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Identification
Name Indomethacin
Accession Number DB00328 (APRD00109)
Type small molecule
Groups approved
Description

Indomethacin is a non-steroidal antiinflammatory agent (NSAIA) with antiinflammatory, analgesic and antipyretic activity. Its pharmacological effect is thought to be mediated through inhibition of the enzyme cyclooxygenase (COX), the enzyme responsible for catalyzes the rate-limiting step in prostaglandin synthesis via the arachidonic acid pathway.
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
IMN
Indometacine
Indometacyna
Indomethacine
Indomethacinum
Indomethancin
Indomethazine
Indomethine
Indometicina
Salts Not Available
Brand names
Name Company
Amuno
Apo-Indomethacin
Arthrexin
Artracin
Artrinovo
Artrivia
Bonidin
Bonidon
Bonidon Gel
Catlep
Chibro-Amuno
Chrono-Indicid
Chrono-Indocid
Confortid
Dolcidium
Dolcidium Pl
Dolovin
Durametacin
Elmetacin
Flexin Continus
Hicin
Idomethine
Imbrilon
Inacid
Indacin
Indaflex
Indameth
Indmethacine
Indo-Lemmon
Indo-Phlogont
Indo-Rectolmin
Indo-Spray
Indo-Tablinen
Indocid
Indocid Pda
Indocid Sr
Indocin
Indocin I.V
Indocin I.V.
Indocin Sr
Indolar Sr
Indomecol
Indomed
Indomee
Indomethegan
Indomo
Indomod
Indoptic
Indoptol
Indorektal
Indoxen
Inflazon
Infrocin
Inteban Sp
Lausit
Liometacen
Metacen
Metartril
Methazine
Metindol
Miametan
Mikametan
Mobilan
Novo-Methacin
Novomethacin
Nu-Indo
Reumacide
Rhemacin La
Rheumacin La
Sadoreum
Tannex
Vonum
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Brand mixtures Not Available
Categories
  • Anti-inflammatory Agents
  • Cyclooxygenase Inhibitors
  • Tocolytic Agents
  • Cardiovascular Agents
  • Nonsteroidal Anti-inflammatory Agents (NSAIAs)
  • Gout Suppressants
CAS number 53-86-1
Weight Average: 357.788
Monoisotopic: 357.076785712
Chemical Formula C19H16ClNO4
InChI Key InChIKey=CGIGDMFJXJATDK-UHFFFAOYSA-N
InChI
InChI=1S/C19H16ClNO4/c1-11-15(10-18(22)23)16-9-14(25-2)7-8-17(16)21(11)19(24)12-3-5-13(20)6-4-12/h3-9H,10H2,1-2H3,(H,22,23)
Plain Text
IUPAC Name
2-{1-[(4-chlorophenyl)carbonyl]-5-methoxy-2-methyl-1H-indol-3-yl}acetic acid
SMILES
COC1=CC2=C(C=C1)N(C(=O)C1=CC=C(Cl)C=C1)C(C)=C2CC(O)=O
Plain Text
Mass Spec show (7.7 KB)
Taxonomy
Kingdom Organic
Classes
  • Indoles and Indole Derivatives
Substructures
  • Hydroxy Compounds
  • Acetates
  • Indoles and Indole Derivatives
  • Phenols and Derivatives
  • Amino Ketones
  • Carboxylic Acids and Derivatives
  • Pyrroles
  • Ethers
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Heterocyclic compounds
  • Aromatic compounds
  • Anisoles
  • Carboxamides and Derivatives
  • Imines
  • Benzoyl Derivatives
  • Phenyl Esters
  • Benzamides
Pharmacology
Indication For moderate to severe rheumatoid arthritis including acute flares of chronic disease, ankylosing spondylitis, osteoarthritis, acute painful shoulder (bursitis and/or tendinitis) and acute gouty arthritis.
Pharmacodynamics Indomethacin, a NSAIA, with analgesic and antipyretic properties exerts its pharmacological effects by inhibiting the synthesis of prostaglandins involved in pain, fever, and inflammation. Indomethacin inhibits the catalytic activity of the COX enzymes, the enzymes responsible for catalyzing the rate-limiting step in prostaglandin synthesis via the arachidonic acid pathway. Indomethacin is known to inhibit two well-characterized isoforms of COX, COX-1 and COX-2, with greater selectivity for COX-1. COX-1 is a constitutively expressed enzyme that is involved in gastric mucosal protection, platelet and kidney function. It catalyzes the conversion of arachidonic acid to prostaglandin (PG) G2 and PGG2 to PGH2. COX-1 is involved in the synthesis pathways of PGE2, PGD2, PDF2a, PGI2 (also known as prostacyclin) and thromboxane A2 (TXA2). COX-2 is constitutively expressed and highly inducible by inflammatory stimuli. It is found in the central nervous system, kidneys, uterus and other organs. It also catalyzes the conversion of arachidonic acid to PGG2 and PGG2 to PGH2. In the COX-2-mediated pathway, PGH2 is subsequently converted to PGE2 and PGI2 (also known as prostacyclin). PGE2 is involved in mediating inflammation, pain and fever. Decreasing levels of PGE2 leads to decreased inflammation.
Mechanism of action Indomethacin is a prostaglandin G/H synthase (also known as cyclooxygenase or COX) inhibitor that acts on both prostaglandin G/H synthase 1 and 2 (COX-1 and -2). Prostaglandin G/H synthase catalyzes the conversion of arachidonic acid to a number of prostaglandins involved in fever, pain, swelling, inflammation, and platelet aggregation. Indomethacin antagonizes COX by binding to the upper portion of the active site, preventing its substrate, arachidonic acid, from entering the active site. Indomethacin, unlike other NSAIDs, also inhibits phospholipase A2, the enzyme responsible for releasing arachidonic acid from phospholipids. Indomethacin is more selective for COX-1 than COX-2, which accounts for its increased adverse gastric effects relative to other NSAIDs. COX-1 is required for maintaining the protective gastric mucosal layer. The analgesic, antipyretic and anti-inflammatory effects of indomethacin occur as a result of decreased prostaglandin synthesis. Its antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Absorption Bioavailability is approximately 100% following oral administration and 80–90% following rectal administration.
Volume of distribution Not Available
Protein binding 97%
Metabolism
Hepatic.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Indomethacin
O-Desmethylindomethacin Details
