Page last updated: 2024-11-11

ciproxifan

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 CID6422124
CHEMBL ID14638
CHEBI ID125467
SCHEMBL ID3335184
MeSH IDM0297810

Synonyms (44)

Synonym
HY-14567
cyclopropyl-[4-[3-(3h-imidazol-4-yl)propoxy]phenyl]methanone
fub359
gtpl1265
PDSP2_001264
PDSP1_001280
NCGC00165775-01
NCGC00165775-02
cyclopropylpyrrol4-[3-(1h-imidazol-4-yl)propoxy] phenylmorphomethanone
fub 359
sc 359
cyclopropyl-(4-(3-1h-imidazol-4-yl)propyloxyphenyl)ketone
methanone, cyclopropyl(4-(3-(1h-imidazol-5-yl)propoxy)phenyl)-
ciproxifan ,
bdbm27213
fub-359
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1h-imidazole
chembl14638 ,
CHEBI:125467
NCGC00165775-03
L000187
cyclopropyl-[4-[3-(1h-imidazol-5-yl)propoxy]phenyl]methanone
184025-18-1
EX-5964
methanone, cyclopropyl(4-(3-(1h-imidazol-4-yl)propoxy)phenyl)-
5evq7irg99 ,
unii-5evq7irg99
CS-0664
BRD-K01767299-001-01-6
cyclopropyl 4-(3-(1h-imidazol-4-yl)propyloxy)phenyl ketone
SCHEMBL3335184
DTXSID50171532
EX-A077
AKOS030526676
(4-(3-(1h-imidazol-4-yl)propoxy)phenyl)(cyclopropyl)methanone
ciproxifan (fub-359)
FT-0707540
BCP04109
Q5121322
(4-(3-(1h-imidazol-5-yl)propoxy)phenyl)(cyclopropyl)methanone
SB19526
SDCCGSBI-0633732.P001
NCGC00165775-10
bdbm50458225

Research Excerpts

Overview

Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist. Its effects are promising for therapeutic applications in aging disorders.

ExcerptReferenceRelevance
"Ciproxifan appears to be a potential therapeutic agent for improving post-anesthesia cognitive memory performance."( Ciproxifan, an H3 receptor antagonist, improves short-term recognition memory impaired by isoflurane anesthesia.
Chen, R; Ding, F; Leung, LS; Liu, M; Luo, T; Zheng, L, 2016
)
2.6
"Ciproxifan appears to be an orally bioavailable, extremely potent and selective H3-receptor antagonist whose vigilance- and attention-promoting effects are promising for therapeutic applications in aging disorders."( Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Elz, S; Ganellin, CR; Jouvet, M; Ligneau, X; Lin, J; Muir, JL; Schunack, W; Schwartz, J; Stark, H; Vanni-Mercier, G, 1998
)
1.29

Treatment

ExcerptReferenceRelevance
"Ciproxifan treatment can improve memory impairment in mice by increasing ACh levels and decreasing AChE levels."( Ciproxifan attenuates the memory impairment induced by lipopolysaccharide through modulation of cholinergic transmission in the mouse brain.
Aldubayan, M; Alhowail, A; Ali, HM; Arfeen, M; Dhanasekaran, M; Hafez Abdel-Moneim, AM; Mani, V, 2022
)
3.61

Compound-Compound Interactions

ExcerptReferenceRelevance
" As ciproxifan and thioperamide are inhibitors of cytochrome P450 enzymes, responsible for metabolizing risperidone and haloperidol, the possibility that the augmentation of antipsychotics by imidazoles resulted from drug-drug interactions was tested."( Lack of cataleptogenic potentiation with non-imidazole H3 receptor antagonists reveals potential drug-drug interactions between imidazole-based H3 receptor antagonists and antipsychotic drugs.
Ballard, ME; Cowart, M; Decker, MW; Esbenshade, TA; Faghih, R; Fox, GB; Hancock, AA; Pan, L; Roberts, S; Rueter, LE; Zhang, M, 2005
)
0.89

