDM0271122

Synonyms (25)

Synonym
1h-imidazole, 2-(2-benzofuranyl)-4,5-dihydro-
BRD-K22745370-003-01-5
tocris-0348
NCGC00024548-01 ,
2-(2-benzofuranyl)-2-imidazoline
2-benzofuran-2-yl-4,5-dihydro-1h-imidazole
bdbm50086502
2-bfi
CHEMBL404505 ,
2-(1-benzofuran-2-yl)-4,5-dihydro-1h-imidazole
CHEBI:103964
(3h)2-bfi
72583-92-7
SCHEMBL563160
2XCG
DTXSID80222905
2-(2-benzofuranyl)-4,5-dihydro-1h-imidazole
Q27181198
2-(1-benzo[b]furan-2-yl)-4,5-dihydro-1h-imidazole
2-(benzofuran-2-yl)-4,5-dihydro-1h-imidazole
rx 801077
HY-100904A
CS-0652192
PD071277
UY7S3D3AJ3

Research Excerpts

Compound-Compound Interactions

ExcerptReferenceRelevance
" Here we investigated the protective effects of 2-BFI in combination with delayed intravenous rt-PA after stroke induced by embolic middle cerebral artery occlusion (eMCAO) in rats."( Protective effects of 2-(2-benzonfuranyl)-2-imidazoline combined with tissue plasminogen activator after embolic stroke in rats.
Cao, Y; Chen, J; Guo, X; Han, Z; Li, L; Zhang, L; Zhang, Z, 2018
)
0.48

Dosage Studied

ExcerptRelevanceReference
" We observed that 2-BFI significantly ameliorated the learning and memory abilities in rat models with AD by dosage treatment, as demonstrated by the shorten learning latency and greater times of travel across the platform quadrant."( 2-(2-benzofuranyl)-2-imidazoline (2-BFI) improved the impairments in AD rat models by inhibiting oxidative stress, inflammation and apoptosis.
Chen, R; Tian, JS; Zhai, QJ; Zhao, LD; Zhao, Y, 2017
)
1.9
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
benzofurans
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (16)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain B, HADH2 proteinHomo sapiens (human)Potency31.62280.025120.237639.8107AID893
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency22.38720.177814.390939.8107AID2147
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency39.81070.00207.533739.8107AID891
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency39.81070.001815.663839.8107AID894
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Alpha-2A adrenergic receptorHomo sapiens (human)Ki26.60900.00010.807410.0000AID1767747; AID772379
Alpha-2B adrenergic receptorHomo sapiens (human)Ki26.60900.00020.725710.0000AID1767747; AID772378
Alpha-2C adrenergic receptorHomo sapiens (human)Ki26.60900.00030.483410.0000AID1767747; AID772377
Alpha-2B adrenergic receptorRattus norvegicus (Norway rat)Ki4.00000.00000.929610.0000AID37090; AID37100
Amine oxidase [flavin-containing] AHomo sapiens (human)Ki17.00000.00192.379710.0000AID1514573
Alpha-2C adrenergic receptorRattus norvegicus (Norway rat)Ki4.00000.00000.970810.0000AID37090; AID37100
Alpha-2A adrenergic receptorRattus norvegicus (Norway rat)Ki4.00000.00000.937510.0000AID37090; AID37100
Amine oxidase [flavin-containing] BHomo sapiens (human)Ki14.20000.00061.777110.0000AID1352194; AID1514574; AID392235
NischarinHomo sapiens (human)IC50 (µMol)6.40000.09702.99936.4000AID223232
NischarinHomo sapiens (human)Ki0.07000.00420.21923.8019AID223237
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Amine oxidase [flavin-containing] BHomo sapiens (human)Kd0.00900.00900.00900.0090AID977611
Amine oxidase [flavin-containing] BHomo sapiens (human)Kd0.00900.00900.11930.2754AID1514575
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (69)

