| Version |
2.5 |
| Creation Date |
2005-06-13 13:24:05 |
| Update Date |
2009-02-19 16:04:27 |
| Primary Accession Number |
DB00390 |
| Secondary Accession Number |
|
| Name |
Digoxin |
| Drug Type |
|
| Description |
A cardiotonic glycoside obtained mainly from Digitalis lanata; it consists of three sugars and the aglycone digoxigenin. Digoxin has positive inotropic and negative chronotropic activity. It is used to control ventricular rate in atrial fibrillation and in the management of congestive heart failure with atrial fibrillation. Its use in congestive heart failure and sinus rhythm is less certain. The margin between toxic and therapeutic doses is small. (From Martindale, The Extra Pharmacopoeia, 30th ed, p666) |
| Synonyms |
- Digitalis Glycoside
|
| Brand Names |
- Cardoxin
- Cogoxin
- Cordioxil
- Davoxin
- Digacin
- Digitekt
- Digoxin Pediatric
- Dilanacin
- Dixina
- Dokim
- Dynamos
- Eudigox
- Homolle's Digitalin
- Lanacordin
- Lanacrist
- Lanicor
- Lanoxicaps
- Lanoxin
- Lenoxicaps
- Lenoxin
- Longdigox
- Neo-Lanicor
- Neodioxanin
- Rougoxin
- SK-Digoxin
- Stillacor
- Vanoxin
|
| Brand Mixtures |
Not Available |
| Chemical IUPAC Name |
4-[(3S,5R,8R,9S,10S,12R,13S,14S)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-12,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-5H-furan-2-one |
| Chemical Formula |
C41H64O14 |
| Chemical Structure |
 |
| CAS Registry Number |
20830-75-5 |
| InChI Identifier |
InChI=1/C41H64O14/c1-19-36(47)28(42)15-34(50-19)54-38-21(3)52-35(17-30(38)44)55-37-20(2)51-33(16-29(37)43)53-24-8-10-39(4)23(13-24)6-7-26-27(39)14-31(45)40(5)25(9-11-41(26,40)48)22-12-32(46)49-18-22/h12,19-21,23-31,33-38,42-45,47-48H,6-11,13-18H2,1-5H3/t19-,20-,21-,23-,24+,25?,26-,27+,28+,29+,30+,31-,33+,34+,35+,36-,37-,38-,39+,40+,41+/m1/s1 |
| InChI Key |
LTMHDMANZUZIPE-YUICGFAKBN |
| KEGG Drug |
D00298  |
| KEGG Compound |
C06956  |
| PubChem Compound |
30322  |
| PubChem Substance |
172469  |
| ChEBI ID |
Not Available |
| PharmGKB ID |
PA449319  |
| HET ID |
Not Available |
| GenBank ID |
Not Available |
| Drug ID Number [DIN] |
02242323  |
| RxList Link |
http://www.rxlist.com/cgi/generic/dig.htm  |
| PDRhealth Link |
Not Available |
| Wikipedia Link |
http://en.wikipedia.org/wiki/Digoxin  |
| FDA Label |
|
| Material Safety Data Sheet (MSDS) |
|
| Synthesis Reference |
S. Smith, J. Chem. Soc. 1930, 508 |
| Average Molecular Weight |
780.9385 |
| Monoisotopic Molecular Weight |
780.4296 |
| State |
Solid |
| Melting Point |
248-250 oC |
| Experimental Water Solubility |
Insoluble
Source: PhysProp
|
| Predicted Water Solubility |
1.27e-01 mg/mL
Calculated using ALOGPS
|
| Experimental LogP/Hydrophobicity |
2.2
Source: PhysProp
|
| Predicted LogP |
1.04
Calculated using ALOGPS
|
| Experimental LogS |
Not Available |
| Predicted LogS |
-3.79
Calculated using ALOGPS
|
| Experimental Caco2 Permeability |
Not Available |
| pKa/Isoelectric Point |
Not Available |
| Mass Spectrum |
Not Available
|
| MOL File |
Show | Download  |
| SDF File |
Show | Download  |
| PDB File |
Show | Download  |
| 2D Structure |
|
| 3D Structure |
|
| Experimental PDB ID |
Not Available |
| Isomeric SMILES |
C[C@H]1O[C@H](C[C@H](O)[C@@H]1O)O[C@H]1[C@@H](O)C[C@@H](O[C@@H]1C)O[C@H]1[C@@H](O)C[C@H](O[C@H]2CC[C@@]3(C)[C@H](CC[C@@H]4[C@@H]3C[C@@H](O)[C@]3(C)[C@H](CC[C@]43O)C3=CC(=O)OC3)C2)O[C@@H]1C |
| Canonical SMILES |
CC1OC(CC(O)C1O)OC1C(O)CC(OC1C)OC1C(O)CC(OC2CCC3(C)C(CCC4C3CC(O)C3(C)C(CCC43O)C3=CC(=O)OC3)C2)OC1C |
| Drug Category |
