DT-Web: DB00594

Identification

Name

Amiloride

Accession Number

DB00594 (APRD00790, EXPT00514)

Type

small molecule

Description

A pyrazine compound inhibiting sodium reabsorption through sodium channels in renal epithelial cells. This inhibition creates a negative potential in the luminal membranes of principal cells, located in the distal convoluted tubule and collecting duct. Negative potential reduces secretion of potassium and hydrogen ions. Amiloride is used in conjunction with diuretics to spare potassium loss. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p705)

Structure

MOL SDF PDB SMILES InChI

Categories ^(*)

Molecular Weight

229.627

Groups

approved

Monoisotopic Weight

229.04788562

Pharmacology

Indication

For use as adjunctive treatment with thiazide diuretics or other kaliuretic-diuretic agents in congestive heart failure or hypertension.

Mechanism of action

Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.

Absorption

Readily absorbed following oral administration.

Protein binding

Not Available

Biotransformation

Amiloride is not metabolized by the liver but is excreted unchanged by the kidneys.

Route of elimination

Amiloride HCl is not metabolized by the liver but is excreted unchanged by the kidneys. About 50 percent of a 20 mg dose of amiloride HCl is excreted in the urine and 40 percent in the stool within 72 hours.

Toxicity

No data are available in regard to overdosage in humans. The oral LD₅₀ of amiloride hydrochloride (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain. The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance.

Affected organisms

Humans and other mammals

Interactions

Drug Interactions

Drug	Mechanism of interaction
Benazepril	Increased risk of hyperkalemia
Candesartan	Increased risk of hyperkalemia
Captopril	Increased risk of hyperkalemia
Cilazapril	Increased risk of hyperkalemia
Dihydroquinidine barbiturate	Decreases the antiarrhythmic effect of quinidine
Enalapril	Increased risk of hyperkalemia
Eplerenone	Increased risk of hyperkalemia. Monitor serum potassium levels during concomitant threapy.
Eprosartan	Increased risk of hyperkalemia
Forasartan	Increased risk of hyperkalemia
Fosinopril	Increased risk of hyperkalemia
Irbesartan	Increased risk of hyperkalemia
Lisinopril	Increased risk of hyperkalemia
Losartan	Increased risk of hyperkalemia
Moexipril	Increased risk of hyperkalemia
Perindopril	Increased risk of hyperkalemia
Polystyrene sulfonate	Risk of alkalosis in renal impairment
Potassium	Increased risk of hyperkalemia
Quinapril	Increased risk of hyperkalemia
Quinidine	Amiloride may decrease the therapeutic effect of quinidine. Monitor for changes in the therapeutic and adverse effects of quinidine if amiloride if initiated, discontinued or dose changed.
Quinidine barbiturate	Decreases the antiarrhythmic effect of quinidine
Ramipril	Increased risk of hyperkalemia
Saprisartan	Increased risk of hyperkalemia
Spirapril	Increased risk of hyperkalemia
Tasosartan	Increased risk of hyperkalemia
Telmisartan	Telmisartan may increase the hyperkalemic effect of Amiloride. Monitor for increased serum potassium concentrations during concomitant therapy.
Trandolapril	Increased risk of hyperkalemia. Monitor serum potassium levels.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Valsartan	Increased risk of hyperkalemia

Food Interactions

Avoid drastic changes in dietary habit.
Take with food to reduce irritation.
Avoid natural licorice.
Avoid salt substitutes containing potassium.