Processvia Protein(s)Taxonomy
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
biogenic amine metabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
positive regulation of signal transductionAmine oxidase [flavin-containing] AHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] AHomo sapiens (human)
response to xenobiotic stimulusAmine oxidase [flavin-containing] BHomo sapiens (human)
response to toxic substanceAmine oxidase [flavin-containing] BHomo sapiens (human)
response to aluminum ionAmine oxidase [flavin-containing] BHomo sapiens (human)
response to selenium ionAmine oxidase [flavin-containing] BHomo sapiens (human)
negative regulation of serotonin secretionAmine oxidase [flavin-containing] BHomo sapiens (human)
phenylethylamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
substantia nigra developmentAmine oxidase [flavin-containing] BHomo sapiens (human)
response to lipopolysaccharideAmine oxidase [flavin-containing] BHomo sapiens (human)
dopamine catabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to ethanolAmine oxidase [flavin-containing] BHomo sapiens (human)
positive regulation of dopamine metabolic processAmine oxidase [flavin-containing] BHomo sapiens (human)
hydrogen peroxide biosynthetic processAmine oxidase [flavin-containing] BHomo sapiens (human)
response to corticosteroneAmine oxidase [flavin-containing] BHomo sapiens (human)
apoptotic processNischarinHomo sapiens (human)
Rac protein signal transductionNischarinHomo sapiens (human)
actin cytoskeleton organizationNischarinHomo sapiens (human)
negative regulation of cell migrationNischarinHomo sapiens (human)
outer dynein arm assemblyNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] AHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] AHomo sapiens (human)
protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
primary amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
electron transfer activityAmine oxidase [flavin-containing] BHomo sapiens (human)
identical protein bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
aliphatic amine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
monoamine oxidase activityAmine oxidase [flavin-containing] BHomo sapiens (human)
flavin adenine dinucleotide bindingAmine oxidase [flavin-containing] BHomo sapiens (human)
integrin bindingNischarinHomo sapiens (human)
protein bindingNischarinHomo sapiens (human)
phosphatidylinositol bindingNischarinHomo sapiens (human)
identical protein bindingNischarinHomo sapiens (human)
dynein heavy chain bindingNischarinHomo sapiens (human)
alpha-tubulin bindingNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] AHomo sapiens (human)
cytosolAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] AHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial envelopeAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrial outer membraneAmine oxidase [flavin-containing] BHomo sapiens (human)
dendriteAmine oxidase [flavin-containing] BHomo sapiens (human)
neuronal cell bodyAmine oxidase [flavin-containing] BHomo sapiens (human)
mitochondrionAmine oxidase [flavin-containing] BHomo sapiens (human)
nucleoplasmNischarinHomo sapiens (human)
early endosomeNischarinHomo sapiens (human)
cytosolNischarinHomo sapiens (human)
plasma membraneNischarinHomo sapiens (human)
microtubule cytoskeletonNischarinHomo sapiens (human)
membraneNischarinHomo sapiens (human)
intracellular membrane-bounded organelleNischarinHomo sapiens (human)
intercellular bridgeNischarinHomo sapiens (human)
recycling endosomeNischarinHomo sapiens (human)
cytoplasmNischarinHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID223256Binding affinity for rat imidazoline I2 receptor from crude P2 membranes2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Binding of an imidazopyridoindole at imidazoline I2 receptors.
AID392232Binding affinity to MAOB imidazoline binding site in rat brain mitochondrial homogenate assessed as 4-hydroxyquinoline production by spectrophotometry2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
AID772378Binding affinity at human alpha2B AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID223254Displacement of [3H]2-BFI from imidazoline receptor I-22004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
AID223232Inhibition of 3 nM [3H]clonidine binding to rat kidney membrane imidazoline receptor I-1 in presence of rauwolscine2000Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6
Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
AID515608Displacement of [3H]2BFI from I2 imidazoline binding site in rat brain membrane2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
AID1767745Displacement of [3H]2-BFI from imidazoline I2 receptor high affinity site in post-mortem human brain frontal cortex membrane two site model measured after 30 mins by liquid scintillation counting spectrometry2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1561263Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at high affinity site incubated for 45 mins by liquid scintillation spectrometry relative to control2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID392231Binding affinity to MAOA imidazoline binding site in rat brain mitochondrial homogenate assessed as 4-hydroxyquinoline production by spectrophotometry2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
AID1561261Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at high affinity site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID772377Binding affinity at human alpha2C AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID1514573Competitive inhibition of human MAOA using p-trifluoromethyl benzylamine as substrate preincubated with substrate for 5 mins followed by enzyme addition by fluorimetric horseradish peroxidase-Amplex Red-coupled assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework.
AID223259Inhibition of 1 nM [3H]2-BFI binding to rat whole brain membrane imidazoline receptor I-22000Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6
Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
AID1561262Displacement of [3H]2-BFI from I2IR in human brain frontal cortex assessed as binding affinity at low affinity site incubated for 45 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1561310Selectivity ratio of Ki for alpha2-AR high binding site in human brain frontal cortex to Ki for I2IR high binding site in human brain frontal cortex2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1767755Permeability of compound by PAMPA-BBB assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID91715Binding affinity for imidazoline receptor I-2 in rabbit kidney homogenate (relative to [3H]-Idazoxan radioligand)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
3D-QSAR CoMFA study on imidazolinergic I(2) ligands: a significant model through a combined exploration of structural diversity and methodology.
