Page last updated: 2024-12-04

ethylisopropylamiloride

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Description

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

ethylisopropylamiloride : A member of the class of pyrazines that is amiloride in which the amino substitutent of the pyrazine ring that is adjacent to the chloro substituent has been substituted by an ethyl group and by an isopropyl group. [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]

Cross-References

ID SourceID
PubMed CID1795
CHEMBL ID517986
CHEBI ID136538
SCHEMBL ID9852524
SCHEMBL ID23663987
MeSH IDM0118534

Synonyms (69)

Synonym
LOPAC0_000045
2-pyrazinecarboxamide, 3-amino-n-(aminoiminomethyl)-6-chloro-5-[ethyl(1-methylethyl)amino]-
3-amino-n-carbamimidoyl-6-chloro-5-[ethyl(isopropyl)amino]pyrazine-2-carboxamide
EU-0100045
5-(n-ethyl-n-isopropyl)amiloride
NCGC00015047-01
lopac-a-3085
MLS000860017
smr000326875
3-amino-n-(aminoiminomethyl)-6-chloro-5-(ethyl(1-methylethyl)amino)pyrazinecarboxamide
n-amidino-3-amino-5-ethylisopropylamino-6-chloropyrazine carboxamide
ethylisopropylamiloride
pyrazinecarboxamide, 3-amino-n-(aminoiminomethyl)-6-chloro-5-(ethyl(1-methylethyl)amino)-
5-(ethylisopropyl)amiloride
eipa
ethyl isopropyl amiloride
NCGC00093559-02
NCGC00093559-01
1154-25-2
NCGC00015047-02
CHEBI:136538
A 3085
NCGC00015047-04
SCHEMBL9852524
5''-(n-ethyl-n-isopropyl)amiloride
bdbm50270005
cid_1795
CHEMBL517986 ,
3-amino-6-chloro-n-(diaminomethylidene)-5-[ethyl(propan-2-yl)amino]pyrazine-2-carboxamide
HMS3260I11
CCG-204141
HMS2235B09
NCGC00015047-03
NCGC00015047-05
vw50ce070t ,
unii-vw50ce070t
5-(n-ethyl-n-isopropyl)-amiloride
FT-0602002
LP00045
REGID_FOR_CID_1795
l-593754
mh-12-43
2-pyrazinecarboxamide, 3-amino-n-(aminoiminomethyl)-6-chloro-5-(ethyl(1-methylethyl)amino)-
mh 12-43
3-amino-n-(aminoiminomethyl)-6-chloro-5-[ethyl(1-methylethyl)amino]-2-pyrazinecarboxamide
gtpl4186
tox21_500045
NCGC00260730-01
AKOS024281351
ethylisopropyl amiloride
HY-101840
CS-7935
mfcd00151710
l593754;mh 12-43
DTXSID80151084
J-003288
AKOS030241586
SR-01000075673-1
sr-01000075673
3-amino-n-carbamimidoyl-6-chloro-5-(ethyl(isopropyl)amino)pyrazine-2-carboxamide
l593754;mh 12-43;ethylisopropylamiloride
Q27077241
AS-30503
SDCCGSBI-0050034.P002
NCGC00015047-06
HMS3740E09
l593754
mh 12-43l593754
SCHEMBL23663987

Research Excerpts

Overview

Ethylisopropylamiloride (EIPA) is a potent inhibitor of Na(+)-H+ exchange in many tissues. It is frequently used to study cellular regulation of pH. The electrophysiologic effects of EIPA on cardiac cells have not been studied previously.

ExcerptReferenceRelevance
"Ethylisopropylamiloride (EIPA) is a potent inhibitor of Na(+)-H+ exchange in many tissues and is frequently used to study cellular regulation of pH, but the electrophysiologic effects of EIPA on cardiac cells have not been studied previously. "( Use-dependent block of atrial sodium current by ethylisopropylamiloride.
Gold, MR; Strichartz, GR, 1991
)
1.98