Amiloride-sensitive sodium channel subunit alpha
Name	Amiloride-sensitive sodium channel subunit alpha
Gene Name	SCNN1A
Pharmacological action	yes
Actions	inhibitor
References	Kelly O, Lin C, Ramkumar M, Saxena NC, Kleyman TR, Eaton DC: Characterization of an amiloride binding region in the alpha-subunit of ENaC. Am J Physiol Renal Physiol. 2003 Dec;285(6):F1279-90. Epub 2003 Aug 19. - Pubmed Ji HL, Benos DJ: Degenerin sites mediate proton activation of deltabetagamma-epithelial sodium channel. J Biol Chem. 2004 Jun 25;279(26):26939-47. Epub 2004 Apr 14. - Pubmed Otulakowski G, Duan W, Gandhi S, O'brodovich H: Steroid and Oxygen Effects on eIF4F Complex, mTOR, and ENaC Translation in Fetal Lung Epithelia. Am J Respir Cell Mol Biol. 2007 Oct;37(4):457-466. Epub 2007 Jun 7. - Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score	1.1336
Amiloride-sensitive sodium channel subunit beta
Name	Amiloride-sensitive sodium channel subunit beta
Gene Name	SCNN1B
Pharmacological action	yes
Actions	inhibitor
References	Lebowitz J, An B, Edinger RS, Zeidel ML, Johnson JP: Effect of altered Na+ entry on expression of apical and basolateral transport proteins in A6 epithelia. Am J Physiol Renal Physiol. 2003 Sep;285(3):F524-31. Epub 2003 May 13. - Pubmed Planes C, Leyvraz C, Uchida T, Angelova MA, Vuagniaux G, Hummler E, Matthay M, Clerici C, Rossier B: In vitro and in vivo regulation of transepithelial lung alveolar sodium transport by serine proteases. Am J Physiol Lung Cell Mol Physiol. 2005 Jun;288(6):L1099-109. Epub 2005 Jan 28. - Pubmed Yamagata T, Yamagata Y, Nishimoto T, Nakanishi M, Nakanishi H, Minakata Y, Mune M, Yukawa S: The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cells. Exp Lung Res. 2002 Oct-Nov;28(7):543-62. - Pubmed Brooks HL, Allred AJ, Beutler KT, Coffman TM, Knepper MA: Targeted proteomic profiling of renal Na(+) transporter and channel abundances in angiotensin II type 1a receptor knockout mice. Hypertension. 2002 Feb;39(2 Pt 2):470-3. - Pubmed Kamide K, Tanaka C, Takiuchi S, Miwa Y, Yoshii M, Horio T, Kawano Y, Miyata T: Six missense mutations of the epithelial sodium channel beta and gamma subunits in Japanese hypertensives. Hypertens Res. 2004 May;27(5):333-8. - Pubmed
DTHybrid score	1.1331
Amiloride-sensitive sodium channel subunit gamma
Name	Amiloride-sensitive sodium channel subunit gamma
Gene Name	SCNN1G
Pharmacological action	yes
Actions	inhibitor
References	Viemann M, Peter M, Lopez-Siguero JP, Simic-Schleicher G, Sippell WG: 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. 2001 May;86(5):2056-9. - Pubmed Iwai N, Baba S, Mannami T, Katsuya T, Higaki J, Ogihara T, Ogata J: Association of sodium channel gamma-subunit promoter variant with blood pressure. Hypertension. 2001 Jul;38(1):86-9. - Pubmed Yamagata T, Yamagata Y, Nishimoto T, Nakanishi M, Nakanishi H, Minakata Y, Mune M, Yukawa S: The impact of phorbol ester on the regulation of amiloride-sensitive epithelial sodium channel in alveolar type ii epithelial cells. Exp Lung Res. 2002 Oct-Nov;28(7):543-62. - Pubmed Akcay A, Yavuz T, Semiz S, Bundak R, Demirdoven M: Pseudohypoaldosteronism type 1 and respiratory distress syndrome. J Pediatr Endocrinol Metab. 2002 Nov-Dec;15(9):1557-61. - Pubmed Ludwig M, Bidlingmaier F, Reissinger A: Pseudohypoaldosteronism type 1 and the genes encoding prostasin, alpha-spectrin, and Nedd4. Int J Mol Med. 2004 Dec;14(6):1101-4. - Pubmed
DTHybrid score	1.1332
Amiloride-sensitive sodium channel subunit delta
Name	Amiloride-sensitive sodium channel subunit delta
Gene Name	SCNN1D
Pharmacological action	yes
Actions	inhibitor
References	Yamamura H, Ugawa S, Ueda T, Nagao M, Shimada S: Protons activate the delta-subunit of the epithelial Na+ channel in humans. J Biol Chem. 2004 Mar 26;279(13):12529-34. Epub 2004 Jan 15. - Pubmed Ji HL, Bishop LR, Anderson SJ, Fuller CM, Benos DJ: The role of Pre-H2 domains of alpha- and delta-epithelial Na+ channels in ion permeation, conductance, and amiloride sensitivity. J Biol Chem. 2004 Feb 27;279(9):8428-40. Epub 2003 Dec 2. - Pubmed Ji HL, Su XF, Kedar S, Li J, Barbry P, Smith PR, Matalon S, Benos DJ: Delta-subunit confers novel biophysical features to alpha beta gamma-human epithelial sodium channel (ENaC) via a physical interaction. J Biol Chem. 2006 Mar 24;281(12):8233-41. Epub 2006 Jan 19. - Pubmed Yamamura H, Ugawa S, Ueda T, Nagao M, Shimada S: Icilin activates the delta-subunit of the human epithelial Na+ channel. Mol Pharmacol. 2005 Oct;68(4):1142-7. Epub 2005 Jul 20. - Pubmed Yamamura H, Ugawa S, Ueda T, Shimada S: Evans blue is a specific antagonist of the human epithelial Na+ channel delta-subunit. J Pharmacol Exp Ther. 2005 Nov;315(2):965-9. Epub 2005 Aug 17. - Pubmed
DTHybrid score	1.133
Amiloride-sensitive amine oxidase [copper-containing]
Name	Amiloride-sensitive amine oxidase [copper-containing]
Gene Name	ABP1
Pharmacological action	unknown
Actions	inhibitor
References	Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. - Pubmed Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. - Pubmed