Indomethacin
Indomethacin acyl glucuronide Details
Indomethacin
N-Deschlorobenzoyl indomethacin Details
Indomethacin
    		Isovalerylglucuronide Details
    Route of elimination Indomethacin is eliminated via renal excretion, metabolism, and biliary excretion.
    Half life 4.5 hours
    Clearance Not Available
    Toxicity The following symptoms may be observed following overdosage: nausea, vomiting, intense headache, dizziness, mental confusion, disorientation, or lethargy. There have been reports of paresthesias, numbness, and convulsions. The oral LD50 of indomethacin in mice and rats (based on 14 day mortality response) was 50 and 12 mg/kg, respectively.
    Affected organisms
    • Humans and other mammals
    Pathways
    Pathway Name SMPDB ID
    Smp00104 Indomethacin Pathway SMP00104
    Pharmacoeconomics
    Manufacturers
    • Iroko pharmaceuticals llc
    • Sandoz inc
    • Able laboratories inc
    • Avanthi inc
    • Inwood laboratories inc sub forest laboratories inc
    • Teva pharmaceuticals usa inc
    • Duramed pharmaceuticals inc sub barr laboratories inc
    • Halsey drug co inc
    • Heritage pharmaceuticals inc
    • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
    • Mutual pharmaceutical co inc
    • Mylan pharmaceuticals inc
    • Parke davis div warner lambert co
    • Pioneer pharmaceuticals inc
    • Pliva inc
    • Roxane laboratories inc
    • Superpharm corp
    • Vintage pharmaceuticals llc
    • Watson laboratories inc
    • App pharmaceuticals llc
    • G and w laboratories inc
    • Lundbeck inc
    • Bedford laboratories div ben venue laboratories inc
    Packagers
    Dosage forms
    Form Route Strength
    Capsule Oral 25 mg
    Capsule Oral 50 mg
    Capsule, extended release Oral 75 mg
    Injection Intravenous 1 mg
    Suppository Rectal 100 mg
    Suppository Rectal 50 mg
    Suspension Oral 25 mg/5 ml
    Prices
    Unit description Cost Unit
    Indocin i.v. 1 mg vial 642.6 USD vial
    Indomethacin 1 mg vial 600.0 USD vial
    Indocin 50 mg suppository 9.56 USD suppository
    Indomethacin CR 75 mg capsule 3.12 USD capsule
    Indocin sr 75 mg capsule 2.92 USD capsule
    Indomethacin powder 2.57 USD g
    Ratio-Indomethacin 100 mg Suppository 0.93 USD suppository
    Sandoz Indomethacin 100 mg Suppository 0.93 USD suppository
    Sandoz Indomethacin 50 mg Suppository 0.93 USD suppository
    Indomethacin 50 mg capsule 0.65 USD capsule
    Indomethacin 25 mg capsule 0.44 USD capsule
    Apo-Indomethacin 50 mg Capsule 0.16 USD capsule
    Novo-Methacin 50 mg Capsule 0.16 USD capsule
    Nu-Indo 50 mg Capsule 0.16 USD capsule
    Apo-Indomethacin 25 mg Capsule 0.09 USD capsule
    Novo-Methacin 25 mg Capsule 0.09 USD capsule
    Nu-Indo 25 mg Capsule 0.09 USD capsule
    First Prev Next Last
    DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
    Patents Not Available
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 158 °C PhysProp
    water solubility 0.937 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 4.27 HANSCH,C ET AL. (1995)
    logS -4.62 ADME Research, USCD
    Caco2 permeability -4.69 ADME Research, USCD
    pKa 4.5 BUDAVARI,S ET AL. (1989)
    Predicted Properties
    Property Value Source
    water solubility 2.40e-03 g/l ALOGPS
    logP 4.25 ALOGPS
    logP 3.53 ChemAxon
    logS -5.2 ALOGPS
    pKa (strongest acidic) 3.8 ChemAxon
    pKa (strongest basic) -2.3 ChemAxon
    physiological charge -1 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 68.53 ChemAxon
    rotatable bond count 4 ChemAxon
    refractivity 94.81 ChemAxon
    polarizability 36.64 ChemAxon
    References
    Synthesis Reference Not Available
    General Reference
    1. Akbarpour F, Afrasiabi A, Vaziri ND: Severe hyperkalemia caused by indomethacin and potassium supplementation. South Med J. 1985 Jun;78(6):756-7. Pubmed
    2. HART FD, BOARDMAN PL: INDOMETHACIN: A NEW NON-STEROID ANTI-INFLAMMATORY AGENT. Br Med J. 1963 Oct 19;2(5363):965-70. Pubmed
    3. Lum GM, Aisenbrey GA, Dunn MJ, Berl T, Schrier RW, McDonald KM: In vivo effect of indomethacin to potentiate the renal medullary cyclic AMP response to vasopressin. J Clin Invest. 1977 Jan;59(1):8-13. Pubmed
    4. Phelan KM, Mosholder AD, Lu S: Lithium interaction with the cyclooxygenase 2 inhibitors rofecoxib and celecoxib and other nonsteroidal anti-inflammatory drugs. J Clin Psychiatry. 2003 Nov;64(11):1328-34. Pubmed
    5. Ragheb M: The clinical significance of lithium-nonsteroidal anti-inflammatory drug interactions. J Clin Psychopharmacol. 1990 Oct;10(5):350-4. Pubmed
    External Links
    Resource Link
    KEGG Drug D00141 Link_out
    KEGG Compound C01926 Link_out
    PubChem Compound 3715 Link_out
    PubChem Substance 46508291 Link_out
    ChemSpider 3584 Link_out
    BindingDB 17638 Link_out
    ChEBI 5918 Link_out
    ChEMBL 5918 Link_out
    Therapeutic Targets Database DAP000617 Link_out
    PharmGKB PA449982 Link_out
    IUPHAR 1909 Link_out
    Guide to Pharmacology 1909 Link_out
    Drug Product Database 2143372 Link_out
    RxList http://www.rxlist.com/cgi/generic/indometh.htm Link_out
    Drugs.com http://www.drugs.com/cdi/indomethacin.html Link_out
    Wikipedia http://en.wikipedia.org/wiki/Indomethacin Link_out
    ATC Codes
    • M01AB01
    • C01EB03
    AHFS Codes
    • 28:08.04.92
    PDB Entries Not Available
    FDA label show (56.2 KB)
    MSDS show (73.2 KB)
    Interactions
    Drug Interactions
    Drug Interaction
    Acebutolol Risk of inhibition of renal prostaglandins
    Acenocoumarol The NSAID, indomethacin, may increase the anticoagulant effect of acenocoumarol.
