Page last updated: 2024-11-05

dihydro-beta-erythroidine

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

Description

Dihydro-beta-erythroidine is a synthetic analog of the natural alkaloid beta-erythroidine. It acts as a potent and selective antagonist of nicotinic acetylcholine receptors, particularly the alpha4beta2 subtype. This makes it a valuable tool for studying the role of these receptors in various biological processes. Dihydro-beta-erythroidine has been used to investigate the involvement of alpha4beta2 receptors in cognition, memory, and the regulation of neuronal excitability. It has also been explored as a potential therapeutic agent for conditions such as Alzheimer's disease and Parkinson's disease. However, its clinical use is limited due to its potential side effects, such as seizures and respiratory depression. Ongoing research focuses on developing safer and more selective derivatives of dihydro-beta-erythroidine for therapeutic applications.'

Dihydro-beta-Erythroidine: Dihydro analog of beta-erythroidine, which is isolated from the seeds and other plant parts of Erythrina sp. Leguminosae. It is an alkaloid with curarimimetic properties. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

dihydro-beta-erythroidine : An organic heterotetracyclic compound resulting from the partial hydrogenation of the 1,3-diene moiety of beta-erythroidine to give the corresponding 2-ene. [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]

FloraRankFlora DefinitionFamilyFamily Definition
ErythrinagenusA genus of leguminous shrubs or trees, mainly tropical, yielding useful compounds such as ALKALOIDS and PLANT LECTINS.[MeSH]FabaceaeThe large family of plants characterized by pods. Some are edible and some cause LATHYRISM or FAVISM and other forms of poisoning. Other species yield useful materials like gums from ACACIA and various LECTINS like PHYTOHEMAGGLUTININS from PHASEOLUS. Many of them harbor NITROGEN FIXATION bacteria on their roots. Many but not all species of beans belong to this family.[MeSH]

Cross-References

ID SourceID
PubMed CID31762
CHEMBL ID293950
CHEBI ID34705
SCHEMBL ID317486
MeSH IDM0006390

Synonyms (44)

Synonym
1328-90-1
beta-erythroidine, dihydro-
erythroidine, beta, dihydro-
16(15h)-oxaerythrinan-15-one, 1,6-didehydro-14,17-dihydro-3-methoxy-, (3beta)-
brn 0036193
b-idroeritroidina [italian]
nsc 9965
16(5h)-oxaerythrinan-15-one, 1,6-didehydro-14,17-dihydro-3-methoxy-, (3-beta)-
23255-54-1
nsc-9965
LOPAC0_000468
dihydro-beta-erythroidine
NCGC00161401-03
NCGC00161401-01
NCGC00161401-02
NCGC00185993-01
(12s,13as)-12-methoxy-1,4,5,6,9,11,12,13-octahydro-8h-pyrano[4'',3'':3,4]pyrido[2,1-i]indol-2-one
bdbm50143313
dhbetae
chebi:34705 ,
CHEMBL293950 ,
dhbe
CCG-204560
(4bs,6s)-6-methoxy-1,4,6,7,9,10,12,13-octahydro-3h,5h-pyrano[4',3':3,4]pyrido[2,1-i]indol-3-one
b-idroeritroidina
rbn56w7u63 ,
4-27-00-03544 (beilstein handbook reference)
unii-rbn56w7u63
bdbm50446501
(1s,16s)-16-methoxy-5-oxa-10-azatetracyclo[8.7.0.0^{1,13}.0^{2,7}]heptadeca-2(7),13-dien-4-one
gtpl4006
1h,12h-benzo(i)pyrano(3,4-g)indolizin-12-one, 2,3,5,6,8,9,10,13-octahydro-2-methoxy-, (2s,13bs)-
dihydro-.beta.-erythroidine
dihydro-.beta.-erythroidine [mi]
2,7-dihydro-.beta.-erythroidine
SCHEMBL317486
3beta-methoxy-14,17-dihydro-16-oxa-erythrin-1(6)-en-15-one
(2s,13bs)-2-methoxy-2,3,5,6,8,9,10,13-octahydro-1h,12h-benzo[i]pyrano[3,4-g]indolizin-12-one
Q27077042
SDCCGSBI-0050453.P002
(1s,16s)-16-methoxy-5-oxa-10-azatetracyclo[8.7.0.01,13.02,7]heptadeca-2(7),13-dien-4-one
dihydro-|a-erythroidine
CS-0568613
HY-N10497

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" In addition to the stimulatory effects of both ethanol and nicotine on the mesolimbic reward pathway, nicotine's ability to counteract some of the adverse effects of ethanol (e."( Protective effects of nicotine on ethanol-induced toxicity in cultured cerebellar granule cells.
Al-Namaeh, M; Manaye, KF; Taylor, RE; Tizabi, Y, 2003
)
0.32