DTHybrid score	0.7131
Amiloride-sensitive cation channel 1, neuronal
Name	Amiloride-sensitive cation channel 1, neuronal
Gene Name	ACCN1
Pharmacological action	unknown
Actions	inhibitor
References	Berdiev BK, Xia J, McLean LA, Markert JM, Gillespie GY, Mapstone TB, Naren AP, Jovov B, Bubien JK, Ji HL, Fuller CM, Kirk KL, Benos DJ: Acid-sensing ion channels in malignant gliomas. J Biol Chem. 2003 Apr 25;278(17):15023-34. Epub 2003 Feb 12. - Pubmed Ugawa S, Yamamoto T, Ueda T, Ishida Y, Inagaki A, Nishigaki M, Shimada S: Amiloride-insensitive currents of the acid-sensing ion channel-2a (ASIC2a)/ASIC2b heteromeric sour-taste receptor channel. J Neurosci. 2003 May 1;23(9):3616-22. - Pubmed Ugawa S: Identification of sour-taste receptor genes. Anat Sci Int. 2003 Dec;78(4):205-10. - Pubmed Peng BG, Ahmad S, Chen S, Chen P, Price MP, Lin X: 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. 2004 Nov 10;24(45):10167-75. - Pubmed Vila-Carriles WH, Kovacs GG, Jovov B, Zhou ZH, Pahwa AK, Colby G, Esimai O, Gillespie GY, Mapstone TB, Markert JM, Fuller CM, Bubien JK, Benos DJ: Surface expression of ASIC2 inhibits the amiloride-sensitive current and migration of glioma cells. J Biol Chem. 2006 Jul 14;281(28):19220-32. Epub 2006 May 16. - Pubmed
DTHybrid score	0.6612
Amiloride-sensitive cation channel 2, neuronal
Name	Amiloride-sensitive cation channel 2, neuronal
Gene Name	ACCN2
Pharmacological action	unknown
Actions	inhibitor
References	Petruska JC, Napaporn J, Johnson RD, Cooper BY: Chemical responsiveness and histochemical phenotype of electrophysiologically classified cells of the adult rat dorsal root ganglion. Neuroscience. 2002;115(1):15-30. - Pubmed Jones NG, Slater R, Cadiou H, McNaughton P, McMahon SB: Acid-induced pain and its modulation in humans. J Neurosci. 2004 Dec 1;24(48):10974-9. - Pubmed Sugiura T, Dang K, Lamb K, Bielefeldt K, Gebhart GF: Acid-sensing properties in rat gastric sensory neurons from normal and ulcerated stomach. J Neurosci. 2005 Mar 9;25(10):2617-27. - Pubmed Wang W, Duan B, Xu H, Xu L, Xu TL: Calcium-permeable acid-sensing ion channel is a molecular target of the neurotoxic metal ion lead. J Biol Chem. 2006 Feb 3;281(5):2497-505. Epub 2005 Nov 29. - Pubmed Xiong ZG, Chu XP, Simon RP: Ca2+ -permeable acid-sensing ion channels and ischemic brain injury. J Membr Biol. 2006 Jan;209(1):59-68. Epub 2006 Apr 17. - Pubmed
DTHybrid score	0.5344
Sodium/hydrogen exchanger 1
Name	Sodium/hydrogen exchanger 1
Gene Name	SLC9A1
Pharmacological action	unknown
Actions	inhibitor
References	Lee MG, Ahn W, Choi JY, Luo X, Seo JT, Schultheis PJ, Shull GE, Kim KH, Muallem S: Na(+)-dependent transporters mediate HCO(3)(-) salvage across the luminal membrane of the main pancreatic duct. J Clin Invest. 2000 Jun;105(11):1651-8. - Pubmed Konstantinou-Tegou A, Kaloyianni M, Bourikas D, Koliakos G: The effect of leptin on Na(+)-H(+) antiport (NHE 1) activity of obese and normal subjects erythrocytes. Mol Cell Endocrinol. 2001 Oct 25;183(1-2):11-8. - Pubmed Serrani RE, Mujica G, Gioia IA, Corchs JL: Neonatal red blood cells: amiloride-insensitive Na+-H+ transport isoform would express Na+-Li+ exchange. Acta Physiol Pharmacol Bulg. 2000;25(3-4):71-4. - Pubmed Cuthbert AW, Supuran CT, MacVinish LJ: Bicarbonate-dependent chloride secretion in Calu-3 epithelia in response to 7,8-benzoquinoline. J Physiol. 2003 Aug 15;551(Pt 1):79-92. Epub 2003 Jul 18. - Pubmed Furukawa O, Bi LC, Guth PH, Engel E, Hirokawa M, Kaunitz JD: NHE3 inhibition activates duodenal bicarbonate secretion in the rat. Am J Physiol Gastrointest Liver Physiol. 2004 Jan;286(1):G102-9. Epub 2003 Jul 24. - Pubmed
DTHybrid score	1.319
Urokinase-type plasminogen activator
Name	Urokinase-type plasminogen activator
Gene Name	PLAU
Pharmacological action	unknown
Actions	inhibitor
References	Vakili J, Standker L, Detheux M, Vassart G, Forssmann WG, Parmentier M: Urokinase plasminogen activator and plasmin efficiently convert hemofiltrate CC chemokine 1 into its active. J Immunol. 2001 Sep 15;167(6):3406-13. - Pubmed Jankun J, Skrzypczak-Jankun E: Binding site of amiloride to urokinase plasminogen activator depends on species. Int J Mol Med. 2001 Oct;8(4):365-71. - Pubmed Luikart S, Masri M, Wahl D, Hinkel T, Beck JM, Gyetko MR, Gupta P, Oegema T: Urokinase is required for the formation of mactinin, an alpha-actinin fragment that promotes monocyte/macrophage maturation. Biochim Biophys Acta. 2002 Aug 19;1591(1-3):99-107. - Pubmed Chen YX, O'Brien ER: Ethyl isopropyl amiloride inhibits smooth muscle cell proliferation and migration by inducing apoptosis and antagonizing urokinase plasminogen activator activity. Can J Physiol Pharmacol. 2003 Jul;81(7):730-9. - Pubmed Cejkova J, Cejka C, Zvarova J: Effects of inhibition of urokinase-type plasminogen activator (u-PA) by amiloride in the cornea and tear fluid of eyes irradiated with UVB. Acta Histochem. 2005;107(1):77-86. Epub 2005 Mar 4. - Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score	1.7719