Toxicity

ExcerptReferenceRelevance
" Weak acids that are normal cellular metabolites are not toxic in vivo, but weak acids carrying cytotoxic groups offer the potential for selective uptake and toxicity under the conditions of low pHe that exist in many solid tumours."( Selective cellular acidification and toxicity of weak organic acids in an acidic microenvironment.
Dobrowsky, E; Karuri, AR; Tannock, IF, 1993
)
0.29
"Cultured cerebellar granule neurons (CGNs) are resistant to the toxic effect of ZnCl2 (0."( Acidosis and 5-(N-ethyl-N-isopropyl)amiloride (EIPA) Attenuate Zinc/Kainate Toxicity in Cultured Cerebellar Granule Neurons.
Amelkina, GA; Genrikhs, EE; Isaev, NK; Ivashkin, EG; Khaspekov, LG; Novikova, SV; Stelmashook, EV, 2015
)
0.42

Bioavailability

ExcerptReferenceRelevance
"An understanding of drug delivery system transport across epithelial cell monolayer is very important for improving the absorption and bioavailability of the drug payload."( Transport pathways of solid lipid nanoparticles across Madin-Darby canine kidney epithelial cell monolayer.
Chai, GH; Du, YZ; Hu, FQ; Sun, J; You, J; Yuan, H, 2014
)
0.4

Dosage Studied

ExcerptRelevanceReference
" Dose-response curves for EIPA indicated that the increased Na(+)-H+ antiport activity in PKE20 vesicles was due to an increased activity of the relatively amiloride-resistant form of the Na(+)-H+ antiporter with little or no change in the amiloride-sensitive form."( Increased Na(+)-H+ antiporter activity in apical membrane vesicles from mutant LLC-PK1 cells.
Adelberg, EA; Aronson, PS; Haggerty, JG; Reilly, RF; Slayman, CW, 1991
)
0.28
" This study was designed to examine the dose-response nature and time-dependent effect of 4 beta-phorbol-12-myristate-13-acetate (PMA) on the rates of bicarbonate absorption (JHCO3) and fluid absorption (Jv) in the proximal convoluted tubule (PCT) of rat kidney."( Time- and dose-dependent effects of protein kinase C on proximal bicarbonate transport.
Chan, YL; Wang, T, 1990
)
0.28
" In contrast to the discrepancy in Tyrphostin dose-response curves, titration curves for 5-(N-ethyl-n-isopropyl)amiloride and 5-(N,N-hexamethylene)amiloride are comparable in SF- or GM-CSF-stimulated cells."( Product of the steel locus suppresses apoptosis in hemopoietic cells. Comparison with pathways activated by granulocyte macrophage colony-stimulating factor.
Cáceres-Cortés, J; Dumouchel, J; Haddad, P; Hoang, T; Rajotte, D, 1994
)
0.29
" However, inhibition reached the maximal level only at 50 mM sodium, and typical sigmoidal dose-response curves were obtained only in the presence of 118 mM sodium."( Regulation of mu-opioid receptor in neural cells by extracellular sodium.
Medzihradsky, F; Yabaluri, N, 1997
)
0.3
" Stimulation by stripped serum or oestradiol resulted in parallel increases of proliferation and pS2 release in both time course and dose-response experiments."( Association of pS2 (TFF1) release with breast tumour proliferative rate: in vitro and in vivo studies.
Casavola, V; Correale, M; Mangia, A; Paradiso, A; Reshkin, SJ; Tedone, T,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anti-arrhythmia drugA drug used for the treatment or prevention of cardiac arrhythmias. Anti-arrhythmia drugs may affect the polarisation-repolarisation phase of the action potential, its excitability or refractoriness, or impulse conduction or membrane responsiveness within cardiac fibres.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
sodium channel blockerAn agent that inhibits sodium influx through cell membranes.
[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 (6)

