Page last updated: 2024-12-10

ar-r 17779

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Description

AR-R 17779: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5310971
CHEMBL ID193016
SCHEMBL ID676252
MeSH IDM0362800

Synonyms (31)

Synonym
178419-47-1
ar-r17779
ar-r13489
ar-r-17779
spiro(1-azabicyclo(2.2.2)octane-3,5'-oxazolidin-2'-one)
ar-r 17779
bdbm50164613
(2s)-2''h-spiro[4-azabicyclo[2.2.2]octane-2,5''-[1,3]oxazolidin]-2''-one
(s)-1''-azaspiro[oxazolidine-5,8''-bicyclo[2.2.2]octan]-2-one
(-)-spiro[1-azabicyclo(2.2.2)octane-3,5''-oxazolidin-2''-one]
CHEMBL193016 ,
(5s)-spiro[1,3-oxazolidine-5,3'-1-azabicyclo[2.2.2]octane]-2-one
AKOS015962649
ar-r17779 hcl
SCHEMBL676252
(3s)-spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin]-2'-one
(s)-spiro[1-azabicyclo[2.2.2]octan-3,5'-oxazolidin]-2'-one
TYAGAVRSOFABFO-VIFPVBQESA-N ,
DTXSID60415499
spiro[1-azabicyclo[2.2.2]octane-3,5-oxazolidin]-2-one, (3s)- (9ci)
(s)-spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one
unii-c3vz57bn3m
BCP24016
Q4653530
(3s)-spiro(1-azabicyclo(2.2.2)octane-3,5'-oxazolidin)-2'-one
spiro(1-azabicyclo(2.2.2)octane-3,5'-oxazolidin)-2'-one, (3s)-
c3vz57bn3m ,
(s)-4-azaspiro[bicyclo[2.2.2]octane-2,5'-oxazolidin]-2'-one
spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin]-2'-one, (3s)-
(2s)-4-azaspiro[bicyclo[2.2.2]octane-2,2'-[1,4]oxazolidin]-5'-one
PD045402

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" Compound 25 has potent binding affinity (K(i) = 9 nmol/L) and good selectivity toward the other nicotinic subtypes (alpha4beta2 and alpha1beta2gammadelta) and has been found in pharmacokinetic evaluation to have good oral bioavailability and brain permeability."( Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
Fujio, M; Hashimoto, K; Katayama, J; Satoh, H; Takanashi, S; Tanaka, H; Tatsumi, R, 2005
)
0.33
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (8)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki16.00000.00000.12345.5000AID220124
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki16.00000.00000.10825.5000AID220124
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)IC50 (µMol)2,000.00000.00110.539010.0000AID146308
Neuronal acetylcholine receptor subunit beta-4Homo sapiens (human)IC50 (µMol)1,000.00000.00181.67796.5000AID146148
Neuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)IC50 (µMol)1,000.00000.00181.31326.5000AID146148
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)Ki0.28400.00221.742710.0000AID690406; AID690417; AID690419
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)2,000.00000.00110.491110.0000AID146308
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.21600.00000.73078.0000AID1338774; AID239253
[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)
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)EC50 (µMol)1.47270.12802.80188.9000AID391584; AID418232; AID690416
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)Kd0.09200.00110.04040.1580AID391583
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)EC50 (µMol)10.69000.00021.848110.0000AID146796; AID690420
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (78)

Processvia Protein(s)Taxonomy
response to hypoxiaNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
smooth muscle contractionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
visual perceptionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
sensory perception of soundNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
associative learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
visual learningNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dopamine secretionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
sensory perception of painNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
vestibulocochlear nerve developmentNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
optic nerve morphogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
lateral geniculate nucleus developmentNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
central nervous system projection neuron axonogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
positive regulation of B cell proliferationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of synaptic transmission, dopaminergicNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
positive regulation of dopamine secretionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
social behaviorNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dopamine metabolic processNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
B cell activationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to cocaineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of circadian sleep/wake cycle, REM sleepNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to ethanolNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
negative regulation of action potentialNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of dendrite morphogenesisNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
nervous system processNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
regulation of synapse assemblyNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
smooth muscle contractionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
regulation of smooth muscle contractionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
neuronal action potentialNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
regulation of neurotransmitter secretionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
positive regulation of transmission of nerve impulseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of smooth muscle contractionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
activation of transmembrane receptor protein tyrosine kinase activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nervous system developmentNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
locomotory behaviorNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of acetylcholine secretion, neurotransmissionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
regulation of dendrite morphogenesisNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synaptic transmission involved in micturitionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein phosphorylationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
intracellular calcium ion homeostasisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
learning or memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
short-term memoryNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of cell population proliferationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of tumor necrosis factor productionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of MAPK cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of angiogenesisNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapse organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
sensory processingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of protein metabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendritic spine organizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
modulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
dendrite arborizationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of long-term synaptic potentiationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
negative regulation of amyloid-beta formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid precursor protein catabolic processNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to amyloid-betaNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
response to acetylcholineNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of amyloid fibril formationNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of CoA-transferase activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
action potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to hypoxiaNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
DNA repairNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
monoatomic ion transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
calcium ion transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to oxidative stressNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
signal transductionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
regulation of dopamine secretionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
sensory perception of painNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
B cell activationNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
regulation of membrane potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
nervous system processNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
cognitionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
inhibitory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
protein-containing complex bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
quaternary ammonium group bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
heterocyclic compound bindingNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
amyloid-beta bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
calcium channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
toxic substance bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
chloride channel regulator activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein homodimerization activityNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
protein bindingNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine bindingNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
external side of plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
presynaptic membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
cholinergic synapseNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
postsynaptic specialization membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit beta-2Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
specific granule membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
tertiary granule membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
cholinergic synapseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit beta-4Homo sapiens (human)
endoplasmic reticulumNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
Golgi apparatusNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic densityNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
nuclear speckNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
dendriteNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuronal cell bodyNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-3Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membrane raftNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
postsynapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
external side of plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
dendriteNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
neuronal cell bodyNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (40)

