DGIdb - AMILORIDE Drug Record

AMILORIDE chembl:CHEMBL945 ApprovedAntineoplastic

Alternate Names:

HYDRO-RIDE
MIDAMOR
AMILORIDE
AMILORID
AMIPRAMIDIN
AMIPRAMIDINE
MIDAMOR®
AMYLORIDE
AMILORIDA
AMILORIDUM
3,5-DIAMINO-N-CARBAMIMIDOYL-6-CHLOROPYRAZINE-2-CARBOXAMIDE
AMILORIDE HCL
N-AMIDINO-3,5-DIAMINO-6-CHLOROPYRAZINECARBOXAMIDE
chemidplus:2609-46-3
chembl:CHEMBL945
drugbank:00594
rxcui:644
pubchem.compound:16231

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antihypertensive agent
Drug Class	diuretics
Year of Approval	1981
Drug Class	antihypertensive agents

(4 More Sources)

Publications:

Sugiura et al., 2005, Acid-sensing properties in rat gastric sensory neurons from normal and ulcerated stomach., J. Neurosci.
Jones et al., 2004, Acid-induced pain and its modulation in humans., J. Neurosci.
Petruska et al., 2002, Chemical responsiveness and histochemical phenotype of electrophysiologically classified cells of the adult rat dorsal root ganglion., Neuroscience
Xiong et al., 2006, Ca2+ -permeable acid-sensing ion channels and ischemic brain injury., J. Membr. Biol.
Wang et al., 2006, Calcium-permeable acid-sensing ion channel is a molecular target of the neurotoxic metal ion lead., J. Biol. Chem.
Kelly et al., 2003, Characterization of an amiloride binding region in the alpha-subunit of ENaC., Am. J. Physiol. Renal Physiol.
Otulakowski et al., 2007, Steroid and oxygen effects on eIF4F complex, mTOR, and ENaC translation in fetal lung epithelia., Am. J. Respir. Cell Mol. Biol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ji et al., 2004, Degenerin sites mediate proton activation of deltabetagamma-epithelial sodium channel., J. Biol. Chem.
Thorn CF et al., 2013, PharmGKB summary: Diuretics pathway, pharmacodynamics., Pharmacogenet Genomics
Yamagata et al., The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cells., Exp. Lung Res.
Ludwig et al., 2004, Pseudohypoaldosteronism type 1 and the genes encoding prostasin, alpha-spectrin, and Nedd4., Int. J. Mol. Med.
Viemann et al., 2001, Evidence for genetic heterogeneity of pseudohypoaldosteronism type 1: identification of a novel mutation in the human mineralocorticoid receptor in one sporadic case and no mutations in two autosomal dominant kindreds., J. Clin. Endocrinol. Metab.
Iwai et al., 2001, Association of sodium channel gamma-subunit promoter variant with blood pressure., Hypertension
Akçay et al., Pseudohypoaldosteronism type 1 and respiratory distress syndrome., J. Pediatr. Endocrinol. Metab.
Ugawa et al., 2003, Amiloride-insensitive currents of the acid-sensing ion channel-2a (ASIC2a)/ASIC2b heteromeric sour-taste receptor channel., J. Neurosci.
Ugawa, 2003, Identification of sour-taste receptor genes., Anat Sci Int
Berdiev et al., 2003, Acid-sensing ion channels in malignant gliomas., J. Biol. Chem.
Peng et al., 2004, Acid-sensing ion channel 2 contributes a major component to acid-evoked excitatory responses in spiral ganglion neurons and plays a role in noise susceptibility of mice., J. Neurosci.
Vila-Carriles et al., 2006, Surface expression of ASIC2 inhibits the amiloride-sensitive current and migration of glioma cells., J. Biol. Chem.
Yamamura et al., 2005, Evans blue is a specific antagonist of the human epithelial Na+ channel delta-subunit., J. Pharmacol. Exp. Ther.
Yamamura et al., 2005, Icilin activates the delta-subunit of the human epithelial Na+ channel., Mol. Pharmacol.
Ji et al., 2004, The role of Pre-H2 domains of alpha- and delta-epithelial Na+ channels in ion permeation, conductance, and amiloride sensitivity., J. Biol. Chem.
Ji et al., 2006, Delta-subunit confers novel biophysical features to alpha beta gamma-human epithelial sodium channel (ENaC) via a physical interaction., J. Biol. Chem.
Yamamura et al., 2004, Protons activate the delta-subunit of the epithelial Na+ channel in humans., J. Biol. Chem.
Brooks et al., 2002, Targeted proteomic profiling of renal Na(+) transporter and channel abundances in angiotensin II type 1a receptor knockout mice., Hypertension
Lebowitz et al., 2003, Effect of altered Na+ entry on expression of apical and basolateral transport proteins in A6 epithelia., Am. J. Physiol. Renal Physiol.
Planès et al., 2005, In vitro and in vivo regulation of transepithelial lung alveolar sodium transport by serine proteases., Am. J. Physiol. Lung Cell Mol. Physiol.
Kamide et al., 2004, Six missense mutations of the epithelial sodium channel beta and gamma subunits in Japanese hypertensives., Hypertens. Res.