- Anti-Arrhythmia Agents
- Antiarrhythmic Agents
- Cardiotonic Agents
- Enzyme Inhibitors
|
| ATC Codes |
|
| AHFS Codes |
|
| Indication |
For the treatment and management of congestive cardiac insufficiency, arrhythmias and heart failure. |
| Pharmacology |
Digoxin, a cardiac glycoside similar to digitoxin, is used to treat congestive heart failure and supraventricular arrhythmias due to reentry mechanisms, and to control ventricular rate in the treatment of chronic atrial fibrillation. |
| Mechanism of Action |
Digoxin inhibits the Na-K-ATPase membrane pump, resulting in an increase in intracellular sodium and calcium concentrations. Increased intracellular concentrations of calcium may promote activation of contractile proteins (e.g., actin, myosin). Digoxin also acts on the electrical activity of the heart, increasing the slope of phase 4 depolarization, shortening the action potential duration, and decreasing the maximal diastolic potential. |
| Absorption |
Absorption of digoxin from the elixir pediatric formulation has been demonstrated to be 70% to 85% complete (90% to 100% from the capsules, and 60% to 80% for tablets). |
| Toxicity |
Toxicity includes ventricular tachycardia or ventricular fibrillation, or progressive bradyarrhythmias, or heart block. LD50 = 7.8 mg/kg (orally in mice). |
| Protein Binding |
25% |
| Biotransformation |
Hepatic (but not dependent upon the cytochrome P-450 system). The end metabolites, which include 3 b-digoxigenin, 3-keto-digoxigenin, and their glucuronide and sulfate conjugates, are polar in nature and are postulated to be formed via hydrolysis, oxidation, and conjugation. |
| Half Life |
3.5 to 5 days |
| Dosage Forms |
| Form |
Route |
| Liquid |
Intravenous |
| Powder, for solution |
Intravenous |
| Solution |
Oral |
| Tablet |
Oral |
|
| Patient Information |
Show  |
| Contraindications |
Show  |
| Interactions |
Show  |
| Drug Interactions |
| Drug |
Interaction |
| Acarbose |
Acarbose decreases the effect of digoxin |
| Alprazolam |
The benzodiazepine increases the effect of digoxin |
| Amiodarone |
Amiodarone increases the effect of digoxin |
| Bendroflumethiazide |
Possible electrolyte variations and arrhythmias |
| Benzthiazide |
Possible electrolyte variations and arrhythmias |
| Bleomycin |
The antineoplasic agent decreases the effect of digoxin |
| Bumetanide |
Possible electrolyte variations and arrhythmias |
| Carmustine |
The antineoplasic agent decreases the effect of digoxin |
| Carvedilol |
Carvedilol increases levels/effect of digoxin |
| Chlorothiazide |
Possible electrolyte variations and arrhythmias |
| Chlorthalidone |
Possible electrolyte variations and arrhythmias |
| Cholestyramine |
The resin decreases the effect of digoxin |
| Clarithromycin |
The macrolide increases the effect of digoxin in 10% of patients |
| Colestipol |
The resin decreases the effect of digoxin |
| Cyclophosphamide |
The antineoplasic agent decreases the effect of digoxin |
| Cyclosporine |
Cyclosporine increases the effect of digoxin |
| Cyclothiazide |
Possible electrolyte variations and arrhythmias |
| Cytarabine |
The antineoplasic agent decreases the effect of digoxin |
| Demeclocycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Dextrothyroxine |
The thyroid hormone decreases the effect of digoxin |
| Diazepam |
The benzodiazepine increases the effect of digoxin |
| Dihydroquinidine barbiturate |
Quinine/quinidine increases the effect of digoxin |
| Doxorubicin |