ClassDescription
guanidinesAny organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
aromatic amineAn amino compound in which the amino group is linked directly to an aromatic system.
organochlorine compoundAn organochlorine compound is a compound containing at least one carbon-chlorine bond.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
pyrazines
monocarboxylic acid amideA carboxamide derived from a monocarboxylic acid.
[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 (40)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency35.48135.623417.292931.6228AID2323
acid sphingomyelinaseHomo sapiens (human)Potency25.118914.125424.061339.8107AID504937
glp-1 receptor, partialHomo sapiens (human)Potency10.00000.01846.806014.1254AID624417
thioredoxin reductaseRattus norvegicus (Norway rat)Potency26.67950.100020.879379.4328AID588453
USP1 protein, partialHomo sapiens (human)Potency177.82800.031637.5844354.8130AID743255
TDP1 proteinHomo sapiens (human)Potency13.95200.000811.382244.6684AID686978; AID686979
ThrombopoietinHomo sapiens (human)Potency10.00000.02517.304831.6228AID917; AID918
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency10.00000.707912.194339.8107AID720542
thyroid stimulating hormone receptorHomo sapiens (human)Potency19.95260.001318.074339.8107AID926
regulator of G-protein signaling 4Homo sapiens (human)Potency9.46620.531815.435837.6858AID504845
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency9.43920.001530.607315,848.9004AID1224819; AID1224820; AID1224821
arylsulfatase AHomo sapiens (human)Potency16.94411.069113.955137.9330AID720538
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency67.455523.934123.934123.9341AID1967
D(1A) dopamine receptorHomo sapiens (human)Potency31.62280.02245.944922.3872AID488983
chromobox protein homolog 1Homo sapiens (human)Potency50.11870.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency35.48130.01789.637444.6684AID588834
flap endonuclease 1Homo sapiens (human)Potency37.68580.133725.412989.1251AID588795
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency100.00000.050127.073689.1251AID588590
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
plasminogen precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency8.91250.15855.287912.5893AID540303
gemininHomo sapiens (human)Potency11.38370.004611.374133.4983AID463097; AID624296; AID624297
M-phase phosphoprotein 8Homo sapiens (human)Potency70.79460.177824.735279.4328AID488949
muscleblind-like protein 1 isoform 1Homo sapiens (human)Potency8.91250.00419.962528.1838AID2675
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency7.94330.00106.000935.4813AID943
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency15.84890.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.84890.00638.235039.8107AID881
[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)
Sodium/hydrogen exchanger 1Homo sapiens (human)IC50 (µMol)0.80000.00500.56013.5000AID358119
Sodium/hydrogen exchanger 1Oryctolagus cuniculus (rabbit)IC50 (µMol)0.02000.00800.01760.0260AID1411093
Sodium/hydrogen exchanger 1Oryctolagus cuniculus (rabbit)Ki0.02000.02000.02000.0200AID1341118; AID1341846
Sodium/hydrogen exchanger 1Rattus norvegicus (Norway rat)IC50 (µMol)0.01000.01000.64613.9000AID1411092
Sodium/hydrogen exchanger 1Rattus norvegicus (Norway rat)Ki0.01000.01000.26151.0000AID1341114; AID1341845
Sodium/hydrogen exchanger 3Rattus norvegicus (Norway rat)IC50 (µMol)2.40000.00930.60862.4000AID1411098
Sodium/hydrogen exchanger 3Rattus norvegicus (Norway rat)Ki2.40002.40002.40002.4000AID1341116; AID1341851
Sodium/hydrogen exchanger 2Rattus norvegicus (Norway rat)Ki0.08000.08000.16500.2500AID1341119; AID1341848
Sodium/hydrogen exchanger 2Oryctolagus cuniculus (rabbit)IC50 (µMol)0.50000.00800.26131.0000AID1411096
Sodium/hydrogen exchanger 2Oryctolagus cuniculus (rabbit)Ki0.50000.50000.75001.0000AID1341115; AID1341849
Sodium/hydrogen exchanger 5Homo sapiens (human)IC50 (µMol)0.42000.42000.42000.4200AID1411100
Sodium/hydrogen exchanger 5Homo sapiens (human)Ki0.42000.37000.39500.4200AID1341117; AID1341852
Sodium/hydrogen exchangerAmphiuma tridactylum (three-toed salamander)IC50 (µMol)8.70008.70008.70008.7000AID358118
[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)
delta-type opioid receptorHomo sapiens (human)EC50 (µMol)36.82050.13203.58649.5690AID588407; AID588411
mu-type opioid receptor isoform MOR-1Homo sapiens (human)EC50 (µMol)51.01950.13203.30049.5690AID588407; AID588435
[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)
PAX8Homo sapiens (human)AC5020.94000.04885.435469.1700AID687027
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (62)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
monoatomic ion transportSodium/hydrogen exchanger 1Homo sapiens (human)
intracellular sodium ion homeostasisSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of pHSodium/hydrogen exchanger 1Homo sapiens (human)
response to acidic pHSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of cardiac muscle hypertrophySodium/hydrogen exchanger 1Homo sapiens (human)
regulation of cardiac muscle contraction by calcium ion signalingSodium/hydrogen exchanger 1Homo sapiens (human)
cell migrationSodium/hydrogen exchanger 1Homo sapiens (human)
maintenance of cell polaritySodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of cell growthSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to insulin stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilitySodium/hydrogen exchanger 1Homo sapiens (human)
response to muscle stretchSodium/hydrogen exchanger 1Homo sapiens (human)