Amiloride-sensitive amine oxidase [copper-containing]
Name	Amiloride-sensitive amine oxidase [copper-containing]
Gene Name	ABP1
Actions	inhibitor
References	Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. - Pubmed Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. - Pubmed
DTHybrid score	0.7131
Amiloride-sensitive amine oxidase [copper-containing]
Name	Amiloride-sensitive amine oxidase [copper-containing]
Gene Name	ABP1
Actions	inhibitor
References	Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Finazzi Agro A, Floris G: Interaction of Pig Kidney and Lentil Seedling Copper-Containing Amine Oxidases with Guanidinium Compounds. J Enzyme Inhib. 1999 Nov;15(1):91-100. - Pubmed Padiglia A, Medda R, Lorrai A, Murgia B, Pedersen JZ, Agro AF, Floris G: Interaction of pig kidney and lentil seedling copper-containing amine oxidases with guanidinium compounds. J Enzyme Inhib. 2000;15(1):91-100. - Pubmed
DTHybrid score	0.7131

Solute carrier family 22 member 2
Name	Solute carrier family 22 member 2
Gene Name	SLC22A2
Actions	inhibitor
References	Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. - Pubmed
DTHybrid score	0.4327
Solute carrier family 22 member 1
Name	Solute carrier family 22 member 1
Gene Name	SLC22A1
Actions	inhibitor
References	Urakami Y, Okuda M, Masuda S, Akazawa M, Saito H, Inui K: Distinct characteristics of organic cation transporters, OCT1 and OCT2, in the basolateral membrane of renal tubules. Pharm Res. 2001 Nov;18(11):1528-34. - Pubmed
DTHybrid score	0.4867
Organic cation/carnitine transporter 1
Name	Organic cation/carnitine transporter 1
Gene Name	SLC22A4
Actions	inhibitor
References	Wu X, George RL, Huang W, Wang H, Conway SJ, Leibach FH, Ganapathy V: Structural and functional characteristics and tissue distribution pattern of rat OCTN1, an organic cation transporter, cloned from placenta. Biochim Biophys Acta. 2000 Jun 1;1466(1-2):315-27. - Pubmed
DTHybrid score	0.4145