Bioavailability

ExcerptReferenceRelevance
", led to an oral bioavailability ratio of 62%."( Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.
Elz, S; Ganellin, CR; Jouvet, M; Ligneau, X; Lin, J; Muir, JL; Schunack, W; Schwartz, J; Stark, H; Vanni-Mercier, G, 1998
)
0.57
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
aromatic ketoneA ketone in which the carbonyl group is attached to an aromatic ring.
[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 (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATAD5 protein, partialHomo sapiens (human)Potency16.14800.004110.890331.5287AID493106; AID493107
ParkinHomo sapiens (human)Potency14.58100.819914.830644.6684AID720573
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency4.22840.035520.977089.1251AID504332
NPC intracellular cholesterol transporter 1 precursorHomo sapiens (human)Potency2.31090.01262.451825.0177AID485313
D(1A) dopamine receptorHomo sapiens (human)Potency15.84890.02245.944922.3872AID488981
chromobox protein homolog 1Homo sapiens (human)Potency44.66840.006026.168889.1251AID488953
ras-related protein Rab-9AHomo sapiens (human)Potency2.31090.00022.621531.4954AID485297
Ataxin-2Homo sapiens (human)Potency3.16230.011912.222168.7989AID588378
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency37.93300.060110.745337.9330AID485368
[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)
CholinesteraseHomo sapiens (human)IC50 (µMol)77.30000.00001.559910.0000AID1540204; AID1545349
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.04270.00010.807410.0000AID365347
Adenosine receptor A3Homo sapiens (human)Ki1.00000.00000.930610.0000AID1810551
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.06310.00030.483410.0000AID365346
Amine oxidase [flavin-containing] AHomo sapiens (human)IC50 (µMol)11.26670.00002.37899.7700AID1383055; AID1540202; AID1545345
AcetylcholinesteraseHomo sapiens (human)IC50 (µMol)86.10000.00000.933210.0000AID1540200; AID1545348
Histamine H2 receptorHomo sapiens (human)Ki5.98940.00062.197310.0000AID1798786; AID365344
Amine oxidase [flavin-containing] BHomo sapiens (human)IC50 (µMol)2.03330.00001.89149.5700AID1383054; AID1540203; AID1545346
Adenosine receptor A2aHomo sapiens (human)Ki1.00000.00001.06099.7920AID1810549
Adenosine receptor A2bHomo sapiens (human)Ki1.00000.00021.635210.0000AID1810550
Adenosine receptor A1Homo sapiens (human)Ki1.00000.00020.931610.0000AID1810548
Histamine H1 receptorHomo sapiens (human)Ki5.55470.00000.511010.0000AID1057471; AID1798786; AID365343
Histamine H4 receptorHomo sapiens (human)Ki3.89020.00060.478710.0000AID1798786; AID365345; AID468419; AID597171
Histamine H3 receptorRattus norvegicus (Norway rat)Ki2.45640.00010.29638.5110AID1798786; AID239562; AID239987; AID365340; AID365342; AID89562; AID89714
Histamine H3 receptorHomo sapiens (human)Ki1.32890.00010.33998.5110AID1057472; AID1383056; AID1540197; AID1545350; AID1728994; AID1729009; AID1798786; AID1810552; AID238933; AID239591; AID239988; AID365339; AID365341; AID468415; AID597172; AID661878; AID725694; AID86456; AID86458; AID86466
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H3 receptorHomo sapiens (human)Kb0.19950.00020.20972.0000AID1728999
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (200)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processCholinesteraseHomo sapiens (human)
learningCholinesteraseHomo sapiens (human)
negative regulation of cell population proliferationCholinesteraseHomo sapiens (human)
neuroblast differentiationCholinesteraseHomo sapiens (human)
peptide hormone processingCholinesteraseHomo sapiens (human)
response to alkaloidCholinesteraseHomo sapiens (human)
cocaine metabolic processCholinesteraseHomo sapiens (human)
negative regulation of synaptic transmissionCholinesteraseHomo sapiens (human)
response to glucocorticoidCholinesteraseHomo sapiens (human)
response to folic acidCholinesteraseHomo sapiens (human)
choline metabolic processCholinesteraseHomo sapiens (human)
acetylcholine catabolic processCholinesteraseHomo sapiens (human)
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)
inflammatory responseAdenosine receptor A3Homo sapiens (human)
signal transductionAdenosine receptor A3Homo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A3Homo sapiens (human)
regulation of heart contractionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A3Homo sapiens (human)
response to woundingAdenosine receptor A3Homo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A3Homo sapiens (human)
negative regulation of cell migrationAdenosine receptor A3Homo sapiens (human)
negative regulation of NF-kappaB transcription factor activityAdenosine receptor A3Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A3Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A3Homo 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)
acetylcholine catabolic process in synaptic cleftAcetylcholinesteraseHomo sapiens (human)
regulation of receptor recyclingAcetylcholinesteraseHomo sapiens (human)