sodium ion export across plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of apoptotic processSodium/hydrogen exchanger 1Homo sapiens (human)
negative regulation of apoptotic processSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of action potentialSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IISodium/hydrogen exchanger 1Homo sapiens (human)
stem cell differentiationSodium/hydrogen exchanger 1Homo sapiens (human)
protein complex oligomerizationSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of intracellular pHSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of stress fiber assemblySodium/hydrogen exchanger 1Homo sapiens (human)
regulation of focal adhesion assemblySodium/hydrogen exchanger 1Homo sapiens (human)
cardiac muscle cell differentiationSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to coldSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of calcineurin-NFAT signaling cascadeSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to antibioticSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to electrical stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to mechanical stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to organic cyclic compoundSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to hypoxiaSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to acidic pHSodium/hydrogen exchanger 1Homo sapiens (human)
cellular response to epinephrine stimulusSodium/hydrogen exchanger 1Homo sapiens (human)
cardiac muscle cell contractionSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of cardiac muscle cell membrane potentialSodium/hydrogen exchanger 1Homo sapiens (human)
regulation of the force of heart contraction by cardiac conductionSodium/hydrogen exchanger 1Homo sapiens (human)
sodium ion import across plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of the force of heart contractionSodium/hydrogen exchanger 1Homo sapiens (human)
proton transmembrane transportSodium/hydrogen exchanger 1Homo sapiens (human)
positive regulation of calcium:sodium antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
potassium ion transmembrane transportSodium/hydrogen exchanger 1Homo sapiens (human)
monoatomic ion transportSodium/hydrogen exchanger 5Homo sapiens (human)
sodium ion transmembrane transportSodium/hydrogen exchanger 5Homo sapiens (human)
regulation of intracellular pHSodium/hydrogen exchanger 5Homo sapiens (human)
proton transmembrane transportSodium/hydrogen exchanger 5Homo sapiens (human)
potassium ion transmembrane transportSodium/hydrogen exchanger 5Homo sapiens (human)
sodium ion import across plasma membraneSodium/hydrogen exchanger 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (20)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
calmodulin bindingSodium/hydrogen exchanger 1Homo sapiens (human)
phospholipid bindingSodium/hydrogen exchanger 1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingSodium/hydrogen exchanger 1Homo sapiens (human)
sodium:proton antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
protein phosphatase 2B bindingSodium/hydrogen exchanger 1Homo sapiens (human)
protein-macromolecule adaptor activitySodium/hydrogen exchanger 1Homo sapiens (human)
identical protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
calcium-dependent protein bindingSodium/hydrogen exchanger 1Homo sapiens (human)
molecular adaptor activitySodium/hydrogen exchanger 1Homo sapiens (human)
sodium:proton antiporter activity involved in regulation of cardiac muscle cell membrane potentialSodium/hydrogen exchanger 1Homo sapiens (human)
potassium:proton antiporter activitySodium/hydrogen exchanger 1Homo sapiens (human)
protein bindingSodium/hydrogen exchanger 5Homo sapiens (human)
sodium:proton antiporter activitySodium/hydrogen exchanger 5Homo sapiens (human)
arrestin family protein bindingSodium/hydrogen exchanger 5Homo sapiens (human)
potassium:proton antiporter activitySodium/hydrogen exchanger 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
nucleoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
cytoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
mitochondrionSodium/hydrogen exchanger 1Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
focal adhesionSodium/hydrogen exchanger 1Homo sapiens (human)
cell surfaceSodium/hydrogen exchanger 1Homo sapiens (human)
intercalated discSodium/hydrogen exchanger 1Homo sapiens (human)
membraneSodium/hydrogen exchanger 1Homo sapiens (human)
basolateral plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
apical plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
lamellipodiumSodium/hydrogen exchanger 1Homo sapiens (human)
T-tubuleSodium/hydrogen exchanger 1Homo sapiens (human)
membrane raftSodium/hydrogen exchanger 1Homo sapiens (human)
perinuclear region of cytoplasmSodium/hydrogen exchanger 1Homo sapiens (human)
extracellular exosomeSodium/hydrogen exchanger 1Homo sapiens (human)
cation-transporting ATPase complexSodium/hydrogen exchanger 1Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 1Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 5Homo sapiens (human)
focal adhesionSodium/hydrogen exchanger 5Homo sapiens (human)
membraneSodium/hydrogen exchanger 5Homo sapiens (human)
dendritic spine membraneSodium/hydrogen exchanger 5Homo sapiens (human)
neuron spineSodium/hydrogen exchanger 5Homo sapiens (human)
synapseSodium/hydrogen exchanger 5Homo sapiens (human)
postsynaptic membraneSodium/hydrogen exchanger 5Homo sapiens (human)
recycling endosome membraneSodium/hydrogen exchanger 5Homo sapiens (human)
plasma membraneSodium/hydrogen exchanger 5Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (52)