Dosage Studied

ExcerptRelevanceReference
" We and others have previously shown that substitution of phenylalanine for tyrosine at position 198 of the alpha subunit (alpha Y198F) leads to a rightward shift in the dose-response curve for acetylcholine-elicited currents."( Selective enhancement of the interaction of curare with the nicotinic acetylcholine receptor.
Aylwin, ML; Filatov, GN; White, MM, 1993
)
0.29
" The nicotine discrimination was acquired successfully and nicotine yielded a steep dose-response curve."( Antagonism of the discriminative and aversive stimulus properties of nicotine in C57BL/6J mice.
Gommans, J; Shoaib, M; Stolerman, IP, 2000
)
0.31
" DMPX (10 microM) caused a leftward shift of the inhibitory dose-response curves for d-tubocurarine (0."( Endogenous adenosine prevents post-tetanic release facilitation mediated by alpha3beta2 nicotinic autoreceptors.
Correia-de-Sá, P; Faria, M; Timóteo, MA, 2003
)
0.32
" Nefiracetam potentiated alpha4beta2-like ACh- and NMDA-induced currents at nanomolar concentrations forming bell-shaped dose-response curves with the maximum potentiation occurring at 1 and 10 nM, respectively."( Unique mechanism of action of Alzheimer's drugs on brain nicotinic acetylcholine receptors and NMDA receptors.
Marszalec, W; Moriguchi, S; Narahashi, T; Yeh, JZ; Zhao, X, 2003
)
0.32
" Dose-response curves for both receptor subtypes indicated that there are at least two different affinity sites for ACh, the fractional contribution of which depended on the ratio of injected RNA."( Rat nicotinic acetylcholine receptor alpha2beta2 channels: comparison of functional properties with alpha4beta2 channels in Xenopus oocytes.
Khiroug, L; Khiroug, SS; Yakel, JL, 2004
)
0.32
" Mecamylamine (1mg/kg) produced parallel rightward shifts in the dose-response curves for nicotine (3."( The effects of nicotine, varenicline, and cytisine on schedule-controlled responding in mice: differences in α4β2 nicotinic receptor activation.
Cunningham, CS; McMahon, LR, 2011
)
0.37
"3 mg/kg) not previously tested on attention improved response accuracy, resulting in an inverted U-shape dose-response function."( Selective nicotinic receptor antagonists: effects on attention and nicotine-induced attentional enhancement.
Hahn, B; Shoaib, M; Stolerman, IP, 2011
)
0.37
" We found that despite the differences in methodological approaches between these technologies, the EC(50) values from the ACh dose-response curves were consistent between all three platforms."( Validation of a high-throughput, automated electrophysiology platform for the screening of nicotinic agonists and antagonists.
Bencherif, M; Benson, LC; Fedorov, NB; Graef, JD; Lippiello, PM; Sidach, SS; Wei, H, 2013
)
0.39
"Low and high doses of NIC, cytisine (CYT), CC4 and CC26 respectively improved and worsened the mean running time, showing an inverted U dose-response function."( Role of neuronal nicotinic acetylcholine receptors (nAChRs) on learning and memory in zebrafish.
Braida, D; Gotti, C; Martucci, R; Ponzoni, L; Sala, M; Sparatore, F, 2014
)
0.4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
nicotinic antagonistAn antagonist at the nicotinic cholinergic receptor.
[role 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]

Drug Classes (3)

ClassDescription
organic heterotetracyclic compound
delta-lactoneA lactone having a six-membered lactone ring.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[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 (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency15.46750.100020.879379.4328AID488773; AID588453
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency22.38720.035520.977089.1251AID504332
[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)
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)IC50 (µMol)74.33330.00300.77706.0000AID1179339; AID1184961; AID379184
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki100.00000.00000.352210.0000AID1184959
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)IC50 (µMol)0.01240.00030.30952.3000AID1179338; AID146641
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki33.65330.00000.12345.5000AID1184956; AID1184957; AID1184958
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)IC50 (µMol)0.03000.00030.32092.3000AID1179338
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki0.48000.00000.10825.5000AID1184956; AID1184957
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)IC50 (µMol)74.33330.00300.88696.0000AID1179339; AID1184961; AID379184
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)Ki100.00000.00000.296310.0000AID1184958; AID1184959
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)IC50 (µMol)0.14700.00110.539010.0000AID746420; AID746424; AID746425
Neuronal acetylcholine receptor subunit beta-2Homo sapiens (human)Ki0.09800.00000.11173.5400AID1127782
Neuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)IC50 (µMol)0.01100.01100.01100.0110AID746420
Neuronal acetylcholine receptor subunit alpha-7Homo sapiens (human)Ki10.50000.00221.742710.0000AID1127781
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)IC50 (µMol)0.14700.00110.491110.0000AID746420; AID746424; AID746425
Neuronal acetylcholine receptor subunit alpha-4Homo sapiens (human)Ki0.09800.00000.11573.5400AID1127782
Neuronal acetylcholine receptor subunit beta-4Mus musculus (house mouse)IC50 (µMol)1.20000.00400.60201.2000AID1184960
Neuronal acetylcholine receptor subunit beta-2Mus musculus (house mouse)IC50 (µMol)1.20000.00400.60201.2000AID1184960
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (72)