osteoblast developmentAcetylcholinesteraseHomo sapiens (human)
acetylcholine catabolic processAcetylcholinesteraseHomo sapiens (human)
cell adhesionAcetylcholinesteraseHomo sapiens (human)
nervous system developmentAcetylcholinesteraseHomo sapiens (human)
synapse assemblyAcetylcholinesteraseHomo sapiens (human)
receptor internalizationAcetylcholinesteraseHomo sapiens (human)
negative regulation of synaptic transmission, cholinergicAcetylcholinesteraseHomo sapiens (human)
amyloid precursor protein metabolic processAcetylcholinesteraseHomo sapiens (human)
positive regulation of protein secretionAcetylcholinesteraseHomo sapiens (human)
retina development in camera-type eyeAcetylcholinesteraseHomo sapiens (human)
acetylcholine receptor signaling pathwayAcetylcholinesteraseHomo sapiens (human)
positive regulation of cold-induced thermogenesisAcetylcholinesteraseHomo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo 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)
synaptic transmission, dopaminergicAdenosine receptor A2aHomo sapiens (human)
response to amphetamineAdenosine receptor A2aHomo sapiens (human)
regulation of DNA-templated transcriptionAdenosine receptor A2aHomo sapiens (human)
phagocytosisAdenosine receptor A2aHomo sapiens (human)
apoptotic processAdenosine receptor A2aHomo sapiens (human)
inflammatory responseAdenosine receptor A2aHomo sapiens (human)
cellular defense responseAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
cell-cell signalingAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, cholinergicAdenosine receptor A2aHomo sapiens (human)
central nervous system developmentAdenosine receptor A2aHomo sapiens (human)
blood coagulationAdenosine receptor A2aHomo sapiens (human)
sensory perceptionAdenosine receptor A2aHomo sapiens (human)
locomotory behaviorAdenosine receptor A2aHomo sapiens (human)
blood circulationAdenosine receptor A2aHomo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A2aHomo sapiens (human)
response to xenobiotic stimulusAdenosine receptor A2aHomo sapiens (human)
response to inorganic substanceAdenosine receptor A2aHomo sapiens (human)
positive regulation of glutamate secretionAdenosine receptor A2aHomo sapiens (human)
positive regulation of acetylcholine secretion, neurotransmissionAdenosine receptor A2aHomo sapiens (human)
regulation of norepinephrine secretionAdenosine receptor A2aHomo sapiens (human)
response to purine-containing compoundAdenosine receptor A2aHomo sapiens (human)
response to caffeineAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, GABAergicAdenosine receptor A2aHomo sapiens (human)
synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
positive regulation of urine volumeAdenosine receptor A2aHomo sapiens (human)
vasodilationAdenosine receptor A2aHomo sapiens (human)
eating behaviorAdenosine receptor A2aHomo sapiens (human)
negative regulation of vascular permeabilityAdenosine receptor A2aHomo sapiens (human)
negative regulation of neuron apoptotic processAdenosine receptor A2aHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, sleepAdenosine receptor A2aHomo sapiens (human)
negative regulation of alpha-beta T cell activationAdenosine receptor A2aHomo sapiens (human)
astrocyte activationAdenosine receptor A2aHomo sapiens (human)
neuron projection morphogenesisAdenosine receptor A2aHomo sapiens (human)
positive regulation of protein secretionAdenosine receptor A2aHomo sapiens (human)
negative regulation of inflammatory responseAdenosine receptor A2aHomo sapiens (human)
regulation of mitochondrial membrane potentialAdenosine receptor A2aHomo sapiens (human)
membrane depolarizationAdenosine receptor A2aHomo sapiens (human)
regulation of calcium ion transportAdenosine receptor A2aHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicAdenosine receptor A2aHomo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
inhibitory postsynaptic potentialAdenosine receptor A2aHomo sapiens (human)
prepulse inhibitionAdenosine receptor A2aHomo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2aHomo sapiens (human)
positive regulation of long-term synaptic potentiationAdenosine receptor A2aHomo sapiens (human)
positive regulation of apoptotic signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
positive regulation of chronic inflammatory response to non-antigenic stimulusAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
activation of adenylate cyclase activityAdenosine receptor A2bHomo sapiens (human)
positive regulation of vascular endothelial growth factor productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
cGMP-mediated signalingAdenosine receptor A2bHomo sapiens (human)
positive regulation of chemokine productionAdenosine receptor A2bHomo sapiens (human)
positive regulation of interleukin-6 productionAdenosine receptor A2bHomo sapiens (human)
mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
positive regulation of mast cell degranulationAdenosine receptor A2bHomo sapiens (human)