The antineoplasic agent decreases the effect of digoxin |
| Doxycycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Erythromycin |
The macrolide increases the effect of digoxin in 10% of patients |
| Ethacrynic acid |
Possible electrolyte variations and arrhythmias |
| Furosemide |
Possible electrolyte variations and arrhythmias |
| Gatifloxacin |
Gatifloxacin increases the effect of digoxin |
| Ginseng |
Changes in digoxin serum levels |
| Hydrochlorothiazide |
Possible electrolyte variations and arrhythmias |
| Hydroflumethiazide |
Possible electrolyte variations and arrhythmias |
| Hydroxychloroquine |
Hydroxychloroquine increases the effect of digoxin |
| Indapamide |
Possible electrolyte variations and arrhythmias |
| Itraconazole |
Itraconazole increases the effect of digoxin |
| Josamycin |
The macrolide increases the efect of digoxin in 10% of patients |
| Levothyroxine |
The thyroid hormones decreases the effect of digoxin |
| Liothyronine |
The thyroid hormones decreases the effect of digoxin |
| Liotrix |
The thyroid hormone decreases the effect of digoxin |
| Methacycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Methimazole |
The antithyroid agent increases the effect of digoxin |
| Methotrexate |
The antineoplasic agent decreases the effect of digoxin |
| Methyclothiazide |
Possible electrolyte variations and arrhythmias |
| Metolazone |
Possible electrolyte variations and arrhythmias |
| Minocycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Oxytetracycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Penicillamine |
Penicillamine decreases the effect of digoxin |
| Polythiazide |
Possible electrolyte variations and arrhythmias |
| Prazosin |
Prazosin increases the effect of digoxin |
| Procarbazine |
The antineoplasic agent decreases the effect of digoxin |
| Propafenone |
Propafenone increases the effect of digoxin |
| Propylthiouracil |
The antithyroid agent increases the effect of digoxin |
| Quinethazone |
Possible electrolyte variations and arrhythmias |
| Quinidine |
Quinine/quinidine increases the effect of digoxin |
| Quinidine barbiturate |
Quinine/quinidine increases the effect of digoxin |
| Quinine |
Quinine/quinidine increases the effect of digoxin |
| Rabeprazole |
Rabeprazole increases the effect of digoxin |
| Ranolazine |
Ranolazine increases digoxin's levels |
| Ritonavir |
Ritonavir increases levels/effect of digoxin |
| Rolitetracycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Spironolactone |
Increased digoxin levels and decreased effect in presence of spironolactone |
| St. John's Wort |
St. John's Wort decreases the effect of digoxin |
| Sulfasalazine |
Sulfasalazine decreases the effect of digoxin |
| Telithromycin |
Telithromycin may increase levels of digoxin |
| Telmisartan |
Telmisartan increases the effect of digoxin |
| Tetracycline |
The tetracycline increases the effect of digoxin in 10% of patients |
| Thyroglobulin |
The thyroid hormone decreases the effect of digoxin |
| Tolbutamide |
Tolbutamide increases the effect of digoxin |
| Trichlormethiazide |
Possible electrolyte variations and arrhythmias |
| Verapamil |
Verapamil increases the effect of digoxin |
| Vincristine |
The antineoplasic agent decreases the effect of digoxin |
|
| Food Interactions |
- Avoid avocado.
- Avoid bran and high fiber foods within 2 hours of taking this medication.
- Avoid excess salt/sodium unless otherwise instructed by your physician.