Assay IDTitleYearJournalArticle
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
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.
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.
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.
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.
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.
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.
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.
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
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.
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.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
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.
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.
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.
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.
AID524790Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524795Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524791Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID521220Inhibition of neurosphere proliferation of mouse neural precursor cells by MTT assay2007Nature chemical biology, May, Volume: 3, Issue:5
Chemical genetics reveals a complex functional ground state of neural stem cells.
AID358310Inhibition of Pleuronectes americanus NHE1 mutant containing TM10-12 domain of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358115Inhibition of osmotic cell shrinkage-induced NHE1 activity in Amphiuma tridactylum RBC2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358314Inhibition of Pleuronectes americanus NHE1 C-terminal mutant with replacement of residues C-terminal to 489 position with corresponding residues of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammon2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID576507Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Discovery of potent small-molecule inhibitors of multidrug-resistant Plasmodium falciparum using a novel miniaturized high-throughput luciferase-based assay.
AID358119Inhibition of human wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358313Inhibition of Pleuronectes americanus NHE1 TM4 mutant containing TFFLF sequence of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358312Inhibition of Pleuronectes americanus NHE1 TM4 mutant containing VFFLF sequence of human expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID524794Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID524792Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID358311Inhibition of Amphiuma tridactylum NHE1 mutant containing TM10-12 domain of Pleuronectes americanus expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358116Inhibition of osmotic cell shrinkage-induced NHE1 activity in Pleuronectes americanus RBC upto 100 uM2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358121Inhibition of Pleuronectes americanus NHE1 C-terminal mutant containing TM10 domain of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID358118Inhibition of Amphiuma tridactylum wild type NHE1 expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
AID524796Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay2009Nature chemical biology, Oct, Volume: 5, Issue:10
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
AID358120Inhibition of Pleuronectes americanus NHE1 C-terminal mutant containing TM7 domain of Amphiuma tridactylum expressed in chinese hamster AP1 cells assessed as intracellular pHi recovery by ammonium chloride prepulse protocol2007The Journal of biological chemistry, Jul-06, Volume: 282, Issue:27
NHE1 inhibition by amiloride- and benzoylguanidine-type compounds. Inhibitor binding loci deduced from chimeras of NHE1 homologues with endogenous differences in inhibitor sensitivity.
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.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1346049Human alpha2A-adrenoceptor (Adrenoceptors)1992Molecular pharmacology, Aug, Volume: 42, Issue:2
Novel amiloride analog allosterically modulates the alpha 2-adrenergic receptor but does not inhibit Na+/H+ exchange.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (587)

TimeframeStudies, This Drug (%)All Drugs %
pre-199049 (8.35)18.7374
1990's277 (47.19)18.2507
2000's168 (28.62)29.6817
2010's84 (14.31)24.3611
2020's9 (1.53)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 16.26

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 Index16.26 (24.57)
Research Supply Index6.40 (2.92)
Research Growth Index5.03 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (16.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (0.50%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other596 (99.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]