Id	Partner name	Gene Name	Score
4200	Cytochrome P450 1A2	CYP1A2	0.2236
3176	Trypsin-1	PRSS1	0.1961
2331	HTH-type transcriptional regulator qacR	qacR	0.1485
6461	HTH-type transcriptional regulator qacR	qacR	0.1485
1119	Peroxiredoxin-5, mitochondrial	PRDX5	0.1431
118	Organic cation/carnitine transporter 2	SLC22A5	0.1173
6147	Solute carrier family 22 member 3	SLC22A3	0.0855
4119	Cytochrome P450 2D6	CYP2D6	0.0733
54	Prothrombin	F2	0.0708
1588	Multidrug resistance protein 1	ABCB1	0.0695
4512	Cytochrome P450 3A4	CYP3A4	0.0657
6142	Solute carrier family 22 member 8	SLC22A8	0.0585
6016	Cytochrome P450 2C19	CYP2C19	0.0445
1729	Solute carrier family 22 member 6	SLC22A6	0.0425
4757	Cytochrome P450 2C9	CYP2C9	0.0369
4118	Cytochrome P450 3A5	CYP3A5	0.0329
862	Multidrug resistance-associated protein 1	ABCC1	0.0322
6024	Cytochrome P450 1A1	CYP1A1	0.0321
1024	Solute carrier family 22 member 11	SLC22A11	0.0302
1735	Canalicular multispecific organic anion transporter 1	ABCC2	0.0297
813	Neuronal acetylcholine receptor subunit alpha-2	CHRNA2	0.0295
617	Muscarinic acetylcholine receptor M2	CHRM2	0.0288
6030	Cytochrome P450 2B6	CYP2B6	0.0271
6107	Cytochrome P450 3A7	CYP3A7	0.0271
6013	Cytochrome P450 2E1	CYP2E1	0.0269
4924	Cytochrome P450 2C8	CYP2C8	0.026
6139	Solute carrier organic anion transporter family member 1A2	SLCO1A2	0.0258
766	Beta-2 adrenergic receptor	ADRB2	0.0249
587	Serum albumin	ALB	0.0247
51	Muscarinic acetylcholine receptor M3	CHRM3	0.0247
3704	Spermidine/putrescine-binding periplasmic protein precursor	potD	0.0242
1490	Solute carrier organic anion transporter family member 1B1	SLCO1B1	0.024
449	Ornithine decarboxylase	ODC1	0.0233
492	Histamine H1 receptor	HRH1	0.0231
6106	Cytochrome P450 2C18	CYP2C18	0.0228
193	Beta-1 adrenergic receptor	ADRB1	0.0216
3560	Gentamicin 3'-acetyltransferase	aacC1	0.021
2429	Putrescine-binding periplasmic protein	potF	0.0206
4097	Neuronal acetylcholine receptor subunit alpha-9	CHRNA9	0.0205
4162	Potassium voltage-gated channel subfamily KQT member 3	KCNQ3	0.0204
556	Alpha-1A adrenergic receptor	ADRA1A	0.02
1732	ATP-binding cassette sub-family G member 2	ABCG2	0.0198
6143	Solute carrier family 22 member 7	SLC22A7	0.0197
776	Bile salt export pump	ABCB11	0.0197
220	Sodium channel protein type 5 subunit alpha	SCN5A	0.0194
1181	Alpha-1-acid glycoprotein 1	ORM1	0.0193
2164	Multidrug resistance-associated protein 4	ABCC4	0.0192
6158	Solute carrier organic anion transporter family member 1C1	SLCO1C1	0.019
3011	Suppressor of tumorigenicity protein 14	ST14	0.019
378	Alpha-2C adrenergic receptor	ADRA2C	0.0188
103	Muscarinic acetylcholine receptor M1	CHRM1	0.0188
3923	Cholinesterase	BCHE	0.0188
1086	Potassium voltage-gated channel subfamily KQT member 2	KCNQ2	0.0186
6154	Multidrug and toxin extrusion protein 1	SLC47A1	0.0185
3804	Sodium channel protein type 4 subunit alpha	SCN4A	0.0181
6160	Solute carrier organic anion transporter family member 3A1	SLCO3A1	0.0175
3851	Serine protease hepsin	HPN	0.0175
831	D(2) dopamine receptor	DRD2	0.0173
124	Histamine H2 receptor	HRH2	0.0171
3610	Thioredoxin reductase 1, cytoplasmic	TXNRD1	0.017
629	Alpha-2B adrenergic receptor	ADRA2B	0.0164
2472	Voltage-gated potassium channel	kcsA	0.0163
6366	Voltage-gated potassium channel	kcsA	0.0163
477	DNA topoisomerase 4 subunit A	parC	0.0162
886	DNA topoisomerase 4 subunit A	parC	0.0162
6226	DNA topoisomerase 4 subunit A	parC	0.0162
502	5-hydroxytryptamine 2A receptor	HTR2A	0.016
6010	Thiamine transporter 1	SLC19A2	0.0159
404	DNA gyrase subunit A	gyrA	0.0159
6224	DNA gyrase subunit A	gyrA	0.0159
341	5-hydroxytryptamine 3 receptor	HTR3A	0.0159
474	Acetylcholinesterase	ACHE	0.0152
113	S-adenosylmethionine decarboxylase proenzyme	AMD1	0.0152
318	Alpha-2A adrenergic receptor	ADRA2A	0.0146
150	Cationic amino acid transporter 3	SLC7A3	0.0144
235	High-affinity cationic amino acid transporter 1	SLC7A1	0.0144
58	Cationic amino acid transporter 4	SLC7A4	0.0144
6178	UDP-glucuronosyltransferase 2B7	UGT2B7	0.0143
7	Nitric oxide synthase, inducible	NOS2	0.0143
175	Thiamin pyrophosphokinase 1	TPK1	0.0142
303	Diamine acetyltransferase 2	SAT2	0.0141
1317	Spermine synthase	SMS	0.0141
623	Spermine oxidase	SMOX	0.0141
23	D(1A) dopamine receptor	DRD1	0.0139
275	Arachidonate 5-lipoxygenase	ALOX5	0.0139
281	5'-AMP-activated protein kinase subunit beta-1	PRKAB1	0.0137
2981	Phospholipase A2, membrane associated	PLA2G2A	0.0136
1632	Solute carrier organic anion transporter family member 2B1	SLCO2B1	0.0135
632	Alpha-1B adrenergic receptor	ADRA1B	0.0135
20	Prostaglandin G/H synthase 1	PTGS1	0.0134
817	DNA topoisomerase 2-alpha	TOP2A	0.0133
1064	DNA (cytosine-5)-methyltransferase 1	DNMT1	0.0131
3947	Xanthine dehydrogenase/oxidase	XDH	0.0131
748	5'-AMP-activated protein kinase catalytic subunit alpha-1	PRKAA1	0.013
123	Diamine acetyltransferase 1	SAT1	0.0127
5126	Arginase	rocF	0.0127
540	Sodium-dependent noradrenaline transporter	SLC6A2	0.0126
672	Prostaglandin F2-alpha receptor	PTGFR	0.0125