- Avoid milk, calcium containing dairy products, iron, antacids, or aluminum salts 2 hours before or 6 hours after using antacids while on this medication.
- Avoid salt substitutes containing potassium.
- Limit garlic, ginger, gingko, and horse chestnut.
|
| Pathways |
Not Available
|
| General References |
- Flanagan RJ, Jones AL: Fab antibody fragments: some applications in clinical toxicology. Drug Saf. 2004;27(14):1115-33. [PubMed
]
- Kaplanski J, Weinhouse E, Topaz M, Genchik G: Verapamil and digoxin: interactions in the rat. Res Commun Chem Pathol Pharmacol. 1983 Dec;42(3):377-88. [PubMed
]
- Thompson DF, Carter JR: Drug-induced gynecomastia. Pharmacotherapy. 1993 Jan-Feb;13(1):37-45. [PubMed
]
- Doering W, Konig E, Sturm W: [Digitalis intoxication: specifity and significance of cardiac and extracardiac symptoms. part I: Patients with digitalis-induced arrhythmias (author's transl)] Z Kardiol. 1977 Mar;66(3):121-8. [PubMed
]
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- Wikipedia

- RxList

|
| Organisms Affected |
|
| Phase 1 Metabolizing Enzymes |
- Cytochrome P450 11A1 (CYP11A1)
|
| Targets |
- Sodium/potassium-transporting ATPase alpha-1 chain
- Solute carrier organic anion transporter family member 1B1
|
|
Drug Target 1
[top]
|
| Target 1 ID |
806 |
| Target 1 Name |
Sodium/potassium-transporting ATPase alpha-1 chain |
| Target 1 Synonyms |
- EC 3.6.3.9
- Na(+)/K(+) ATPase alpha-1 subunit
- Sodium pump subunit alpha 1
- Sodium/potassium-transporting ATPase alpha-1 chain precursor
|
| Target 1 Gene Name |
ATP1A1 |
| Target 1 Protein Sequence |
>Sodium/potassium-transporting ATPase alpha-1 chain precursor
MGKGVGRDKYEPAAVSEQGDKKGKKGKKDRDMDELKKEVSMDDHKLSLDELHRKYGTDLS
RGLTSARAAEILARDGPNALTPPPTTPEWIKFCRQLFGGFSMLLWIGAILCFLAYSIQAA
TEEEPQNDNLYLGVVLSAVVIITGCFSYYQEAKSSKIMESFKNMVPQQALVIRNGEKMSI
NAEEVVVGDLVEVKGGDRIPADLRIISANGCKVDNSSLTGESEPQTRSPDFTNENPLETR
NIAFFSTNCVEGTARGIVVYTGDRTVMGRIATLASGLEGGQTPIAAEIEHFIHIITGVAV
FLGVSFFILSLILEYTWLEAVIFLIGIIVANVPEGLLATVTVCLTLTAKRMARKNCLVKN
LEAVETLGSTSTICSDKTGTLTQNRMTVAHMWFDNQIHEADTTENQSGVSFDKTSATWLA
LSRIAGLCNRAVFQANQENLPILKRAVAGDASESALLKCIELCCGSVKEMRERYAKIVEI
PFNSTNKYQLSIHKNPNTSEPQHLLVMKGAPERILDRCSSILLHGKEQPLDEELKDAFQN
AYLELGGLGERVLGFCHLFLPDEQFPEGFQFDTDDVNFPIDNLCFVGLISMIDPPRAAVP
DAVGKCRSAGIKVIMVTGDHPITAKAIAKGVGIISEGNETVEDIAARLNIPVSQVNPRDA
KACVVHGSDLKDMTSEQLDDILKYHTEIVFARTSPQQKLIIVEGCQRQGAIVAVTGDGVN
DSPALKKADIGVAMGIAGSDVSKQAADMILLDDNFASIVTGVEEGRLIFDNLKKSIAYTL
TSNIPEITPFLIFIIANIPLPLGTVTILCIDLGTDMVPAISLAYEQAESDIMKRQPRNPK
TDKLVNERLISMAYGQIGMIQALGGFFTYFVILAENGFLPIHLLGLRVDWDDRWINDVED
SYGQQWTYEQRKIVEFTCHTAFFVSIVVVQWADLVICKTRRNSVFQQGMKNKILIFGLFE
ETALAAFLSYCPGMGVALRMYPLKPTWWFCAFPYSLLIFVYDEVRKLIIRRRPGGWVEKE
TYY
|
| Target 1 Number of Residues |
1040 |
| Target 1 Molecular Weight |
112897 |
| Target 1 Theoretical pI |
5.15 |
| Target 1 GO Classification |
|
Function
|
hydrolase activity
hydrolase activity, acting on acid anhydrides
hydrolase activity, acting on acid anhydrides, catalyzing transmembrane movement of substances
catalytic activity
binding
nucleotide binding
purine nucleotide binding
adenyl nucleotide binding
ATP binding
monovalent inorganic cation transporter activity
transporter activity
ion transporter activity
cation transporter activity
ATPase activity, coupled to transmembrane movement of ions, phosphorylative mechanism |
|
Process
|
metabolism
monovalent inorganic cation transport
physiological process
cellular physiological process
transport
ion transport
cation transport |
|
Component
|
intrinsic to membrane
integral to membrane
cell
membrane |