relaxation of vascular associated smooth muscleAdenosine receptor A2bHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAdenosine receptor A2bHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAdenosine receptor A2bHomo sapiens (human)
vasodilationAdenosine receptor A2bHomo sapiens (human)
temperature homeostasisAdenosine receptor A1Homo sapiens (human)
response to hypoxiaAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of respiratory gaseous exchange by nervous system processAdenosine receptor A1Homo sapiens (human)
negative regulation of acute inflammatory responseAdenosine receptor A1Homo sapiens (human)
negative regulation of leukocyte migrationAdenosine receptor A1Homo sapiens (human)
positive regulation of peptide secretionAdenosine receptor A1Homo sapiens (human)
positive regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
negative regulation of systemic arterial blood pressureAdenosine receptor A1Homo sapiens (human)
regulation of glomerular filtrationAdenosine receptor A1Homo sapiens (human)
protein targeting to membraneAdenosine receptor A1Homo sapiens (human)
phagocytosisAdenosine receptor A1Homo sapiens (human)
inflammatory responseAdenosine receptor A1Homo sapiens (human)
signal transductionAdenosine receptor A1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
cell-cell signalingAdenosine receptor A1Homo sapiens (human)
nervous system developmentAdenosine receptor A1Homo sapiens (human)
negative regulation of cell population proliferationAdenosine receptor A1Homo sapiens (human)
response to inorganic substanceAdenosine receptor A1Homo sapiens (human)
negative regulation of glutamate secretionAdenosine receptor A1Homo sapiens (human)
response to purine-containing compoundAdenosine receptor A1Homo sapiens (human)
lipid catabolic processAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, GABAergicAdenosine receptor A1Homo sapiens (human)
positive regulation of nucleoside transportAdenosine receptor A1Homo sapiens (human)
negative regulation of neurotrophin productionAdenosine receptor A1Homo sapiens (human)
positive regulation of protein dephosphorylationAdenosine receptor A1Homo sapiens (human)
vasodilationAdenosine receptor A1Homo sapiens (human)
negative regulation of circadian sleep/wake cycle, non-REM sleepAdenosine receptor A1Homo sapiens (human)
negative regulation of apoptotic processAdenosine receptor A1Homo sapiens (human)
positive regulation of potassium ion transportAdenosine receptor A1Homo sapiens (human)
positive regulation of MAPK cascadeAdenosine receptor A1Homo sapiens (human)
negative regulation of hormone secretionAdenosine receptor A1Homo sapiens (human)
cognitionAdenosine receptor A1Homo sapiens (human)
leukocyte migrationAdenosine receptor A1Homo sapiens (human)
detection of temperature stimulus involved in sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
positive regulation of lipid catabolic processAdenosine receptor A1Homo sapiens (human)
regulation of sensory perception of painAdenosine receptor A1Homo sapiens (human)
negative regulation of synaptic transmission, glutamatergicAdenosine receptor A1Homo sapiens (human)
fatty acid homeostasisAdenosine receptor A1Homo sapiens (human)
excitatory postsynaptic potentialAdenosine receptor A1Homo sapiens (human)
long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
mucus secretionAdenosine receptor A1Homo sapiens (human)
negative regulation of mucus secretionAdenosine receptor A1Homo sapiens (human)
triglyceride homeostasisAdenosine receptor A1Homo sapiens (human)
regulation of cardiac muscle cell contractionAdenosine receptor A1Homo sapiens (human)
apoptotic signaling pathwayAdenosine receptor A1Homo sapiens (human)
regulation of presynaptic cytosolic calcium ion concentrationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic potentiationAdenosine receptor A1Homo sapiens (human)
negative regulation of long-term synaptic depressionAdenosine receptor A1Homo sapiens (human)
G protein-coupled receptor signaling pathwayAdenosine receptor A1Homo sapiens (human)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
negative regulation of receptor internalizationAtaxin-2Homo sapiens (human)
regulation of translationAtaxin-2Homo sapiens (human)
RNA metabolic processAtaxin-2Homo sapiens (human)
P-body assemblyAtaxin-2Homo sapiens (human)
stress granule assemblyAtaxin-2Homo sapiens (human)
RNA transportAtaxin-2Homo sapiens (human)
inflammatory responseHistamine H4 receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationHistamine H4 receptorHomo sapiens (human)
biological_processHistamine H4 receptorHomo sapiens (human)
regulation of MAPK cascadeHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H4 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H4 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H4 receptorHomo sapiens (human)
neurotransmitter secretionHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H3 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H3 receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (49)