4773	Deoxycytidine kinase	DCK	0.0124
6022	UDP-glucuronosyltransferase 1-1	UGT1A1	0.0123
824	Sodium-dependent serotonin transporter	SLC6A4	0.0119
789	Alpha-1D adrenergic receptor	ADRA1D	0.0118
4209	ATP-sensitive inward rectifier potassium channel 8	KCNJ8	0.0116
2889	Kallikrein-6	KLK6	0.0115
2947	Trypsin	sprT	0.0114
221	Lysyl-tRNA synthetase	KARS	0.0112
320	5-hydroxytryptamine 1A receptor	HTR1A	0.0109
290	Prostaglandin G/H synthase 2	PTGS2	0.0107
6148	Multidrug resistance-associated protein 7	ABCC10	0.0107
373	Transthyretin	TTR	0.0106
6098	Potassium voltage-gated channel subfamily D member 2	KCND2	0.0106
6099	Potassium voltage-gated channel subfamily D member 3	KCND3	0.0106
677	Choline-phosphate cytidylyltransferase A	PCYT1A	0.0105
3834	Nidogen-1	NID1	0.0104
5718	Cytochrome P450 2A6	CYP2A6	0.0101
624	Guanidinoacetate N-methyltransferase	GAMT	0.01
3211	3,2-trans-enoyl-CoA isomerase, mitochondrial	DCI	0.0099
4814	Copper transport protein ATOX1	ATOX1	0.0099
3939	Amine oxidase [flavin-containing] B	MAOB	0.0099
619	Low-affinity cationic amino acid transporter 2	SLC7A2	0.0098
509	Thymidine kinase	TK	0.0097
570	Thymidine kinase	TK	0.0097
2559	Thymidine kinase	TK	0.0097
3430	Thymidine kinase	tdk	0.0097
3518	Thymidine kinase	TK	0.0097
5301	Thymidine kinase	tdk	0.0097
5771	Thymidine kinase	ORF36	0.0097
7009	Thymidine kinase	ORF36	0.0097
3970	Voltage-dependent N-type calcium channel subunit alpha-1B	CACNA1B	0.0093
6153	Solute carrier organic anion transporter family member 4A1	SLCO4A1	0.0091
3833	Plasma serine protease inhibitor	SERPINA5	0.009
1349	Plasminogen activator inhibitor 2	SERPINB2	0.009
976	Platelet glycoprotein IX	GP9	0.009
1898	Cytochrome P450 1B1	CYP1B1	0.0089
6070	Nischarin	NISCH	0.0089
6151	Monocarboxylate transporter 10	SLC16A10	0.0087
147	Aldehyde dehydrogenase, mitochondrial	ALDH2	0.0087
694	Matrix protein 2	M	0.0086
101	Potassium voltage-gated channel subfamily H member 2	KCNH2	0.0086
706	Glutamate [NMDA] receptor subunit 3A	GRIN3A	0.0084
4203	Histamine N-methyltransferase	HNMT	0.0083
6164	POU domain, class 5, transcription factor 1	POU5F1	0.0081
6432	Transporter	snf	0.0081
738	Monocarboxylate transporter 1	SLC16A1	0.008
1830	5'-nucleotidase	NT5E	0.0077
713	Sodium-dependent dopamine transporter	SLC6A3	0.0077
6014	Cytochrome P450 2A13	CYP2A13	0.0076
2886	Trypsin-3	PRSS3	0.0075
791	Urokinase plasminogen activator surface receptor	PLAUR	0.0075
125	DNA polymerase beta	POLB	0.0074
131	Synaptic vesicular amine transporter	SLC18A2	0.0074
338	DNA polymerase	UL30	0.0073
379	DNA polymerase	UL54	0.0073
697	DNA polymerase	ORF28	0.0073
2482	DNA polymerase	43	0.0073
4104	DNA polymerase	BALF5	0.0073
1709	Canalicular multispecific organic anion transporter 2	ABCC3	0.0073
6141	Sodium/bile acid cotransporter	SLC10A1	0.0072
2300	Lysozyme	E	0.0072
3633	Lysozyme	R	0.0072
5597	Lysozyme	17	0.0072
5682	Ribonuclease pancreatic	RNASE1	0.0071
3929	Phosphoethanolamine/phosphocholine phosphatase	PHOSPHO1	0.0071
3933	Choline/ethanolaminephosphotransferase	CEPT1	0.0071
549	Choline-phosphate cytidylyltransferase B	PCYT1B	0.0071
264	Choline/ethanolamine kinase [Includes: Choline kinase beta	CHKB	0.0071
769	High-affinity choline transporter 1	SLC5A7	0.0071
3926	Choline transporter-like protein 2	SLC44A2	0.0071
1686	Choline transporter-like protein 1	SLC44A1	0.0071
3927	Choline transporter-like protein 3	SLC44A3	0.0071
3925	Choline transporter-like protein 4	SLC44A4	0.0071
861	Choline kinase alpha	CHKA	0.0071
576	Choline O-acetyltransferase	CHAT	0.0071
700	Choline dehydrogenase, mitochondrial	CHDH	0.0071
3922	Phospholipase D2	PLD2	0.0071
3924	Phospholipase D1	PLD1	0.0071
756	Sex hormone-binding globulin	SHBG	0.0071
1244	Low-density lipoprotein receptor-related protein 2	LRP2	0.0071
3941	Amine oxidase [flavin-containing] A	MAOA	0.0071
6171	Solute carrier family 28 member 3	SLC28A3	0.007
828	Phenylalanine-4-hydroxylase	PAH	0.0068
3109	Phenylalanine-4-hydroxylase	phhA	0.0068
401	Glutamate [NMDA] receptor subunit zeta-1	GRIN1	0.0068
267	Plasminogen activator inhibitor 1	SERPINE1	0.0067
1757	Myeloperoxidase	MPO	0.0067
3876	Aromatic-L-amino-acid decarboxylase	DDC	0.0067
6137	Multidrug resistance-associated protein 6	ABCC6	0.0065
462	Intermediate conductance calcium-activated potassium channel protein 4	KCNN4	0.0065
3611	Cytidine deaminase	cdd	0.0065
3707	Cytidine deaminase	cdd	0.0065
4211	Cytidine deaminase	CDA	0.0065
709	ATP-sensitive inward rectifier potassium channel 1	KCNJ1	0.0065
6136	Multidrug resistance-associated protein 5	ABCC5	0.0061
234	Plasminogen	PLG	0.006
2236	Casein kinase II subunit alpha	CSNK2A1	0.006
1341	Histamine H3 receptor	HRH3	0.006
1792	Tissue-type plasminogen activator	PLAT	0.006
751	Potassium channel subfamily K member 6	KCNK6	0.0058
6111	DNA polymerase epsilon subunit 4	POLE4	0.0058
6112	DNA polymerase epsilon subunit 3	POLE3	0.0058
6108	Ribonucleoside-diphosphate reductase subunit M2 B	RRM2B	0.0058
6110	DNA polymerase epsilon subunit 2	POLE2	0.0058