    Alendronate Increased risk of gastric toxicity
    Anisindione The NSAID, indomethacin, may increase the anticoagulant effect of anisindione.
    Atenolol Risk of inhibition of renal prostaglandins
    Azilsartan medoxomil Increases toxicity of each. May deteriorate renal function, particularly in volume depleted or elderly patients. Decreases effects of azilsartan by antagonism.
    Betaxolol Nonsteroidal Anti-Inflammatory Agents such as indomethacin may diminish the antihypertensive effect of Beta-Blockers such as betaxolol. Monitor for increases in blood pressure if a nonsteroidal anti-inflammatory agent (NSAID) is initiated/dose increased, or decreases in blood pressure if a NSAID is discontinued/dose decreased; this is particularly important if NSAID treatment is for extended periods of time. Ophthalmic beta-blockers are likely of little concern.
    Bevantolol Risk of inhibition of renal prostaglandins
    Bisoprolol Risk of inhibition of renal prostaglandins
    Bumetanide The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, bumetanide.
    Carteolol Risk of inhibition of renal prostaglandins
    Carvedilol Risk of inhibition of renal prostaglandins
    Colesevelam Bile acid sequestrants may decrease the absorption of Nonsteroidal Anti-Inflammatory Agents. Monitor for decreased serum concentrations/therapeutic effects of nonsteroidal anti-inflammatory agents (NSAID) if coadministered with bile acid sequestrants. Separating the administration of doses by 2 or more hours may reduce (but not eliminate) the risk of interaction. The manufacturer of colesevelam recommends that drugs should be administered at least 1 hour before or 4 hours after colesevelam.
    Cyclosporine Monitor for nephrotoxicity
    Dicumarol The NSAID, indomethacin, may increase the anticoagulant effect of dicumarol.
    Diflunisal Concomitant therapy with the two NSAIDs, indomethacin and diflunisal, increases the risk of NSAID-related adverse effects (e.g. GI ulcers, bleeds, increased blood pressure).
    Eltrombopag Increases levels of Indomethacin via metabolism decrease. UDP-glucuronosyltransferase inhibition with unclear significance.
    Esmolol Risk of inhibition of renal prostaglandins
    Ethacrynic acid The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, ethacrynic acid.
    Furosemide The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, furosemide.
    Ginkgo biloba Additive anticoagulant/antiplatelet effects may increase bleed risk. Concomitant therapy should be avoided.
    Labetalol Risk of inhibition of renal prostaglandins
    Lithium The NSAID, indomethacin, may decrease the renal excretion of lithium. Increased risk of lithium toxicity.
    Losartan Indomethacin decreases the effect of losartan
    Methotrexate The NSAID, indomethacin, may decrease the renal excretion of methotrexate. Increased risk of methotrexate toxicity.
    Metoprolol Risk of inhibition of renal prostaglandins
    Nadolol Risk of inhibition of renal prostaglandins
    Oxprenolol Risk of inhibition of renal prostaglandins
    Penbutolol Risk of inhibition of renal prostaglandins
    Pindolol Risk of inhibition of renal prostaglandins
    Practolol Risk of inhibition of renal prostaglandins
    Pralatrexate NSAIDs increase the risk of toxicity due to impairment of renal clearance of pralatrexate thus increasing exposure. Monitor for adverse effects or adjust dose of pralatrexate.
    Probenecid Probenecid increases the effect/toxicity of indomethacin
    Propranolol Risk of inhibition of renal prostaglandins
    Sotalol Risk of inhibition of renal prostaglandins
    Tamoxifen Indomethacin may reduce clearance rate of Tamoxifen. Monitor for changes in therapeutic/adverse effects of Tamoxifen if Indomethacin is initiated, discontinued or dose changed.
    Telmisartan Concomitant use of Telmisartan and Indomethacin may increase the risk of acute renal failure and hyperkalemia. Monitor renal function at the beginning and during treatment.
    Timolol Risk of inhibition of renal prostaglandins
    Tolbutamide Indomethacin, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Indomethacin is initiated, discontinued or dose changed.
    Torasemide The NSAID, indomethacin, may decrease the diuretic and antihypertensive effects of the loop diuretic, torasemide.
    Trandolapril The NSAID, Indomethacin, may reduce the antihypertensive effect of Trandolapril. Consider alternate therapy or monitor for changes in Trandolapril efficacy if Indomethacin is initiated, discontinued or dose changed.
    Treprostinil The prostacyclin analogue, Treprostinil, may increase the risk of bleeding when combined with the NSAID, Indomethacin. Monitor for increased bleeding during concomitant thearpy.
    Triamterene Risk of acute renal impairment with this combination
    Trimethoprim The strong CYP2C9 inhibitor, Indomethacine, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Indomethacine is initiated, discontinued or dose changed.
    Voriconazole Indomethacin, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole if indomethacin is initiated, discontinued or dose changed.
    Warfarin Indomethacin, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. The antiplatelet effect of indomethacin may also increase the bleed risk associated with warfarin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if indomethacin is initiated, discontinued or dose changed.
    Food Interactions
    • Avoid alcohol.
    • Take with food or antacids to reduce irritation.
    Targets