Processvia Protein(s)Taxonomy
amyloid-beta bindingCholinesteraseHomo sapiens (human)
catalytic activityCholinesteraseHomo sapiens (human)
acetylcholinesterase activityCholinesteraseHomo sapiens (human)
cholinesterase activityCholinesteraseHomo sapiens (human)
protein bindingCholinesteraseHomo sapiens (human)
hydrolase activity, acting on ester bondsCholinesteraseHomo sapiens (human)
enzyme bindingCholinesteraseHomo sapiens (human)
choline bindingCholinesteraseHomo sapiens (human)
identical protein bindingCholinesteraseHomo sapiens (human)
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)
G protein-coupled adenosine receptor activityAdenosine receptor A3Homo 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)
amyloid-beta bindingAcetylcholinesteraseHomo sapiens (human)
acetylcholinesterase activityAcetylcholinesteraseHomo sapiens (human)
cholinesterase activityAcetylcholinesteraseHomo sapiens (human)
protein bindingAcetylcholinesteraseHomo sapiens (human)
collagen bindingAcetylcholinesteraseHomo sapiens (human)
hydrolase activityAcetylcholinesteraseHomo sapiens (human)
serine hydrolase activityAcetylcholinesteraseHomo sapiens (human)
acetylcholine bindingAcetylcholinesteraseHomo sapiens (human)
protein homodimerization activityAcetylcholinesteraseHomo sapiens (human)
laminin bindingAcetylcholinesteraseHomo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo 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)
G protein-coupled adenosine receptor activityAdenosine receptor A2aHomo sapiens (human)
protein bindingAdenosine receptor A2aHomo sapiens (human)
calmodulin bindingAdenosine receptor A2aHomo sapiens (human)
lipid bindingAdenosine receptor A2aHomo sapiens (human)
enzyme bindingAdenosine receptor A2aHomo sapiens (human)
type 5 metabotropic glutamate receptor bindingAdenosine receptor A2aHomo sapiens (human)
identical protein bindingAdenosine receptor A2aHomo sapiens (human)
protein-containing complex bindingAdenosine receptor A2aHomo sapiens (human)
alpha-actinin bindingAdenosine receptor A2aHomo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A2bHomo sapiens (human)
protein bindingAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor activityAdenosine receptor A2bHomo sapiens (human)
G protein-coupled receptor bindingAdenosine receptor A1Homo sapiens (human)
purine nucleoside bindingAdenosine receptor A1Homo sapiens (human)
protein bindingAdenosine receptor A1Homo sapiens (human)
heat shock protein bindingAdenosine receptor A1Homo sapiens (human)
G-protein beta/gamma-subunit complex bindingAdenosine receptor A1Homo sapiens (human)
heterotrimeric G-protein bindingAdenosine receptor A1Homo sapiens (human)
protein heterodimerization activityAdenosine receptor A1Homo sapiens (human)
G protein-coupled adenosine receptor activityAdenosine receptor A1Homo sapiens (human)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
RNA bindingAtaxin-2Homo sapiens (human)
epidermal growth factor receptor bindingAtaxin-2Homo sapiens (human)
protein bindingAtaxin-2Homo sapiens (human)
mRNA bindingAtaxin-2Homo sapiens (human)
histamine receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H4 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H4 receptorHomo sapiens (human)
histamine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled acetylcholine receptor activityHistamine H3 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (46)