164	Histamine H4 receptor	HRH4	0.0058
6109	DNA polymerase epsilon catalytic subunit A	POLE	0.0058
274	Muscarinic acetylcholine receptor M5	CHRM5	0.0057
499	Arginine decarboxylase	ADC	0.0057
6017	Cholesterol side-chain cleavage enzyme, mitochondrial	CYP11A1	0.0056
1360	Sphingomyelin phosphodiesterase	SMPD1	0.0056
450	Muscarinic acetylcholine receptor M4	CHRM4	0.0056
2222	Equilibrative nucleoside transporter 1	SLC29A1	0.0055
109	Mitochondrial carnitine/acylcarnitine carrier protein CACL	SLC25A29	0.0055
636	Mitochondrial carnitine/acylcarnitine carrier protein	SLC25A20	0.0055
1759	85 kDa calcium-independent phospholipase A2	PLA2G6	0.0055
1770	Phospholipase C	PLCL1	0.0055
2841	Phospholipase C	plc	0.0055
577	Argininosuccinate lyase	ASL	0.0054
834	Arginase-2, mitochondrial	ARG2	0.0054
172	Potassium channel subfamily K member 1	KCNK1	0.0053
163	D(1B) dopamine receptor	DRD5	0.0052
6157	Solute carrier organic anion transporter family member 1B3	SLCO1B3	0.0052
1517	Beta-3 adrenergic receptor	ADRB3	0.0051
4218	Ribonucleoside-diphosphate reductase M2 subunit	RRM2	0.005
136	Estrogen receptor	ESR1	0.005
432	D(4) dopamine receptor	DRD4	0.005
6165	Copper-transporting ATPase 1	ATP7A	0.0049
6163	Copper-transporting ATPase 2	ATP7B	0.0049
740	Argininosuccinate synthase	ASS1	0.0048
865	Argininosuccinate synthase	ASS1	0.0048
2680	Argininosuccinate synthase	argG	0.0048
3194	Argininosuccinate synthase	argG	0.0048
6104	Dimethylaniline monooxygenase [N-oxide-forming] 1	FMO1	0.0048
6152	Solute carrier organic anion transporter family member 2A1	SLCO2A1	0.0048
638	D(3) dopamine receptor	DRD3	0.0048
948	Neuronal acetylcholine receptor subunit beta-2	CHRNB2	0.0048
6080	Neuronal acetylcholine receptor subunit alpha-5	CHRNA5	0.0048
6082	Neuronal acetylcholine receptor subunit beta-3	CHRNB3	0.0048
6168	Solute carrier family 22 member 16	SLC22A16	0.0047
200	Carnitine O-palmitoyltransferase 2, mitochondrial	CPT2	0.0047
451	Carnitine O-palmitoyltransferase I, liver isoform	CPT1A	0.0047
731	HIV-1 protease	HIV-1 protease	0.0047
412	Peroxisomal carnitine O-octanoyltransferase	CROT	0.0047
6146	High affinity copper uptake protein 1	SLC31A1	0.0047
551	Carnitine O-acetyltransferase	CRAT	0.0046
514	Potassium voltage-gated channel subfamily H member 6	KCNH6	0.0045
772	Potassium voltage-gated channel subfamily H member 7	KCNH7	0.0045
4152	Superoxide dismutase [Cu-Zn]	SOD1	0.0045
908	Glutathione S-transferase theta-1	GSTT1	0.0044
6081	Neuronal acetylcholine receptor subunit alpha-6	CHRNA6	0.0044
465	Calmodulin	CALM1	0.0044
342	P protein [Includes: DNA-directed DNA polymerase	P	0.0044
612	P protein [Includes: DNA-directed DNA polymerase	P	0.0044
603	DNA polymerase alpha catalytic subunit	POLA1	0.0043
3755	Nucleoside-specific channel-forming protein tsx precursor	tsx	0.0043
885	5-hydroxytryptamine 1B receptor	HTR1B	0.0041
360	Ribonucleoside-diphosphate reductase large subunit	RRM1	0.0041
6078	Neuronal acetylcholine receptor subunit beta-4	CHRNB4	0.0041
6101	Dimethylaniline monooxygenase [N-oxide-forming] 3	FMO3	0.0041
6140	Ileal sodium/bile acid cotransporter	SLC10A2	0.004
896	Glutathione S-transferase Mu 1	GSTM1	0.0039
869	Estrogen receptor beta	ESR2	0.0039
5626	Nucleoside diphosphate kinase B	NME2	0.0038
3811	Cytochrome P450 19A1	CYP19A1	0.0038
702	UMP-CMP kinase	CMPK1	0.0037
805	Cytochrome P450 11B1, mitochondrial	CYP11B1	0.0037
6079	Neuronal acetylcholine receptor subunit alpha-3	CHRNA3	0.0037
2157	NAD(P)H dehydrogenase [quinone] 1	NQO1	0.0037
458	Neuronal acetylcholine receptor subunit alpha-10	CHRNA10	0.0037
5878	Alpha-7 nicotinic cholinergic receptor subunit	CHRFAM7A	0.0037
527	Prostacyclin receptor	PTGIR	0.0036
6167	Organic solute transporter subunit beta	OSTB	0.0036
6166	Organic solute transporter subunit alpha	OSTA	0.0036
723	Cytosolic phospholipase A2	PLA2G4A	0.0036
904	Glutathione S-transferase P	GSTP1	0.0035
464	Glutamate [NMDA] receptor subunit epsilon-2	GRIN2B	0.0034
1864	RET proto-oncogene	RET	0.0034
1950	Epithelial discoidin domain-containing receptor 1	DDR1	0.0033
6094	BCR/ABL fusion protein isoform X9	BCR/ABL fusion	0.0033
6170	ATP-binding cassette sub-family A member 3	ABCA3	0.0033
1974	Oligopeptide transporter, kidney isoform	SLC15A2	0.0033
277	Purine nucleoside phosphorylase	PNP	0.0033
2870	Purine nucleoside phosphorylase	punA	0.0033
2945	Purine nucleoside phosphorylase	punA	0.0033
4659	Purine nucleoside phosphorylase	TM_1596	0.0033
4825	Purine nucleoside phosphorylase	TTHA1435	0.0033
291	Nitric-oxide synthase, endothelial	NOS3	0.0033
2251	Thymidylate kinase	tmk	0.0033
2254	Thymidylate kinase	DTYMK	0.0033
3522	Thymidylate kinase	tmk	0.0033
3478	Glucose-1-phosphate thymidylyltransferase	rmlA	0.0032
4277	Glucose-1-phosphate thymidylyltransferase	rmlA	0.0032
837	Glutamate [NMDA] receptor subunit epsilon-1	GRIN2A	0.0032
1539	Oligopeptide transporter, small intestine isoform	SLC15A1	0.0032
153	Dopamine beta-hydroxylase	DBH	0.0031
2257	Uridine phosphorylase	udp	0.0031