|
| Target 1 General Function |
Inorganic ion transport and metabolism |
| Target 1 Specific Function |
This is the catalytic component of the active enzyme, which catalyzes the hydrolysis of ATP coupled with the exchange of sodium and potassium ions across the plasma membrane. This action creates the electrochemical gradient of sodium and potassium ions, providing the energy for active transport of various nutrients |
| Target 1 Pathways |
Not Available
|
| Target 1 Reactions |
- ATP + H2O + Na+in + K+out = ADP + phosphate + Na+out + K+in
|
| Target 1 Pfam Domain Function |
|
| Target 1 Signals |
|
| Target 1 Transmembrane Regions |
- 88-108
- 132-152
- 289-308
- 321-338
- 773-792
- 803-823
- 844-866
- 919-938
- 952-970
- 986-1006
|
| Target 1 Essentiality |
Non-Essential |
| Target 1 GenBank ID Protein |
219942  |
| Target 1 UniProtKB/Swiss-Prot ID |
P05023  |
| Target 1 UniProtKB/Swiss-Prot Entry Name |
AT1A1_HUMAN  |
| Target 1 PDB ID |
1MO8  |
| Target 1 PDB File |
Show |
| Target 1 3D Structure |
|
| Target 1 Cellular Location |
- Membrane
- multi-pass membrane protein
|
| Target 1 Gene Sequence |
>3072 bp
ATGGGGAAGGGGGTTGGACGTGATAAGTATGAGCCTGCAGCTGTTTCAGAACAAGGTGAT
AAAAAGGGCAAAAAGGGCAAAAAAGACAGGGACATGGATGAACTGAAGAAAGAAGTTTCT
ATGGATGATCATAAACTTAGCCTTGATGAACTTCATCGTAAATATGGAACAGACTTGAGC
CGGGGATTAACATCTGCTCGTGCAGCTGAGATCCTGGCGCGAGATGGTCCCAACGCCCTC
ACTCCCCCTCCCACTACTCCTGAATGGATCAAGTTTTGTCGGCAGCTCTTTGGGGGGTTC
TCAATGTTACTGTGGATTGGAGCGATTCTTTGTTTCTTGGCTTATAGCATCCAAGCTGCT
ACAGAAGAGGAACCTCAAAACGATAATCTGTACCTGGGTGTGGTGCTATCAGCCGTTGTA
ATCATAACTGGTTGCTTCTCCTACTATCAAGAAGCTAAAAGTTCAAAGATCATGGAATCC
TTCAAAAACATGGTCCCTCAGCAAGCCCTTGTGATTCGAAATGGTGAGAAAATGAGCATA
AATGCGGAGGAAGTTGTGGTTGGGGATCTGGTGGAAGTAAAAGGAGGAGACCGAATTCCT
GCTGACCTCAGAATCATATCTGCAAATGGCTGCAAGGTGGATAACTCCTCGCTCACTGGT
GAATCAGAACCCCAGACTAGGTCTCCAGATTTCACAAATGAAAACCCCCTGGAGACGAGG
AACATTGCCTTCTTTTCAACAAATTGTGTTGAAGGCACCGCACGTGGTATTGTTGTCTAC
ACTGGGGATCGCACTGTGATGGGAAGAATTGCCACACTTGCTTCTGGGCTGGAAGGAGGC
CAGACCCCCATTGCTGCAGAAATTGAACATTTTATCCACATCATCACGGGTGTGGCTGTG
TTCCTGGGTGTGTCTTTCTTCATCCTTTCTCTCATCCTTGAGTACACCTGGCTTGAGGCT
GTCATCTTCCTCATCGGTATCATCGTAGCCAATGTGCCGGAAGGTTTGCTGGCCACTGTC
ACGGTCTGTCTGACACTTACTGCCAAACGCATGGCAAGGAAAAACTGCTTAGTGAAGAAC
TTAGAAGCTGTGGAGACCTTGGGGTCCACGTCCACCATCTGCTCTGATAAAACTGGAACT
CTGACTCAGAACCGGATGACAGTGGCCCACATGTGGTTTGACAATCAAATCCATGAAGCT
GATACGACAGAGAATCAGAGTGGTGTCTCTTTTGACAAGACTTCAGCTACCTGGCTTGCT
CTGTCCAGAATTGCAGGTCTTTGTAACAGGGCAGTGTTTCAGGCTAACCAGGAAAACCTA
CCTATTCTTAAGCGGGCAGTTGCAGGAGATGCCTCTGAGTCAGCACTCTTAAAGTGCATA
GAGCTGTGCTGTGGTTCCGTGAAGGAGATGAGAGAAAGATACGCCAAAATCGTCGAGATA
CCCTTCAACTCCACCAACAAGTACCAGTTGTCTATTCATAAGAACCCCAACACATCGGAG
CCCCAACACCTGTTGGTGATGAAGGGCGCCCCAGAAAGGATCCTAGACCGTTGCAGCTCT
ATCCTCCTCCACGGCAAGGAGCAGCCCCTGGATGAGGAGCTGAAAGACGCCTTTCAGAAC
GCCTATTTGGAGCTGGGGGGCCTCGGAGAACGAGTCCTAGGTTTCTGCCACCTCTTTCTG
CCAGATGAACAGTTTCCTGAAGGGTTCCAGTTTGACACTGACGATGTGAATTTCCCTATC
GATAATCTGTGCTTTGTTGGGCTCATCTCCATGATTGACCCTCCACGGGCGGCCGTTCCT
GATGCCGTGGGCAAATGTCGAAGTGCTGGAATTAAGGTCATCATGGTCACAGGAGACCAT
CCAATCACAGCTAAAGCTATTGCCAAAGGTGTGGGCATCATCTCAGAAGGCAATGAGACC
GTGGAAGACATTGCTGCCCGCCTCAACATCCCAGTCAGCCAGGTGAACCCCAGGGATGCC
AAGGCCTGCGTAGTACACGGCAGTGATCTAAAGGACATGACCTCCGAGCAGCTGGATGAC
ATTTTGAAGTACCACACTGAGATAGTGTTTGCCAGGACCTCCCCTCAGCAGAAGCTCATC
ATTGTGGAAGGCTGCCAAAGACAGGGTGCTATCGTGGCTGTGACTGGTGACGGTGTGAAT
GACTCTCCAGCTTTGAAGAAAGCAGACATTGGGGTTGCTATGGGGATTGCTGGCTCAGAT
GTGTCCAAGCAAGCTGCTGACATGATTCTTCTGGATGACAACTTTGCCTCAATTGTGACT
GGAGTAGAGGAAGGTCGTCTGATCTTTGATAACTTGAAGAAATCCATTGCTTATACCTTA