AID223237Binding affinity for rat imidazoline receptor I-1 from crude P2 membranes2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Binding of an imidazopyridoindole at imidazoline I2 receptors.
AID1767780Cytotoxicity against human NCI-H460 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID37090Displacement of [3H]RX-821002 from alpha-2 adrenergic receptor2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Pyrazino[1,2-a]indoles as novel high-affinity and selective imidazoline I(2) receptor ligands.
AID515607Intrinsic activity at dopamine D2-like receptor in pig striatal membrane assessed as [35S]GTPgammaS binding relative to control2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
AID1767779Cytotoxicity against human HCT-116 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1767744Displacement of [3H]2-BFI from imidazoline I2 receptor in post-mortem human brain frontal cortex membrane one site model measured after 30 mins by liquid scintillation counting spectrometry2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1767782Cytotoxicity against human HL-60 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1767748Selectivity index, ratio of pKi for displacement of [3H]2-BFI from imidazoline I2 receptor in post-mortem human brain frontal cortex membrane to pKi for displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in post-mortem human brain frontal cort2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1767746Displacement of [3H]2-BFI from imidazoline I2 receptor low affinity site in post-mortem human brain frontal cortex membrane two site model measured after 30 mins by liquid scintillation counting spectrometry2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID772379Binding affinity at human alpha2A AR2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID1767777Cytotoxicity against human LN-229 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID392233Selectivity index, ratio of Ki rat for MAOA to Ki for rat MAOB2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
AID1352194Competitive inhibition of recombinant human MAO-B using farnesylamine as substrate by horseradish peroxidase-Amplex red-coupled assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Design, synthesis and bioevalucation of novel 2,3-dihydro-1H-inden-1-amine derivatives as potent and selective human monoamine oxidase B inhibitors based on rasagiline.
AID1767781Cytotoxicity against human DND41 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID37100Binding affinity for rat alpha-2 adrenergic receptor from crude P2 membranes2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Binding of an imidazopyridoindole at imidazoline I2 receptors.
AID1767747Displacement of [3H]-RX821002 from adrenergic alpha 2 receptor in post-mortem human brain frontal cortex membrane measured after 30 mins by liquid scintillation counting spectrometry2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1514574Competitive inhibition of human MAOB using farnesylamine as substrate preincubated with substrate for 5 mins followed by enzyme addition by fluorimetric horseradish peroxidase-Amplex Red-coupled assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework.
AID515606Agonist activity at D2-like receptor in pig striatal membrane assessed as [35S]GTPgammaS binding2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
AID1767784Cytotoxicity against human Z138 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1514575Inhibition of tranylcypromine binding to human MAOB by fluorescence assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Novel monoamine oxidase inhibitors based on the privileged 2-imidazoline molecular framework.
AID392235Binding affinity to human MAOB imidazoline binding site2009Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2
Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
AID37362Inhibition of 1 nM [3H]RX-821002 binding to rat whole brain membrane Alpha-2 adrenergic receptors2000Bioorganic & medicinal chemistry letters, Mar-20, Volume: 10, Issue:6
Probes for imidazoline binding sites: synthesis and evaluation of a selective, irreversible I2 ligand.
AID1767783Cytotoxicity against human K562 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID1767778Cytotoxicity against human CAPAN-1 cells at 100 uM by real time IncuCyte proliferation assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID772361Antidepressant-like activity in ip dosed mouse assessed as dosed required for reduction in immobility time by forced swimming test2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID515609Displacement of [3H]RX821002 from alpha2 adrenergic receptor in rat brain membrane2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
AID772359Reduction in morphine dependence expression in ip dosed mouse assessed as dosed required for decrease in expression of naloxone-precipitated withdrawal syndrome2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID220599Compound was evaluated for hypotensive activity;no data2003Journal of medicinal chemistry, May-08, Volume: 46, Issue:10
Synthesis and biological evaluation of new 2-(4,5-dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives.
AID772372Binding affinity to I2 imidazoline binding site in rat brain membrane2013ACS medicinal chemistry letters, Sep-12, Volume: 4, Issue:9
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
AID1767743Displacement of [3H]2-BFI from imidazoline I2 receptor in post-mortem human brain frontal cortex membrane assessed as occupancy at high affinity site measured after 30 mins by liquid scintillation counting spectrometry2021European journal of medicinal chemistry, Oct-15, Volume: 222Benzofuranyl-2-imidazoles as imidazoline I
AID515605Displacement of [3H]YM-09-151-2 from D2-like receptor in pig striatal membrane2010Bioorganic & medicinal chemistry, Oct-01, Volume: 18, Issue:19
Novel imidazoline compounds as partial or full agonists of D2-like dopamine receptors inspired by I2-imidazoline binding sites ligand 2-BFI.
AID1561258Displacement of [3H]RX821002 from alpha2-AR in human brain frontal cortex incubated for 30 mins by liquid scintillation spectrometry2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Bicyclic α-Iminophosphonates as High Affinity Imidazoline I
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID977611Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB2010The Journal of biological chemistry, Nov-19, Volume: 285, Issue:47
Potentiation of ligand binding through cooperative effects in monoamine oxidase B.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (88)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's19 (21.59)18.2507
2000's26 (29.55)29.6817
2010's34 (38.64)24.3611
2020's9 (10.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.16

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 Index10.16 (24.57)
Research Supply Index4.49 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other88 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]