AMILORIDE SCNN1D

Interaction Score: 14.88

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
16107516 16033954 14660613 16423824 14726523

Sources:
TdgClinicalTrial TEND
AMILORIDE SCNN1G

Interaction Score: 9.57

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
12396248 15547682 11344206 11463765 12503866 23788015

Sources:
TdgClinicalTrial TEND PharmGKB
AMILORIDE SCNN1A

Interaction Score: 8.51

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
12928313 17556672 11752352 15084585 23788015

Sources:
TdgClinicalTrial TEND PharmGKB
AMILORIDE SCNN1B

Interaction Score: 6.38

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
23788015 11882592 12746257 12396248 15681398 15198480

Sources:
TdgClinicalTrial TEND PharmGKB
AMILORIDE ASIC1

Interaction Score: 5.95

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction ASIC1a

Endogenous Drug? False

PMIDs:
15758172 15574747 12401318 16685601 16319075

Sources:
GuideToPharmacology TTD
AMILORIDE ASIC2

Interaction Score: 5.1

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
12736332 14686475 12584187 15537887 16704974

Sources:
GuideToPharmacology
AMILORIDE TRPC7

Interaction Score: 4.25

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMILORIDE SLC9A5

Interaction Score: 4.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMILORIDE CYP4A11

Interaction Score: 2.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
AMILORIDE TRPV2

Interaction Score: 2.13

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMILORIDE PKD2L1

Interaction Score: 1.42

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
AMILORIDE KCNJ5

Interaction Score: 1.42

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Na-Ca chanel blocker

Alteration KCNJ5:L168R

PMIDs:
None found

Sources:
CGI
AMILORIDE ASIC3

Interaction Score: 0.53

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Details of Interaction transient component only - sustained component enhanced by 200μM amiloride at pH 4

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
AMILORIDE HSD17B10

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AMILORIDE EHMT2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

TEND: AMILORIDE
- Version: 01-August-2011
Alternate Names:

AMILORIDE Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1981

Drug Class diuretics

Publications:
TdgClinicalTrial: AMILORIDE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antihypertensive agent

Drug Class Small Molecule

FDA Approval approved

Publications:
PharmGKB: amiloride
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Thorn CF et al., 2013, PharmGKB summary: Diuretics pathway, pharmacodynamics., Pharmacogenet Genomics
DTC: AMILORIDE
- Version: 02-September-2020
Alternate Names:

CHEMBL945 ChEMBL Drug ID

Drug Info:

Publications:
TTD: Amiloride
- Version: 2020.06.01
Alternate Names:

D0I0RJ TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 135649936
- Version: 29-September-2020
Alternate Names:

AMILORIDE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL945
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
CGI: Amiloride
- Version: 27-September-2017
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	None
Details of Interaction	ASIC1a
Endogenous Drug?	False

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	False

Trial Name	HTI-101
Novel drug target	Established target

blocker (inhibitory)
inhibitor (inhibitory)

Trial Name	HTI-101
Novel drug target	Established target

blocker (inhibitory)
inhibitor (inhibitory)

AMILORIDE Drug Record

AMILORIDE chembl:CHEMBL945 ApprovedAntineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name HTI-101 Novel drug target Established target

PMIDs: 16107516 16033954 14660613 16423824 14726523

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name HTI-101 Novel drug target Established target

PMIDs: 12396248 15547682 11344206 11463765 12503866 23788015

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name HTI-101 Novel drug target Established target

PMIDs: 12928313 17556672 11752352 15084585 23788015

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Trial Name HTI-101 Novel drug target Established target

PMIDs: 23788015 11882592 12746257 12396248 15681398 15198480

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand None Details of Interaction ASIC1a Endogenous Drug? False

PMIDs: 15758172 15574747 12401318 16685601 16319075

Sources: GuideToPharmacology TTD

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False

PMIDs: 12736332 14686475 12584187 15537887 16704974

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Drug family Na-Ca chanel blocker Alteration KCNJ5:L168R

PMIDs: None found

Sources: CGI

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Endogenous Drug? False Details of Interaction transient component only - sustained component enhanced by 200&mu;M amiloride at pH 4 Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: AMILORIDE

Alternate Names: AMILORIDE Primary Drug Name

Drug Info: Drug Class antihypertensive agents Year of Approval 1981 Drug Class diuretics

Publications:

TdgClinicalTrial: AMILORIDE

Alternate Names:

Drug Info: Drug Indications antihypertensive agent Drug Class Small Molecule FDA Approval approved

Publications:

PharmGKB: amiloride

Alternate Names:

Drug Info:

Publications: Thorn CF et al., 2013, PharmGKB summary: Diuretics pathway, pharmacodynamics., Pharmacogenet Genomics

DTC: AMILORIDE

Alternate Names: CHEMBL945 ChEMBL Drug ID

Drug Info:

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
16107516 16033954 14660613 16423824 14726523

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
12396248 15547682 11344206 11463765 12503866 23788015

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
12928313 17556672 11752352 15084585 23788015

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name HTI-101

Novel drug target Established target

PMIDs:
23788015 11882592 12746257 12396248 15681398 15198480

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction ASIC1a

Endogenous Drug? False

PMIDs:
15758172 15574747 12401318 16685601 16319075

Sources:
GuideToPharmacology TTD

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
12736332 14686475 12584187 15537887 16704974

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family Na-Ca chanel blocker

Alteration KCNJ5:L168R

PMIDs:
None found

Sources:
CGI

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Endogenous Drug? False

Details of Interaction transient component only - sustained component enhanced by 200μM amiloride at pH 4

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

AMILORIDE Primary Drug Name

Drug Info:

Drug Class antihypertensive agents

Year of Approval 1981

Drug Class diuretics

Drug Info:

Drug Indications antihypertensive agent

Drug Class Small Molecule

FDA Approval approved

Publications:

Thorn CF et al., 2013, PharmGKB summary: Diuretics pathway, pharmacodynamics., Pharmacogenet Genomics

Alternate Names:

CHEMBL945 ChEMBL Drug ID

Alternate Names:

D0I0RJ TTD Drug ID

Alternate Names:

AMILORIDE GuideToPharmacology Ligand Name