ACCAGTAACATTCCCGAGATCACCCCGTTCCTGATATTTATTATTGCAAACATTCCACTA
CCACTGGGGACTGTCACCATCCTCTGCATTGACTTGGGCACTGACATGGTTCCTGCCATC
TCCCTGGCTTATGAGCAGGCTGAGAGTGACATCATGAAGAGACAGCCCAGAAATCCCAAA
ACAGACAAACTTGTGAATGAGCGGCTGATCAGCATGGCCTATGGGCAGATTGGAATGATC
CAGGCCCTGGGAGGCTTCTTTACTTACTTTGTGATTCTGGCTGAGAACGGCTTCCTCCCA
ATTCACCTGTTGGGCCTCCGAGTGGACTGGGATGACCGCTGGATCAACGATGTGGAAGAC
AGCTACGGGCAGCAGTGGACCTATGAGCAGAGGAAAATCGTGGAGTTCACCTGCCACACA
GCCTTCTTCGTCAGTATCGTGGTGGTGCAGTGGGCCGACTTGGTCATCTGTAAGACCAGG
AGGAATTCGGTCTTCCAGCAGGGGATGAAGAACAAGATCTTGATATTTGGCCTCTTTGAA
GAGACAGCCCTGGCTGCTTTCCTTTCCTACTGCCCTGGAATGGGTGTTGCTCTTAGGATG
TATCCCCTCAAACCTACCTGGTGGTTCTGTGCCTTCCCCTACTCTCTTCTCATCTTCGTA
TATGACGAAGTCAGAAAACTCATCATCAGGCGACGCCCTGGCGGCTGGGTGGAGAAGGAA
ACCTACTATTAG
|
| Target 1 GenBank Gene ID |
|
| Target 1 GeneCard ID |
ATP1A1  |
| Target 1 GenAtlas ID |
ATP1A1  |
| Target 1 HGNC ID |
HGNC:799  |
| Target 1 Chromosome Location |
1 |
| Target 1 Locus |
1p21 |
| Target 1 SNPs |
SNPJam Report  |
| Target 1 General References |
- Shull MM, Pugh DG, Lingrel JB: The human Na, K-ATPase alpha 1 gene: characterization of the 5'-flanking region and identification of a restriction fragment length polymorphism. Genomics. 1990 Mar;6(3):451-60. [PubMed
]
- Kawakami K, Ohta T, Nojima H, Nagano K: Primary structure of the alpha-subunit of human Na,K-ATPase deduced from cDNA sequence. J Biochem (Tokyo). 1986 Aug;100(2):389-97. [PubMed
]
- Chehab FF, Kan YW, Law ML, Hartz J, Kao FT, Blostein R: Human placental Na+,K+-ATPase alpha subunit: cDNA cloning, tissue expression, DNA polymorphism, and chromosomal localization. Proc Natl Acad Sci U S A. 1987 Nov;84(22):7901-5. [PubMed
]
- Shull MM, Lingrel JB: Multiple genes encode the human Na+,K+-ATPase catalytic subunit. Proc Natl Acad Sci U S A. 1987 Jun;84(12):4039-43. [PubMed
]
- Sverdlov ED, Monastyrskaya GS, Broude NE, Ushkaryov YuA, Allikmets RL, Melkov AM, Smirnov YuV, Malyshev IV, Dulobova IE, Petrukhin KE, et al.: The family of human Na+,K+-ATPase genes. No less than five genes and/or pseudogenes related to the alpha-subunit. FEBS Lett. 1987 Jun 15;217(2):275-8. [PubMed
]
- Ruiz A, Bhat SP, Bok D: Characterization and quantification of full-length and truncated Na,K-ATPase alpha 1 and beta 1 RNA transcripts expressed in human retinal pigment epithelium. Gene. 1995 Apr 3;155(2):179-84. [PubMed
]
|
| Target 1 Drug References |
- Ravikumar A, Arun P, Devi KV, Augustine J, Kurup PA: Isoprenoid pathway and free radical generation and damage in neuropsychiatric disorders. Indian J Exp Biol. 2000 May;38(5):438-46. [PubMed
]
- Chen JJ, Wang PS, Chien EJ, Wang SW: Direct inhibitory effect of digitalis on progesterone release from rat granulosa cells. Br J Pharmacol. 2001 Apr;132(8):1761-8. [PubMed
]
- Ke YS, Liu ZF, Yang H, Yang T, Huang JS, Rui SB, Cheng GH, Wang YX: Effect of anti-digoxin antiserum on endoxin and membrane ATPase activity in hypoxia-reoxygenation induced myocardial injury. Acta Pharmacol Sin. 2000 Apr;21(4):345-7. [PubMed
]
- Kumar AR, Kurup PA: A hypothalamic digoxin mediated model for conscious and subliminal perception. J Neural Transm. 2001;108(7):855-68. [PubMed
]
- Aizman O, Uhlen P, Lal M, Brismar H, Aperia A: Ouabain, a steroid hormone that signals with slow calcium oscillations. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13420-4. Epub 2001 Oct 30. [PubMed
]
|
|
Drug Target 2
[top]
|
| Target 2 ID |
1490 |
| Target 2 Name |
Solute carrier organic anion transporter family member 1B1 |