    1. Prostaglandin G/H synthase 1

    Pharmacological action: unknown
    Actions: inhibitor

    May play an important role in regulating or promoting cell proliferation in some normal and neoplastically transformed cells

    Organism class: human
    UniProt ID: P23219 Link_out
    Gene: PTGS1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Bobadilla L RA, Perez-Alvarez V, Bracho Valdes I, Lopez-Sanchez P: Effect of pregnancy on the roles of nitric oxide and prostaglandins in 5-hydroxytryptamine-induced contractions in rat isolated thoracic and abdominal aorta. Clin Exp Pharmacol Physiol. 2005 Mar;32(3):202-9. Pubmed
    2. Fornai M, Blandizzi C, Colucci R, Antonioli L, Bernardini N, Segnani C, Baragatti B, Barogi S, Berti P, Spisni R, Del Tacca M: Role of cyclooxygenases 1 and 2 in the modulation of neuromuscular functions in the distal colon of humans and mice. Gut. 2005 May;54(5):608-16. Pubmed
    3. Higuchi K, Tominaga K, Watanabe T, Uno H, Shiba M, Sasaki E, Tanigawa T, Takashima T, Hamaguchi M, Oshitani N, Matsumoto T, Iwanaga Y, Fukuda T, Fujiwara Y, Arakawa T: Indomethacin, but not Helicobacter pylori, inhibits adaptive relaxation in isolated guinea-pig stomach. Drugs Exp Clin Res. 2004;30(5-6):235-41. Pubmed
    4. Kundu N, Walser TC, Ma X, Fulton AM: Cyclooxygenase inhibitors modulate NK activities that control metastatic disease. Cancer Immunol Immunother. 2005 Oct;54(10):981-7. Epub 2005 May 13. Pubmed
    5. Moth CW, Prusakiewicz JJ, Marnett LJ, Lybrand TP: Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1. J Med Chem. 2005 May 19;48(10):3613-20. Pubmed