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)
signal transductionNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
monoatomic ion transmembrane transportNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
behavioral response to nicotineNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
excitatory postsynaptic potentialNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
acetylcholine receptor signaling pathwayNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
membrane depolarizationNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
response to nicotineNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
synaptic transmission, cholinergicNeuronal acetylcholine receptor subunit alpha-5Homo 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 alpha-5Homo sapiens (human)
ligand-gated monoatomic ion channel activityNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
acetylcholine receptor activityNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
acetylcholine-gated monoatomic cation-selective channel activityNeuronal acetylcholine receptor subunit alpha-5Homo 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 (16)

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 alpha-5Homo sapiens (human)
postsynaptic membraneNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
dopaminergic synapseNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
presynapseNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
acetylcholine-gated channel complexNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
synapseNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
plasma membraneNeuronal acetylcholine receptor subunit alpha-5Homo sapiens (human)
neuron projectionNeuronal acetylcholine receptor subunit alpha-5Homo 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 (37)

Assay IDTitleYearJournalArticle
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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
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.
AID379184Activity at rat alpha3beta4 nicotinic receptor expressed in KXalpha-3-beta-4R2 cells assessed as nicotine-induced 86Rb+ efflux2006Journal of natural products, Oct, Volume: 69, Issue:10
Isolation, structure elucidation, and biological evaluation of 15-amido-3-demethoxy-2alpha,3alpha-methylenedioxyerythroculine, a new alkaloid from Hyperbaena valida.
AID746424Antagonist activity at (alpha4beta2)2alpha4 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
AID1127781Displacement of [3H]cytisine from alpha7 nAChR (unknown origin)2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.
AID1179338Antagonist activity at rat alpha4beta2 nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID1184957Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID1184956Inhibition of rat membrane alpha4beta2 nAChR by [3H]cytisine binding assay2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID1184961Antagonist activity at rat alpha3beta4 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID746420Antagonist activity at (alpha4beta2)2alpha5 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
AID1179339Antagonist activity at rat alpha3beta4 nAChR2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID146641Blockade of Nicotinic acetylcholine receptor alpha4-beta22004Bioorganic & medicinal chemistry letters, Apr-19, Volume: 14, Issue:8
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
AID1184959Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID1184960Antagonist activity at mouse alpha4beta2 nAChR transfected in HEK293 cells by FLIPR membrane potential blue (FMP) assay2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID746425Antagonist activity at (alpha4beta2)2beta2 nAChR (unknown origin) expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced current after 2 mins by two-electrode voltage clamp assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Neonicotinic analogues: selective antagonists for α4β2 nicotinic acetylcholine receptors.
AID1127782Displacement of [3H]cytisine from alpha4/beta2 nAChR (unknown origin)2013Journal of medicinal chemistry, Dec-12, Volume: 56, Issue:23
Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists.
AID1243914Antagonist activity at nAChR in Sprague-Dawley rat striatal slices assessed as inhibition of nicotine-induced [3H]-dopamine release2015European journal of medicinal chemistry, Aug-28, Volume: 101Bifunctional compounds targeting both D2 and non-α7 nACh receptors: design, synthesis and pharmacological characterization.
AID1184958Displacement of [3H]epibatidine from rat alpha4beta4 nAChR transfected in HEK293 cells after 4 hrs by scintillation count analysis2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Synthesis and Pharmacological Evaluation of DHβE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
AID1179340Inhibition of nicotine-induced [3H]dopamine release in rat striatum2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Recent developments in novel antidepressants targeting α4β2-nicotinic acetylcholine receptors.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (381)

TimeframeStudies, This Drug (%)All Drugs %
pre-199043 (11.29)18.7374
1990's57 (14.96)18.2507
2000's152 (39.90)29.6817
2010's113 (29.66)24.3611
2020's16 (4.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.40

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

MetricThis Compound (vs All)
Research Demand Index16.40 (24.57)
Research Supply Index5.96 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.40)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (0.78%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other382 (99.22%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]