| Target 2 Synonyms |
- LST-1
- Liver-specific organic anion transporter 1
- OATP 2
- OATP-C
- Sodium-independent organic anion- transporting polypeptide 2
- Solute carrier family 21 member 6
|
| Target 2 Gene Name |
SLCO1B1 |
| Target 2 Protein Sequence |
>Solute carrier organic anion transporter family member 1B1
MDQNQHLNKTAEAQPSENKKTRYCNGLKMFLAALSLSFIAKTLGAIIMKSSIIHIERRFE
ISSSLVGFIDGSFEIGNLLVIVFVSYFGSKLHRPKLIGIGCFIMGIGGVLTALPHFFMGY
YRYSKETNINSSENSTSTLSTCLINQILSLNRASPEIVGKGCLKESGSYMWIYVFMGNML
RGIGETPIVPLGLSYIDDFAKEGHSSLYLGILNAIAMIGPIIGFTLGSLFSKMYVDIGYV
DLSTIRITPTDSRWVGAWWLNFLVSGLFSIISSIPFFFLPQTPNKPQKERKASLSLHVLE
TNDEKDQTANLTNQGKNITKNVTGFFQSFKSILTNPLYVMFVLLTLLQVSSYIGAFTYVF
KYVEQQYGQPSSKANILLGVITIPIFASGMFLGGYIIKKFKLNTVGIAKFSCFTAVMSLS
FYLLYFFILCENKSVAGLTMTYDGNNPVTSHRDVPLSYCNSDCNCDESQWEPVCGNNGIT
YISPCLAGCKSSSGNKKPIVFYNCSCLEVTGLQNRNYSAHLGECPRDDACTRKFYFFVAI
QVLNLFFSALGGTSHVMLIVKIVQPELKSLALGFHSMVIRALGGILAPIYFGALIDTTCI
KWSTNNCGTRGSCRTYNSTSFSRVYLGLSSMLRVSSLVLYIILIYAMKKKYQEKDINASE
NGSVMDEANLESLNKNKHFVPSAGADSETHC
|
| Target 2 Number of Residues |
702 |
| Target 2 Molecular Weight |
76450 |
| Target 2 Theoretical pI |
8.68 |
| Target 2 GO Classification |
|
Function
|
| transporter activity |
|
Process
|
physiological process
cellular physiological process
transport |
|
Component
|
cell
membrane
intrinsic to membrane
integral to membrane |
|
| Target 2 General Function |
Carbohydrate transport and metabolism |
| Target 2 Specific Function |
Mediates the Na(+)-independent transport of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. May play an important role in the clearance of bile acids and organic anions from the liver |
| Target 2 Pathways |
Not Available
|
| Target 2 Reactions |
Not Available |
| Target 2 Pfam Domain Function |
|
| Target 2 Signals |
|
| Target 2 Transmembrane Regions |
- 97-117
- 207-227
- 259-279
- 336-356
- 376-396
- 410-430
- 575-595
|
| Target 2 Essentiality |
Non-Essential |
| Target 2 GenBank ID Protein |
5051630  |
| Target 2 UniProtKB/Swiss-Prot ID |
Q9Y6L6  |
| Target 2 UniProtKB/Swiss-Prot Entry Name |
SO1B1_HUMAN  |
| Target 2 PDB ID |
Not Available |
| Target 2 Cellular Location |
- Cell membrane
- basolateral cell membrane
- multi-pass membrane protein. Note=Detected in basolateral
|
| Target 2 Gene Sequence |
>2076 bp
ATGGACCAAAATCAACATTTGAATAAAACAGCAGAGGCACAACCTTCAGAGAATAAGAAA
ACAAGATACTGCAATGGATTGAAGATGTTCTTGGCAGCTCTGTCACTCAGCTTTATTGCT
AAGACACTAGGTGCAATTATTATGAAAAGTTCCATCATTCATATAGAACGGAGATTTGAG
ATATCCTCTTCTCTTGTTGGTTTTATTGACGGAAGCTTTGAAATTGGAAATTTGCTTGTG
ATTGTATTTGTGAGTTACTTTGGATCCAAACTACATAGACCAAAGTTAATTGGAATCGGT
TGTTTCATTATGGGAATTGGAGGTGTTTTGACTGCTTTGCCACATTTCTTCATGGGATAT
TACAGGTATTCTAAAGAAACTAATATCAATTCATCAGAAAATTCAACATCGACCTTATCC
ACTTGTTTAATTAATCAAATTTTATCACTCAATAAAGCATCACCTGAGATAGTGGGAAAA
GGTTGTTTAAAGGAATCTGGGTCATACATGTGGATATATGTGTTCATGGGTAATATGCTT
CGTGGAATAGGGGAGACTCCCATAGTACCACTGGGGCTTTCTTACATTGATGATTTCGCT
AAAGAAGGACATTCTTCTTTGTATTTAGGTATATTGAATGCAATAGCAATGATTGGTCCA
ATCATTGGCTTTACCCTGGGATCTCTGTTTTCTAAAATGTACGTGGATATTGGATATGTT
AATCTAAGCACTATCAGGATAACTCCTACTGATTCTCGATGGGTTGGAGCTTGGTGGCTT
AATTTCCTTGTGTCTGGACTATTCTCCATTATTTCTTCCATACCATTCTTTTTCTTGCCC
CAAACTCCAAATAAACCACAAAAAGAAAGAAAAGCTTCACTGTCTTTGCATGTGCTGGAA
ACAAATGATGAAAAGGATCAAACAGCTAATTTGACCAATCAAGGAAAAAATATTACCAAA
AATGTGACTGGTTTTTTCCAGTCTTTTAAAAGCATCCTTACTAATCCCCTGTATGTTATG
TTTGTGCTTTTGACGTTGTTACAAGTAAGCAGCTATATTGGTGCTTTTACTTATGTCTTC
AAATACGTAGAGCAACAGTATGGTCAGCCTTCATCTAAGGCTAACATCTTATTGGGAGTC
ATAACCATACCTATTTTTGCAAGTGGAATGTTTTTAGGAGGATATATCATTAAAAAATTC