    2. Prostaglandin G/H synthase 2

    Pharmacological action: yes
    Actions: inhibitor

    May have a role as a major mediator of inflammation and/or a role for prostanoid signaling in activity-dependent plasticity

    Organism class: human
    UniProt ID: P35354 Link_out
    Gene: PTGS2 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Armstrong PJ, Franklin DP, Carey DJ, Elmore JR: Suppression of experimental aortic aneurysms: comparison of inducible nitric oxide synthase and cyclooxygenase inhibitors. Ann Vasc Surg. 2005 Mar;19(2):248-57. Pubmed
    2. Jerde TJ, Calamon-Dixon JL, Bjorling DE, Nakada SY: Celecoxib inhibits ureteral contractility and prostanoid release. Urology. 2005 Jan;65(1):185-90. Pubmed
    3. Pilane CM, Labelle EF: Nitric oxide stimulated vascular smooth muscle cells undergo apoptosis induced in part by arachidonic acid derived eicosanoids. J Cell Physiol. 2005 Aug;204(2):423-7. Pubmed
    4. Yokota A, Taniguchi M, Takahira Y, Tanaka A, Takeuchi K: Rofecoxib produces intestinal but not gastric damage in the presence of a low dose of indomethacin in rats. J Pharmacol Exp Ther. 2005 Jul;314(1):302-9. Epub 2005 Apr 14. Pubmed
    5. Zhang GS, Fu YB, Xia M: [Proliferation inhibition effect of indomethacin on CML cells associated with down-regulation of phosphorylated STAT1/STAT5 and inhibition of COX-2 expression.] Zhonghua Xue Ye Xue Za Zhi. 2004 Dec;25(12):732-5. Pubmed

    3. Phospholipase A2, membrane associated

    Pharmacological action: yes
    Actions: inhibitor

    Thought to participate in the regulation of the phospholipid metabolism in biomembranes including eicosanoid biosynthesis. Catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides

    Organism class: human
    UniProt ID: P14555 Link_out
    Gene: PLA2G2A Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Geisslinger, G., & Lötsch, J. (2004). Non-steroidal anti-inflammatory drugs. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (pp. 667-671). Berlin, Germany: Springer.

    4. Prostaglandin reductase 2

    Pharmacological action: unknown
    Actions: inhibitor

    Functions as 15-oxo-prostaglandin 13-reductase and acts on 15-keto-PGE1, 15-keto-PGE2, 15-keto-PGE1-alpha and 15-keto- PGE2-alpha with highest activity towards 15-keto-PGE2. Overexpression represses transcriptional activity of PPARG and inhibits adipocyte differentiation (By similarity)

    Organism class: human
    UniProt ID: Q8N8N7 Link_out
    Gene: PTGR2 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Wu YH, Ko TP, Guo RT, Hu SM, Chuang LM, Wang AH: Structural basis for catalytic and inhibitory mechanisms of human prostaglandin reductase PTGR2. Structure. 2008 Nov 12;16(11):1714-23. Pubmed

    5. Peroxisome proliferator-activated receptor gamma

    Pharmacological action: unknown
    Actions: activator

    Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Once activated by a ligand, the receptor binds to a promoter element in the gene for acyl-CoA oxidase and activates its transcription. It therefore controls the peroxisomal beta-oxidation pathway of fatty acids. Key regulator of adipocyte differentiation and glucose homeostasis

    Organism class: human
    UniProt ID: P37231 Link_out
    Gene: PPARG Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Cho MC, Lee HS, Kim JH, Choe YK, Hong JT, Paik SG, Yoon DY: A simple ELISA for screening ligands of peroxisome proliferator-activated receptor-gamma. J Biochem Mol Biol. 2003 Mar 31;36(2):207-13. Pubmed

    6. Lactoylglutathione lyase

    Pharmacological action: unknown
    Actions: inhibitor

    Catalyzes the conversion of hemimercaptal, formed from methylglyoxal and glutathione, to S-lactoylglutathione

    Organism class: human
    UniProt ID: Q04760 Link_out
    Gene: GLO1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Sato S, Kwon Y, Kamisuki S, Srivastava N, Mao Q, Kawazoe Y, Uesugi M: Polyproline-rod approach to isolating protein targets of bioactive small molecules: isolation of a new target of indomethacin. J Am Chem Soc. 2007 Jan 31;129(4):873-80. Pubmed