5132	Uridine phosphorylase	udp	0.0031
6212	Tubulin gamma-1 chain	TUBG1	0.0031
6210	Tubulin delta chain	TUBD1	0.0031
6211	Tubulin epsilon chain	TUBE1	0.0031
5294	Nucleoside diphosphate kinase A	NME1	0.003
4604	Liver carboxylesterase 1	CES1	0.003
6155	ATP-binding cassette transporter sub-family C member 11	ABCC11	0.003
6218	Pannexin-1	PANX1	0.003
4095	Neuronal acetylcholine receptor subunit alpha-7	CHRNA7	0.0029
947	Neuronal acetylcholine receptor subunit alpha-4	CHRNA4	0.0029
6002	Prostaglandin E2 receptor EP4 subtype	PTGER4	0.0028
436	5-hydroxytryptamine 2B receptor	HTR2B	0.0028
6180	UDP-glucuronosyltransferase 2B4	UGT2B4	0.0027
1618	High affinity nerve growth factor receptor	NTRK1	0.0027
6031	Cytochrome P450 3A43	CYP3A43	0.0027
725	5-hydroxytryptamine 1D receptor	HTR1D	0.0027
4131	Prostaglandin E2 receptor, EP3 subtype	PTGER3	0.0027
406	Prostaglandin E2 receptor, EP2 subtype	PTGER2	0.0026
950	Alpha platelet-derived growth factor receptor	PDGFRA	0.0026
951	Macrophage colony-stimulating factor 1 receptor	CSF1R	0.0026
215	Sodium channel protein type 11 subunit alpha	SCN11A	0.0026
590	5-hydroxytryptamine 2C receptor	HTR2C	0.0025
3810	Catechol O-methyltransferase	COMT	0.0025
228	Beta platelet-derived growth factor receptor	PDGFRB	0.0025
4217	Telomerase reverse transcriptase	TERT	0.0024
6149	Solute carrier family 22 member 10	SLC22A10	0.0024
380	Cytochrome P450 17A1	CYP17A1	0.0024
1629	Transcription factor AP-1	JUN	0.0024
73	Prostaglandin E2 receptor, EP1 subtype	PTGER1	0.0023
504	Mast/stem cell growth factor receptor	KIT	0.0023
4114	Voltage-dependent L-type calcium channel subunit beta-3	CACNB3	0.0022
4112	Voltage-dependent L-type calcium channel subunit beta-4	CACNB4	0.0022
737	Mineralocorticoid receptor	NR3C2	0.0022
392	Voltage-dependent P/Q-type calcium channel subunit alpha-1A	CACNA1A	0.0022
2449	Tubulin alpha-3 chain	TUBA1A	0.0022
146	Androgen receptor	AR	0.0022
161	Tubulin beta chain	TUBB	0.0021
312	Tubulin beta chain	TUB2	0.0021
4113	Voltage-dependent L-type calcium channel subunit alpha-1F	CACNA1F	0.0021
333	Voltage-dependent L-type calcium channel subunit beta-1	CACNB1	0.002
15	Voltage-dependent T-type calcium channel subunit alpha-1I	CACNA1I	0.002
17	Proto-oncogene tyrosine-protein kinase ABL1	ABL1	0.002
614	Progesterone receptor	PGR	0.002
781	ATP-sensitive inward rectifier potassium channel 11	KCNJ11	0.002
535	Voltage-dependent T-type calcium channel subunit alpha-1G	CACNA1G	0.0019
6085	Fatty acid-binding protein, intestinal	FABP2	0.0019
489	Monocarboxylate transporter 2	SLC16A7	0.0019
467	Delta-type opioid receptor	OPRD1	0.0019
696	Kappa-type opioid receptor	OPRK1	0.0019
6091	Gamma-aminobutyric acid receptor subunit theta	GABRQ	0.0019
4192	DNA topoisomerase 2-beta	TOP2B	0.0019
2320	Thymidine kinase, cytosolic	TK1	0.0018
847	Mu-type opioid receptor	OPRM1	0.0018
4110	Voltage-dependent L-type calcium channel subunit beta-2	CACNB2	0.0017
4115	Voltage-dependent L-type calcium channel subunit alpha-1D	CACNA1D	0.0017
6086	Gamma-aminobutyric acid receptor subunit gamma-2	GABRG2	0.0017
4111	Voltage-dependent L-type calcium channel subunit alpha-1S	CACNA1S	0.0017
6092	Gamma-aminobutyric acid receptor subunit rho-2	GABRR2	0.0017
6090	Gamma-aminobutyric acid receptor subunit pi	GABRP	0.0017
6088	Gamma-aminobutyric acid receptor subunit gamma-3	GABRG3	0.0017
6115	Gamma-aminobutyric acid receptor subunit rho-3	GABRR3	0.0017
4100	Gamma-aminobutyric-acid receptor subunit beta-2	GABRB2	0.0017
6093	Gamma-aminobutyric acid receptor subunit delta	GABRD	0.0017
478	Voltage-dependent L-type calcium channel subunit alpha-1C	CACNA1C	0.0017
6087	Gamma-aminobutyric acid receptor subunit gamma-1	GABRG1	0.0017
6089	Gamma-aminobutyric acid receptor subunit epsilon	GABRE	0.0017
142	Gamma-aminobutyric-acid receptor subunit rho-1	GABRR1	0.0017
198	Sodium channel protein type 10 subunit alpha	SCN10A	0.0017
1284	Nuclear receptor subfamily 1 group I member 2	NR1I2	0.0017
4098	Gamma-aminobutyric-acid receptor subunit beta-1	GABRB1	0.0016
4099	Gamma-aminobutyric-acid receptor subunit beta-3	GABRB3	0.0016
4120	NADPH--cytochrome P450 reductase	POR	0.0016
6161	Probable low affinity copper uptake protein 2	SLC31A2	0.0016
841	Gamma-aminobutyric-acid receptor subunit alpha-6	GABRA6	0.0016
530	Gamma-aminobutyric-acid receptor subunit alpha-4	GABRA4	0.0015
523	Gamma-aminobutyric-acid receptor subunit alpha-5	GABRA5	0.0015
580	Gamma-aminobutyric-acid receptor subunit alpha-3	GABRA3	0.0015
423	Gamma-aminobutyric-acid receptor subunit alpha-2	GABRA2	0.0015
872	Gamma-aminobutyric-acid receptor subunit alpha-1	GABRA1	0.0014
3587	Gastrotropin	FABP6	0.0012
468	Cytochrome P450 4A11	CYP4A11	0.0012
33	Cystine/glutamate transporter	SLC7A11	0.001
6025	UDP-glucuronosyltransferase 1-4	UGT1A4	0.0009

(*) Categorization taken from DrugBank: therapeutic category or general category of a drug (i.e. anti-convulsant, antibacterial, etc.)

DB00594 - Amiloride

Targets

Enzymes

Transporters

Predictions