AAACTGAACACCGTTGGAATTGCCAAATTCTCATGTTTTACTGCTGTGATGTCATTGTCC
TTTTACCTATTATATTTTTTCATACTCTGTGAAAACAAATCAGTTGCCGGACTAACCATG
ACCTATGATGGAAATAATCCAGTGACATCTCATAGAGATGTACCACTTTCTTATTGCAAC
TCAGACTGCAATTGTGATGAAAGTCAATGGGAACCAGTCTGTGGAAACAATGGAATAACT
TACATCTCACCCTGTCTAGCAGGTTGCAAATCTTCAAGTGGCAATAAAAAGCCTATAGTG
TTTTACAACTGCAGTTGTTTGGAAGTAACTGGTCTCCAGAACAGAAATTACTCAGCCCAT
TTGGGTGAATGCCCAAGAGATGATGCTTGTACAAGGAAATTTTACTTTTTTGTTGCAATA
CAAGTCTTGAATTTATTTTTCTCTGCACTTGGAGGCACCTCACATGTCATGCTGATTGTT
AAAATTGTTCAACCTGAATTGAAATCACTTGCACTGGGTTTCCACTCAATGGTTATACGA
GCACTAGGAGGAATTCTAGCTCCTATATATTTTGGGGCTCTGATTGATACAACGTGTATA
AAGTGGTCCACCAACAACTGTGGCACACGTGGGTCATGTAGGACATATAATTCCACATCA
TTTTCAAGGGTCTACTTGGGCTTGTCTTCAATGTTAAGAGTCTCATCACTTGTTTTATAT
ATTATATTAATTTATGCCATGAAGAAAAAATATCAAGAGAAAGATATCAATGCATCAGAA
AATGGAAGTGTCATGGATGAAGCAAACTTAGAATCCTTAAATAAAAATAAACATTTTGTC
CCTTCTGCTGGGGCAGATAGTGAAACACATTGTTAA
|
| Target 2 GenBank Gene ID |
|
| Target 2 GeneCard ID |
SLCO1B1  |
| Target 2 GenAtlas ID |
SLCO1B1  |
| Target 2 HGNC ID |
HGNC:10959  |
| Target 2 Chromosome Location |
12 |
| Target 2 Locus |
12p |
| Target 2 SNPs |
SNPJam Report  |
| Target 2 General References |
- Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, Nomura H, Unno M, Suzuki M, Naitoh T, Matsuno S, Yawo H: Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem. 1999 Jun 11;274(24):17159-63. [PubMed
]
- Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed
]
- Konig J, Cui Y, Nies AT, Keppler D: A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. Am J Physiol Gastrointest Liver Physiol. 2000 Jan;278(1):G156-64. [PubMed
]
- Konig J, Cui Y, Nies AT, Keppler D: Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide. J Biol Chem. 2000 Jul 28;275(30):23161-8. [PubMed
]
- Tirona RG, Leake BF, Merino G, Kim RB: Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans. J Biol Chem. 2001 Sep 21;276(38):35669-75. Epub 2001 Jul 26. [PubMed
]
- Nozawa T, Nakajima M, Tamai I, Noda K, Nezu J, Sai Y, Tsuji A, Yokoi T: Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis. J Pharmacol Exp Ther. 2002 Aug;302(2):804-13. [PubMed
]
- Michalski C, Cui Y, Nies AT, Nuessler AK, Neuhaus P, Zanger UM, Klein K, Eichelbaum M, Keppler D, Konig J: A naturally occurring mutation in the SLC21A6 gene causing impaired membrane localization of the hepatocyte uptake transporter. J Biol Chem. 2002 Nov 8;277(45):43058-63. Epub 2002 Aug 23. [PubMed
]
|
| Target 2 Drug References |
- Dagenais C, Ducharme J, Pollack GM: Uptake and efflux of the peptidic delta-opioid receptor agonist. Neurosci Lett. 2001 Apr 6;301(3):155-8. [PubMed
]
- Sugiyama D, Kusuhara H, Shitara Y, Abe T, Meier PJ, Sekine T, Endou H, Suzuki H, Sugiyama Y: Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier. J Pharmacol Exp Ther. 2001 Jul;298(1):316-22. [PubMed
]
- Hagenbuch N, Reichel C, Stieger B, Cattori V, Fattinger KE, Landmann L, Meier PJ, Kullak-Ublick GA: Effect of phenobarbital on the expression of bile salt and organic anion transporters of rat liver. J Hepatol. 2001 Jun;34(6):881-7. [PubMed
]
- Gao B, Wenzel A, Grimm C, Vavricka SR, Benke D, Meier PJ, Reme CE: Localization of organic anion transport protein 2 in the apical region of rat retinal pigment epithelium. Invest Ophthalmol Vis Sci. 2002 Feb;43(2):510-4. [PubMed
]
- Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y: Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res. 2002 Feb;19(2):147-53. [PubMed
]
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