    7. Putative G-protein coupled receptor 44

    Pharmacological action: unknown
    Actions: other/unknown

    Orphan receptor

    Organism class: human
    UniProt ID: Q9Y5Y4 Link_out
    Gene: GPR44 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Hata AN, Lybrand TP, Breyer RM: Identification of determinants of ligand binding affinity and selectivity in the prostaglandin D2 receptor CRTH2. J Biol Chem. 2005 Sep 16;280(37):32442-51. Epub 2005 Jul 19. Pubmed
    2. Hata AN, Lybrand TP, Marnett LJ, Breyer RM: Structural determinants of arylacetic acid nonsteroidal anti-inflammatory drugs necessary for binding and activation of the prostaglandin D2 receptor CRTH2. Mol Pharmacol. 2005 Mar;67(3):640-7. Epub 2004 Nov 24. Pubmed
    3. Mathiesen JM, Ulven T, Martini L, Gerlach LO, Heinemann A, Kostenis E: Identification of indole derivatives exclusively interfering with a G protein-independent signaling pathway of the prostaglandin D2 receptor CRTH2. Mol Pharmacol. 2005 Aug;68(2):393-402. Epub 2005 May 3. Pubmed
    Enzymes

    1. Cytochrome P450 2C19

    Actions: substrate, inhibitor

    Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine

    UniProt ID: P33261 Link_out
    Gene: CYP2C19 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
    2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

    2. Cytochrome P450 2C9

    Actions: substrate

    Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

    UniProt ID: P11712 Link_out
    Gene: CYP2C9
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

    3. Liver carboxylesterase 1

    Actions: substrate

    Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl CoA ester

    UniProt ID: P23141 Link_out
    Gene: CES1
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed

    4. UDP-glucuronosyltransferase 1-9

    Actions: substrate

    UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols

    UniProt ID: O60656 Link_out
    Gene: UGT1A9 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Mano Y, Usui T, Kamimura H: Contribution of UDP-glucuronosyltransferases 1A9 and 2B7 to the glucuronidation of indomethacin in the human liver. Eur J Clin Pharmacol. 2007 Mar;63(3):289-96. Epub 2007 Jan 24. Pubmed

    5. UDP-glucuronosyltransferase 1-1

    Actions: substrate, inhibitor

    UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX- alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate

    UniProt ID: P22309 Link_out
    Gene: UGT1A1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. Pubmed
    2. Mano Y, Usui T, Kamimura H: In vitro inhibitory effects of non-steroidal antiinflammatory drugs on UDP-glucuronosyltransferase 1A1-catalysed estradiol 3beta-glucuronidation in human liver microsomes. Biopharm Drug Dispos. 2005 Jan;26(1):35-9. Pubmed

    6. UDP-glucuronosyltransferase 2B7

    Actions: substrate, inhibitor

    Its unique specificity for 3,4-catechol estrogens and estriol suggests it may play an important role in regulating the level and activity of these potent and active estrogen metabolites

    UniProt ID: P16662 Link_out
    Gene: UGT2B7 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Mano Y, Usui T, Kamimura H: Contribution of UDP-glucuronosyltransferases 1A9 and 2B7 to the glucuronidation of indomethacin in the human liver. Eur J Clin Pharmacol. 2007 Mar;63(3):289-96. Epub 2007 Jan 24. Pubmed
    2. Mano Y, Usui T, Kamimura H: Inhibitory potential of nonsteroidal anti-inflammatory drugs on UDP-glucuronosyltransferase 2B7 in human liver microsomes. Eur J Clin Pharmacol. 2007 Feb;63(2):211-6. Epub 2007 Jan 3. Pubmed
    Transporters

    1. Canalicular multispecific organic anion transporter 2

    Actions: inhibitor

    May act as an inducible transporter in the biliary and intestinal excretion of organic anions

    UniProt ID: O15438 Link_out
    Gene: ABCC3 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Zelcer N, Saeki T, Reid G, Beijnen JH, Borst P: Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3). J Biol Chem. 2001 Dec 7;276(49):46400-7. Pubmed
    2. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. Pubmed

    2. Multidrug resistance-associated protein 4

    Actions: inhibitor

    May be an organic anion pump relevant to cellular detoxification

    UniProt ID: O15439 Link_out
    Gene: ABCC4 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. Pubmed
    2. Bai J, Lai L, Yeo HC, Goh BC, Tan TM: Multidrug resistance protein 4 (MRP4/ABCC4) mediates efflux of bimane-glutathione. Int J Biochem Cell Biol. 2004 Feb;36(2):247-57. Pubmed
    3. Ose A, Ito M, Kusuhara H, Yamatsugu K, Kanai M, Shibasaki M, Hosokawa M, Schuetz JD, Sugiyama Y: Limited brain distribution of [3R,4R,5S]-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxyl ate phosphate (Ro 64-0802), a pharmacologically active form of oseltamivir, by active efflux across the blood-brain barrier mediated by organic anion transporter 3 (Oat3/Slc22a8) and multidrug resistance-associated protein 4 (Mrp4/Abcc4). Drug Metab Dispos. 2009 Feb;37(2):315-21. Epub 2008 Nov 24. Pubmed