Assay IDTitleYearJournalArticle
AID145997Activation responses to that evoked by Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes at 300 uM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID236430Area under plasma concentration time curve 24 hours after peroral dosing of 10.0 mg/kg (AUC) in rats (N=4)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID242611Inhibition of [3H]-Cytisine binding to nicotinic acetylcholine receptor alpha4-beta2 from rat cerebral cortex2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID418232Agonist activity at human recombinant alpha7 nAChR expressed in rat GH3 cells by calcium influx assay2009Bioorganic & medicinal chemistry letters, Mar-01, Volume: 19, Issue:5
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists.
AID146921Potency was determined by measuring current activation in Xenopus oocytes expressing rat alpha-7 nAChRs; ND denotes no data.2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
AID690417Displacement of [3H]-MLA from alpha7 nAChR2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID1338778Antagonist activity at 5-HT3A (unknown origin) at 10 uM2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
AID1338774Displacement of [125I]alpha-bungarotoxin from rat hippocampal alpha7 nAChR measured after 2 hrs by TopCount scintillation counting method2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
AID236146Oral bioavailability of compound after peroral dosing of 10.0 mg/kg in rats (N=4)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID146957Maximum responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID146796Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID690418Agonist activity at rat alpha7 nAchR expressed in Xenopus oocyte relative to control2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID146148Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID690416Agonist activity at human recombinant alpha7 nAChR expressed in GH4 cells2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID1338779Intrinsic activity at rat alpha7 nAChR expressed in Xenopus oocytes measured after 5 mins relative to acetylcholine2016Journal of medicinal chemistry, 12-22, Volume: 59, Issue:24
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
AID465084Selectivity of beta4 nAChR over beta2 nAChR2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Phantasmidine: an epibatidine congener from the ecuadorian poison frog Epipedobates anthonyi.
AID690279Binding affinity to human 5HT3 receptor at 10 uM by radioligand binding assay2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID146645Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-3-beta-2-alpha-5 expressed in xenopus oocytes at 100 uM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID690415Agonist activity at human recombinant alpha7 nAChR expressed in GH4 cells relative to control2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID391584Agonist activity at human cloned wild-type alpha7 nAChR expressed in Xenopus laevis oocytes assessed as channel opening by voltage clamp electrophysiology2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
AID236942Half-life of plasma concentration after peroral dosing of 10.0 mg/kg in rats (N=4)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID690420Agonist activity at rat alpha7 nAchR expressed in Xenopus oocyte2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID146303Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha4-beta22004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID237800Brain permeability is determined by ratio of concentration of compound in brain to that of in plasma (CB/CP) 1 hr after subcutaneous dosing of 1.0 mg/kg (N=3)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID146145Activation responses to that evoked by ACh at human alpha3-beta4 receptor expressed in xenopus oocytes at 1 mM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID146304Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes at 300 uM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID145996Activation responses to that evoked by Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes at 1 mM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID391583Displacement of [125I]alpha-bungarotoxin from alpha7 nAChR2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
AID220455binding affinity in rat hippocampi against alpha7 nicotinic receptor2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
AID146308Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID690406Binding affinity to alpha7 nAChR2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID147081Intrinsic activity was determined by measuring current activation in Xenopus oocytes expressing rat alpha-7 nAChRs; ND denotes no data.2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
AID690419Displacement of [125I]alpha-Bungarotoxin from alpha7 nAchR2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Discovery and development of α7 nicotinic acetylcholine receptor modulators.
AID6381Ability to block serotonin (30 uM)-evoked responses at rat 5HT3-alpha receptor expressed in xenopus oocytes2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID236625Maximum plasma concentration after peroral dosing of 10.0 mg/kg in rats (N=4)2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID6382Effect on rat 5-hydroxytryptamine 3a receptor expressed in xenopus oocytes at concentration up to 100 uM2004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
AID391585Agonist activity at human cloned alpha7 nAChR Gln117Phe mutant expressed in Xenopus laevis oocytes assessed as channel opening by voltage clamp electrophysiology2008Journal of medicinal chemistry, Oct-23, Volume: 51, Issue:20
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
AID242603Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha1-beta2-delta-gamma from BC3H1 cells2005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
AID220124binding affinity in rat forebrain against alpha4-beta2 nicotinic receptor2000Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
AID239253Inhibition of [125I]alpha-bungarotoxin binding to rat nicotinic acetylcholine receptor alpha72005Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7
Discovery of the alpha7 nicotinic acetylcholine receptor agonists. (R)-3'-(5-Chlorothiophen-2-yl)spiro-1-azabicyclo[2.2.2]octane-3,5'-[1',3']oxazolidin-2'-one as a novel, potent, selective, and orally bioavailable ligand.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (34)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (2.94)18.2507
2000's18 (52.94)29.6817
2010's13 (38.24)24.3611
2020's2 (5.88)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.38

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

MetricThis Compound (vs All)
Research Demand Index11.38 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index4.96 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (11.38)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (2.86%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other34 (97.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]