Processvia Protein(s)Taxonomy
extracellular regionCholinesteraseHomo sapiens (human)
nuclear envelope lumenCholinesteraseHomo sapiens (human)
endoplasmic reticulum lumenCholinesteraseHomo sapiens (human)
blood microparticleCholinesteraseHomo sapiens (human)
plasma membraneCholinesteraseHomo sapiens (human)
extracellular spaceCholinesteraseHomo sapiens (human)
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)
plasma membraneAdenosine receptor A3Homo sapiens (human)
presynaptic membraneAdenosine receptor A3Homo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A3Homo sapiens (human)
dendriteAdenosine receptor A3Homo sapiens (human)
plasma membraneAdenosine receptor A3Homo sapiens (human)
synapseAdenosine receptor A3Homo 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)
extracellular regionAcetylcholinesteraseHomo sapiens (human)
basement membraneAcetylcholinesteraseHomo sapiens (human)
extracellular spaceAcetylcholinesteraseHomo sapiens (human)
nucleusAcetylcholinesteraseHomo sapiens (human)
Golgi apparatusAcetylcholinesteraseHomo sapiens (human)
plasma membraneAcetylcholinesteraseHomo sapiens (human)
cell surfaceAcetylcholinesteraseHomo sapiens (human)
membraneAcetylcholinesteraseHomo sapiens (human)
neuromuscular junctionAcetylcholinesteraseHomo sapiens (human)
synaptic cleftAcetylcholinesteraseHomo sapiens (human)
synapseAcetylcholinesteraseHomo sapiens (human)
perinuclear region of cytoplasmAcetylcholinesteraseHomo sapiens (human)
side of membraneAcetylcholinesteraseHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo 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)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
intermediate filamentAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2aHomo sapiens (human)
membraneAdenosine receptor A2aHomo sapiens (human)
dendriteAdenosine receptor A2aHomo sapiens (human)
axolemmaAdenosine receptor A2aHomo sapiens (human)
asymmetric synapseAdenosine receptor A2aHomo sapiens (human)
presynaptic membraneAdenosine receptor A2aHomo sapiens (human)
neuronal cell bodyAdenosine receptor A2aHomo sapiens (human)
postsynaptic membraneAdenosine receptor A2aHomo sapiens (human)
presynaptic active zoneAdenosine receptor A2aHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2aHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
Schaffer collateral - CA1 synapseAdenosine receptor A2bHomo sapiens (human)
presynapseAdenosine receptor A2bHomo sapiens (human)
glutamatergic synapseAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A2bHomo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
plasma membraneAdenosine receptor A1Homo sapiens (human)
basolateral plasma membraneAdenosine receptor A1Homo sapiens (human)
axolemmaAdenosine receptor A1Homo sapiens (human)
asymmetric synapseAdenosine receptor A1Homo sapiens (human)
presynaptic membraneAdenosine receptor A1Homo sapiens (human)
neuronal cell bodyAdenosine receptor A1Homo sapiens (human)
terminal boutonAdenosine receptor A1Homo sapiens (human)
dendritic spineAdenosine receptor A1Homo sapiens (human)
calyx of HeldAdenosine receptor A1Homo sapiens (human)
postsynaptic membraneAdenosine receptor A1Homo sapiens (human)
presynaptic active zoneAdenosine receptor A1Homo sapiens (human)
synapseAdenosine receptor A1Homo sapiens (human)
dendriteAdenosine receptor A1Homo sapiens (human)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
cytoplasmAtaxin-2Homo sapiens (human)
Golgi apparatusAtaxin-2Homo sapiens (human)
trans-Golgi networkAtaxin-2Homo sapiens (human)
cytosolAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
membraneAtaxin-2Homo sapiens (human)
perinuclear region of cytoplasmAtaxin-2Homo sapiens (human)
ribonucleoprotein complexAtaxin-2Homo sapiens (human)
cytoplasmic stress granuleAtaxin-2Homo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H4 receptorHomo sapiens (human)
dendriteHistamine H4 receptorHomo sapiens (human)
synapseHistamine H4 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
presynapseHistamine H3 receptorHomo sapiens (human)
plasma membraneHistamine H3 receptorHomo sapiens (human)
synapseHistamine H3 receptorHomo sapiens (human)
dendriteHistamine H3 receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (125)