    3. Multidrug resistance-associated protein 6

    Actions: inhibitor

    May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4) and N-ethylmaleimide S-glutathione (NEM-GS)

    UniProt ID: O95255 Link_out
    Gene: ABCC6 Link_out
    Protein Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Ilias A, Urban Z, Seidl TL, Le Saux O, Sinko E, Boyd CD, Sarkadi B, Varadi A: Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). J Biol Chem. 2002 May 10;277(19):16860-7. Epub 2002 Mar 5. Pubmed

    4. Multidrug resistance protein 1

    Actions: substrate, inhibitor

    Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells

    UniProt ID: P08183 Link_out
    Gene: ABCB1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Wang EJ, Casciano CN, Clement RP, Johnson WW: Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors. Biochem Biophys Res Commun. 2001 Nov 30;289(2):580-5. Pubmed
    2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. Pubmed

    5. Multidrug resistance-associated protein 1

    Actions: inhibitor

    May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Confers resistance to anticancer drugs. Transports LTC4. May protect milk against xenobiotics

    UniProt ID: P33527 Link_out
    Gene: ABCC1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Evers R, de Haas M, Sparidans R, Beijnen J, Wielinga PR, Lankelma J, Borst P: Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. Br J Cancer. 2000 Aug;83(3):375-83. Pubmed
    2. Hong J, Lambert JD, Lee SH, Sinko PJ, Yang CS: Involvement of multidrug resistance-associated proteins in regulating cellular levels of (-)-epigallocatechin-3-gallate and its methyl metabolites. Biochem Biophys Res Commun. 2003 Oct 10;310(1):222-7. Pubmed
    3. Ilias A, Urban Z, Seidl TL, Le Saux O, Sinko E, Boyd CD, Sarkadi B, Varadi A: Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). J Biol Chem. 2002 May 10;277(19):16860-7. Epub 2002 Mar 5. Pubmed
    4. Reid G, Wielinga P, Zelcer N, van der Heijden I, Kuil A, de Haas M, Wijnholds J, Borst P: The human multidrug resistance protein MRP4 functions as a prostaglandin efflux transporter and is inhibited by nonsteroidal antiinflammatory drugs. Proc Natl Acad Sci U S A. 2003 Aug 5;100(16):9244-9. Epub 2003 Jun 30. Pubmed
    5. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. Pubmed

    6. Solute carrier organic anion transporter family member 1A2

    Actions: substrate, inhibitor

    Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity)

    UniProt ID: P46721 Link_out
    Gene: SLCO1A2 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. 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
    2. Kouzuki H, Suzuki H, Sugiyama Y: Pharmacokinetic study of the hepatobiliary transport of indomethacin. Pharm Res. 2000 Apr;17(4):432-8. Pubmed

    7. Solute carrier family 22 member 6

    Actions: inhibitor
    UniProt ID: Q4U2R8 Link_out
    Gene: hROAT1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Mulato AS, Ho ES, Cihlar T: Nonsteroidal anti-inflammatory drugs efficiently reduce the transport and cytotoxicity of adefovir mediated by the human renal organic anion transporter 1. J Pharmacol Exp Ther. 2000 Oct;295(1):10-5. Pubmed
    2. Jung KY, Takeda M, Kim DK, Tojo A, Narikawa S, Yoo BS, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001 Sep 21;69(18):2123-35. Pubmed
    3. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
    4. Hosoyamada M, Sekine T, Kanai Y, Endou H: Molecular cloning and functional expression of a multispecific organic anion transporter from human kidney. Am J Physiol. 1999 Jan;276(1 Pt 2):F122-8. Pubmed
    5. Lu R, Chan BS, Schuster VL: Cloning of the human kidney PAH transporter: narrow substrate specificity and regulation by protein kinase C. Am J Physiol. 1999 Feb;276(2 Pt 2):F295-303. Pubmed
    6. Sandhu P, Lee W, Xu X, Leake BF, Yamazaki M, Stone JA, Lin JH, Pearson PG, Kim RB: Hepatic uptake of the novel antifungal agent caspofungin. Drug Metab Dispos. 2005 May;33(5):676-82. Epub 2005 Feb 16. Pubmed
    7. Kuze K, Graves P, Leahy A, Wilson P, Stuhlmann H, You G: Heterologous expression and functional characterization of a mouse renal organic anion transporter in mammalian cells. J Biol Chem. 1999 Jan 15;274(3):1519-24. Pubmed
    8. Uwai Y, Saito H, Inui K: Interaction between methotrexate and nonsteroidal anti-inflammatory drugs in organic anion transporter. Eur J Pharmacol. 2000 Dec 1;409(1):31-6. Pubmed
    9. Apiwattanakul N, Sekine T, Chairoungdua A, Kanai Y, Nakajima N, Sophasan S, Endou H: Transport properties of nonsteroidal anti-inflammatory drugs by organic anion transporter 1 expressed in Xenopus laevis oocytes. Mol Pharmacol. 1999 May;55(5):847-54. Pubmed