Assay IDTitleYearJournalArticle
AID1346055Human H4 receptor (Histamine receptors)2004Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
AID1346107Human H3 receptor (Histamine receptors)2004Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
AID1346017Rat H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
AID1346107Human H3 receptor (Histamine receptors)2001The Biochemical journal, Apr-15, Volume: 355, Issue:Pt 2
Genomic organization and characterization of splice variants of the human histamine H3 receptor.
AID1346088Mouse H3 receptor (Histamine receptors)2004Journal of neurochemistry, Sep, Volume: 90, Issue:6
Cloning and expression of the mouse histamine H3 receptor: evidence for multiple isoforms.
AID1346095Human H2 receptor (Histamine receptors)2015Pharmacological reviews, Jul, Volume: 67, Issue:3
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346107Human H3 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346017Rat H3 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1346017Rat H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1346017Rat H3 receptor (Histamine receptors)2004Biochemical pharmacology, Sep-01, Volume: 68, Issue:5
Pharmacological and behavioral properties of A-349821, a selective and potent human histamine H3 receptor antagonist.
AID1346107Human H3 receptor (Histamine receptors)2000British journal of pharmacology, Dec, Volume: 131, Issue:7
Distinct pharmacology of rat and human histamine H(3) receptors: role of two amino acids in the third transmembrane domain.
AID1346107Human H3 receptor (Histamine receptors)2015Pharmacological reviews, Jul, Volume: 67, Issue:3
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346017Rat H3 receptor (Histamine receptors)2001Biochemical and biophysical research communications, Jan-12, Volume: 280, Issue:1
The rat H3 receptor: gene organization and multiple isoforms.
AID1346107Human H3 receptor (Histamine receptors)2002European journal of pharmacology, Oct-18, Volume: 453, Issue:1
Characteristics of recombinantly expressed rat and human histamine H3 receptors.
AID1346055Human H4 receptor (Histamine receptors)2015Pharmacological reviews, Jul, Volume: 67, Issue:3
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346037Human H1 receptor (Histamine receptors)2015Pharmacological reviews, Jul, Volume: 67, Issue:3
International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346055Human H4 receptor (Histamine receptors)2003The Journal of pharmacology and experimental therapeutics, Jun, Volume: 305, Issue:3
Two novel and selective nonimidazole histamine H3 receptor antagonists A-304121 and A-317920: I. In vitro pharmacological effects.
AID1540200Inhibition of human AChE2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID365358Antagonist activity at histamine H3 receptor in guinea pig ileum assessed as inhibition of (R)-alpha-methylhistamine-induced response2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1383056Binding affinity to human H3R
AID238933Antagonist potency against human H3 receptor in GTPgamma-S-Assay2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
2-(4-alkylpiperazin-1-yl)quinolines as a new class of imidazole-free histamine H3 receptor antagonists.
AID239591In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID1810554Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis
AID365347Displacement of [3H]rauwolscine from human adrenergic alpha 2C10 receptor expressed in mouse LTK- cells2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID365345Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK cells2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID365356Antagonist activity at human full length histamine H3 receptor expressed in HEK293 cells assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1540197Inhibition of human histamine H3 receptor2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID661878Binding affinity to human H3 receptor2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
AID365357Antagonist activity at rat full length histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced intracellular calcium release by FLIPR2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID365355Antagonist activity at rat full length histamine H3 receptor expressed in HEK cells assessed as inhibition of forskolin-induced intracellular calcium release by SPA2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID365343Displacement of [3H]mepyramine from human histamine H1 receptor2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1728998Agonist activity at C-terminal SmBit/mini-Gi protein-fused/N-terminal LgBit-tagged human H3R stably expressed in HEK293T cells assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by Nano-glo luminescence2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID725694Displacement of [3H]Nalpha-methylhistamine from human recombinant histamine H3 receptor expressed in HEK-293 cells2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.
AID1729009Binding affinity to human H3R2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID597171Displacement of [3H]histamine from human full-length histamine H4 receptor expressed in HEK293 cells after 60 mins2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID1057468Reversal of RAMH-induced dipsogenia in Lister Hooded rat at 3 mg/kg, po2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
The discovery of the benzazepine class of histamine H3 receptor antagonists.
AID236100Oral bioavailability in rat (dose 1-5 mg/kg i.v.)2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365344Displacement of [3H]tiotidine from human histamine H2 receptor2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID239562In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID86456Antagonist potency against human histamine H3 receptor expressed in CHO cells was determined by GTPgamma-S-assay2004Journal of medicinal chemistry, May-20, Volume: 47, Issue:11
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
AID1545349Inhibition of human plasma butyrylcholinesterase by Ellman's method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID780102Awakening activity in rat assessed as increased wakefulness at 10 mg/kg, ip after 3 hrs2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Discovery of a potent, selective, and orally bioavailable histamine H3 receptor antagonist SAR110068 for the treatment of sleep-wake disorders.
AID1728994Displacement of [3H]UR-PI294 from human SP-FLAG-tagged H3R expressed in HEK293T cells measured after 60 to 120 mins by liquid scintillation counting analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID86627In vivo effects in mice against H3 receptor on N6-methylhistamine levels in brain (following oral dosing of compound)2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
AID239987In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing rat histamine H3 receptor2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365352Antagonist activity at human full length histamine H3 receptor expressed in HEK cells assessed as inhibition of [35S]gammaGTP binding relative to control2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID468419Displacement of [3H]histamine from human histamine H4 receptor expressed in HEK293 cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID1810548Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting analysis
AID237820Concentration in brain of rats after 1 hr of intravenous administration2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365349Displacement of [3H]LY278584 from 5HT2 receptor in rat frontal cortex2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID597172Displacement of [125I]iodoproxyfan from human full-length histamine H3 receptor expressed in HEK293 cells after 60 mins2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID597174Antagonist activity at histamine H3 receptor in po dosed 24 hrs fasted Swiss mouse brain assessed as t-MeHA level2011Bioorganic & medicinal chemistry, May-01, Volume: 19, Issue:9
N-Alkenyl and cycloalkyl carbamates as dual acting histamine H3 and H4 receptor ligands.
AID89716In vitro inhibitory activity against Histamine H3 receptor for K+ evoked depolarization-induced release of [3H]histamine from synaptosomes of rat cerebral cortex2000Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
AID1545350Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID86458Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID1540204Inhibition of human BChE2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID236517Clearance was observed in rat after intravenous administration of 1-5 mg/kg2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365350Displacement of [3H]LY278584 from 5HT3 receptor in rat frontal cortex2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1545348Inhibition of human acetylcholinesterase expressed in HEK 293 cells using acetylthiocholine iodide as substrate by Ellman's method2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1810550Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis
AID1810551Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis
AID89708Histamine H3 receptor antagonist activity in an assay with K+ evoked depolarization-induced release of [3H]-histamine from rat synaptosomes.2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
AID1728993Inhibition of recombinant CYP3A4 (unknown origin) at 10 uM measured after 30 mins by luciferase reporter gene assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID1383054Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method
AID1810555Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis
AID1810549Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis
AID1057472Antagonist activity at human histamine H3 receptor expressed in CHOK1 cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
The discovery of the benzazepine class of histamine H3 receptor antagonists.
AID365354Antagonist activity at human full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of forskolin-induced cAMP release by SPA2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID88633In vivo Histamine H3 receptor antagonism, dose required to increase in N-t-methylhistamine levels in Swiss mice brains 90 min after p.o. administration2000Bioorganic & medicinal chemistry letters, Oct-16, Volume: 10, Issue:20
Analogues and derivatives of ciproxifan, a novel prototype for generating potent histamine H3-receptor antagonists.
AID1540203Inhibition of human MAOB2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID1383055Inhibition of human MAO-A expressed in baculovirus infected insect cell membranes using kynuramine as substrate up to 30 mins by spectrophotometric method
AID1810553Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis
AID130836In vivo potency on [3H]histamine level in mouse brain cortex at a dose of 3 mg/kg2002Journal of medicinal chemistry, Feb-28, Volume: 45, Issue:5
Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
AID365342Displacement of [3H]NAMH from histamine H3 receptor in rat cortex2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID86466Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressing CHO cells2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel nonimidazole histamine H3 receptor antagonists: 1-(4-(phenoxymethyl)benzyl)piperidines and related compounds.
AID131007Potency after oral administration in vivo in mice2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
AID661879Selectivity ratio of Ki for human H3 receptor to Ki for rat H3 receptor2012Journal of medicinal chemistry, Mar-08, Volume: 55, Issue:5
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype.
AID237554Volume of distribution was observed in rat after intravenous administration of 1-5 mg/kg2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID89885Ratio of binding affinity of rat histamine H3 receptor to that of human histamine H3 receptor; 1:122001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID239988In vitro binding affinity was determined as displacement of [3H]N-R-methylhistamine from C6 cell membranes expressing human histamine H3 receptor2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365353Antagonist activity at rat full length histamine H3 receptor expressed in rat C6 cells assessed as inhibition of [35S]gammaGTP binding relative to control2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1545346Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID365346Displacement of [3H]rauwolscine from human adrenergic alpha 2C4 receptor expressed in mouse LTK- cells2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1057471Antagonist activity at human recombinant histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced effect by FLIPR assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
The discovery of the benzazepine class of histamine H3 receptor antagonists.
AID302579Memory enhancing effect in ip dosed adult rat by social recognition memory method2007Journal of medicinal chemistry, Nov-01, Volume: 50, Issue:22
Synthesis, potency, and in vivo profiles of quinoline containing histamine H3 receptor inverse agonists.
AID468415Displacement of [3H]iodoproxyfan from human histamine H3 receptor expressed in CHO-K1 cells2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID131347Dose required to increase N-methyl-histamine levels in mouse brain cortex after perorally administration as an index of increased histaminergic neuron activity.2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
New histamine H(3)-receptor ligands of the proxifan series: imoproxifan and other selective antagonists with high oral in vivo potency.
AID365340Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1545345Inhibition of recombinant human MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate by Amplex red reagent/horseradish peroxidase coupled fluorescence assay2019Bioorganic & medicinal chemistry, 03-15, Volume: 27, Issue:6
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
AID1637854Reduction in food consumption in Wistar rat at 3 mg/kg, sc administered daily for 5 days relative to control2019MedChemComm, Feb-01, Volume: 10, Issue:2
Design, synthesis, and
AID1057470Binding affinity to human serum albumin2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
The discovery of the benzazepine class of histamine H3 receptor antagonists.
AID1728999Antagonist activity at C-terminal SmBit/mini-Gi protein-fused/N-terminal LgBit-tagged human H3R stably expressed in HEK293T cells assessed as inhibition of histamine-induced mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by2021European journal of medicinal chemistry, Mar-05, Volume: 213Structural modifications in the distal, regulatory region of histamine H
AID1810556Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells at 1 uM by liquid scintillation counting analysis
AID1810552Displacement of [3H] N-alpha methylhistamine from human recombinant histamine H3 receptor expressed in HEK293 cells measured after 90 mins
AID246007Tested for their ability to enhance memory in the adult rats using social recognition memory test2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365341Displacement of [3H]NAMH from histamine H3 receptor in human cortex2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID239893Tested for its ability to block human histamine H3 receptor activation by the agonist R-alpha-methyl histamine in a [Ca2+] flux assay2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID89714In vitro binding affinity against rat histamine H3 receptor2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
4-(omega-(alkyloxy)alkyl)-1H-imidazole derivatives as histamine H(3) receptor antagonists/agonists.
AID365339Displacement of [3H]NAMH from human full length histamine H3 receptor expressed in rat C6 cells2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID237264Half life was observed in rat after intravenous administration of 3-5 mg/kg; (n=3)2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID246006Lowest dose to induce CNS side effects was assessed in a general behavioral screen in rats2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID468416Selectivity, ratio of Ki for human histaminee H4 receptor to Ki for human histamine H3 receptor2009Bioorganic & medicinal chemistry letters, Dec-01, Volume: 19, Issue:23
Histamine H3 and H4 receptor affinity of branched 3-(1H-imidazol-4-yl)propyl N-alkylcarbamates.
AID89562Inhibition of [125I]iodoproxyfan from rat histamine H3 receptor expressed in CHO-K1 cells2001Bioorganic & medicinal chemistry letters, Apr-09, Volume: 11, Issue:7
Different antagonist binding properties of human and rat histamine H3 receptors.
AID246008Tested for their ability to enhance learning in the rat pups using inhibitory avoidance acquisition model2005Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
4-(2-[2-(2(R)-methylpyrrolidin-1-yl)ethyl]benzofuran-5-yl)benzonitrile and related 2-aminoethylbenzofuran H3 receptor antagonists potently enhance cognition and attention.
AID365348Displacement of [3H]LY278584 from 5HT1 receptor in rat frontal cortex2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
AID1540202Inhibition of human MAOA2019European journal of medicinal chemistry, Oct-15, Volume: 180Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
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.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1798786Radioligand Binding Assay from Article 10.1021/jm8003625: \\The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.\\2008Journal of medicinal chemistry, Sep-11, Volume: 51, Issue:17
The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (105)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's4 (3.81)18.2507
2000's48 (45.71)29.6817
2010's39 (37.14)24.3611
2020's14 (13.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 37.09

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

MetricThis Compound (vs All)
Research Demand Index37.09 (24.57)
Research Supply Index4.67 (2.92)
Research Growth Index4.91 (4.65)
Search Engine Demand Index50.74 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (37.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (2.83%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other103 (97.17%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]