    8. Solute carrier family 22 member 8

    Actions: inhibitor

    Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone- 3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA)

    UniProt ID: Q8TCC7 Link_out
    Gene: SLC22A8 Link_out
    Protein Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. Pubmed
    2. Jung KY, Takeda M, Kim DK, Tojo A, Narikawa S, Yoo BS, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of ochratoxin A transport by human organic anion transporters. Life Sci. 2001 Sep 21;69(18):2123-35. Pubmed
    3. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
    4. Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. Pubmed
    5. Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. Pubmed
    6. Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. Pubmed

    9. Canalicular multispecific organic anion transporter 1

    Actions: substrate, inhibitor

    Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter

    UniProt ID: Q92887 Link_out
    Gene: ABCC2 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. Pubmed
    2. Dahan A, Amidon GL: Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G371-7. Epub 2009 Jun 18. Pubmed
    3. Dahan A, Sabit H, Amidon GL: The H2 receptor antagonist nizatidine is a P-glycoprotein substrate: characterization of its intestinal epithelial cell efflux transport. AAPS J. 2009 Jun;11(2):205-13. Epub 2009 Mar 25. Pubmed
    4. Kouzuki H, Suzuki H, Sugiyama Y: Pharmacokinetic study of the hepatobiliary transport of indomethacin. Pharm Res. 2000 Apr;17(4):432-8. Pubmed

    10. ATP-binding cassette transporter sub-family C member 11

    Actions: inhibitor

    Participates in physiological processes involving bile acids, conjugated steroids and cyclic nucleotides. Enhances the cellular extrusion of cAMP and cGMP. Stimulates the ATP-dependent uptake of a range of physiological and synthetic lipophilic anions, including the glutathione S-conjugates leukotriene C4 and dinitrophenyl S-glutathione, steroid sulfates such as dehydroepiandrosterone 3-sulfate (DHEAS) and estrone 3-sulfate, glucuronides such as estradiol 17-beta-D-glucuronide (E(2)17betaG), the monoanionic bile acids glycocholate and taurocholate, and methotrexate. Probably functions to secrete earwax

    UniProt ID: Q96J66 Link_out
    Gene: ABCC11 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Chen ZS, Guo Y, Belinsky MG, Kotova E, Kruh GD: Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). Mol Pharmacol. 2005 Feb;67(2):545-57. Epub 2004 Nov 10. Pubmed

    11. Solute carrier family 22 member 11

    Actions: inhibitor

    Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds

    UniProt ID: Q9NSA0 Link_out
    Gene: SLC22A11 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Babu E, Takeda M, Narikawa S, Kobayashi Y, Enomoto A, Tojo A, Cha SH, Sekine T, Sakthisekaran D, Endou H: Role of human organic anion transporter 4 in the transport of ochratoxin A. Biochim Biophys Acta. 2002 Jun 12;1590(1-3):64-75. Pubmed
    2. Takeda M, Khamdang S, Narikawa S, Kimura H, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of methotrexate transport and its drug interactions with human organic anion transporters. J Pharmacol Exp Ther. 2002 Aug;302(2):666-71. Pubmed
    3. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. Pubmed

    12. Sodium/bile acid cotransporter

    Actions: substrate

    The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presence of sodium

    UniProt ID: Q14973 Link_out
    Gene: SLC10A1 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Kouzuki H, Suzuki H, Sugiyama Y: Pharmacokinetic study of the hepatobiliary transport of indomethacin. Pharm Res. 2000 Apr;17(4):432-8. Pubmed

    13. Solute carrier family 22 member 7

    Actions: substrate

    Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulfate, allopurinol, 5-fluorouracil, paclitaxel, L-ascorbic acid, salicylate, ethotrexate, and alpha- ketoglutarate

    UniProt ID: Q9Y694 Link_out
    Gene: SLC22A7 Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Morita N, Kusuhara H, Sekine T, Endou H, Sugiyama Y: Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1179-84. Pubmed
    Carriers

    1. Serum albumin

    Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood

    UniProt ID: P02768 Link_out
    Gene: ALB Link_out
    Protein Sequence: FASTA
    Gene Sequence: FASTA
    SNPs: SNPJam Report Link_out

    References:
    1. Bertucci C, Wainer IW: Improved chromatographic performance of a modified human albumin based stationary phase. Chirality. 1997;9(4):335-40. Pubmed
    Comments
    Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19