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Identification
NameConjugated Estrogens
Accession NumberDB00286  (APRD00396)
TypeSmall Molecule
GroupsApproved
Description

Conjugated estrogens, a mixture of the water-soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics.

Structure
Thumb
Synonyms
17-Oxoestra-1,3,5(10)-trien-3-yl sodium sulfate
Conestoral
Estrogenic substances (conjugated)
Estrogens
Estrogens, Conjugated
Estrone sodium sulfate
Estrone sulfate sodium
Estrone-3-sulfate sodium salt
Evex
Hyhorin
Morestin
Oestrone-3-sulphate sodium salt
Premarin
Sodium estrone 3-sulfate
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
C.E.S. Tabletstablet1.25 mgoralValeant Canada Lp Valeant Canada S.E.C.1963-12-312014-07-30Canada
C.E.S. Tabletstablet0.625 mgoralValeant Canada Lp Valeant Canada S.E.C.1963-12-31Not applicableCanada
C.E.S. Tabletstablet0.9 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-03-142014-07-30Canada
C.E.S. Tabletstablet0.3 mgoralValeant Canada Lp Valeant Canada S.E.C.1997-03-142014-07-30Canada
Congest Tab 0.3mgtablet0.3 mgoralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 0.625mgtablet0.625 mgoralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 0.9mgtablet0.9 mgoralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 1.25mgtablet1.25 mgoralLaboratoires Trianon Inc1990-12-31Not applicableCanada
Congest Tab 2.5mgtablet2.5 mgoralLaboratoires Trianon Inc1990-12-31Not applicableCanada
PMS-conjugated Estrogens C.S.D.tablet1.25 mgoralPharmascience Inc1983-12-31Not applicableCanada
PMS-conjugated Estrogens C.S.D.tablet0.625 mgoralPharmascience Inc1983-12-31Not applicableCanada
PMS-conjugated Estrogens C.S.D.tablet0.9 mgoralPharmascience Inc1999-03-03Not applicableCanada
PMS-conjugated Estrogens C.S.D.tablet0.3 mgoralPharmascience Inc1999-03-03Not applicableCanada
Premarintablet, film coated.625 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-21Not applicableUs
Premarininjection, powder, lyophilized, for solution25 mg/5mLintramuscular; intravenousWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.1956-12-01Not applicableUs
Premarintablet, film coated.625 mg/1oralA S Medication Solutions Llc2006-01-01Not applicableUs
Premarintablet, film coated1.25 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2004-09-01Not applicableUs
Premarintablet, film coated.45 mg/1oralCardinal Health2006-01-01Not applicableUs
Premarintablet, film coated.625 mg/1oralAphena Pharma Solutions Tennessee, Inc.2006-01-01Not applicableUs
Premarintablet, film coated.9 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2006-01-01Not applicableUs
Premarintablet, film coated.3 mg/1oralCardinal Health2006-01-01Not applicableUs
Premarintablet, film coated.3 mg/1oralAphena Pharma Solutions Tennessee, Inc.2006-01-01Not applicableUs
Premarintablet (extended-release)1.25 mgoralPfizer Canada Inc2014-10-03Not applicableCanada
Premarintablet, film coated.625 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2006-01-01Not applicableUs
Premarintablet, film coated.625 mg/1oralCardinal Health2006-01-01Not applicableUs
Premarintablet, film coated1.25 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-22Not applicableUs
Premarintablet (extended-release)0.625 mgoralPfizer Canada Inc2014-10-03Not applicableCanada
Premarintablet, film coated.45 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2006-01-01Not applicableUs
Premarintablet, film coated.3 mg/1oralPhysicians Total Care, Inc.2004-11-16Not applicableUs
Premarintablet, film coated.45 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-22Not applicableUs
Premarintablet (extended-release)0.3 mgoralPfizer Canada Inc2014-10-03Not applicableCanada
Premarintablet, film coated.3 mg/1oralWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.2006-01-01Not applicableUs
Premarintablet1.25 mgoralPfizer Canada Inc1994-12-31Not applicableCanada
Premarintablet, film coated.625 mg/1oralPhysicians Total Care, Inc.2005-02-08Not applicableUs
Premarintablet, film coated.9 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-22Not applicableUs
Premarintablet, film coated.3 mg/1oralA S Medication Solutions2006-01-01Not applicableUs
Premarintablet, film coated.9 mg/1oralAvera Mc Kennan Hospital2015-08-03Not applicableUs
Premarintablet, film coated.625 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Premarintablet0.3 mgoralPfizer Canada Inc1994-12-31Not applicableCanada
Premarintablet0.625 mgoralPfizer Canada Inc1994-12-31Not applicableCanada
Premarintablet, film coated1.25 mg/1oralA S Medication Solutions Llc2004-09-01Not applicableUs
Premarintablet, film coated.3 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-22Not applicableUs
Premarintablet, film coated.9 mg/1oralCardinal Health2006-01-01Not applicableUs
Premarin Crm 0.625mg/gmcream.625 mgtopical; vaginalAyerst Laboratories1951-12-311996-09-10Canada
Premarin Inj 25mg/5mlpowder for solution25 mgintramuscular; intravenousAyerst Laboratories1953-12-311996-09-10Canada
Premarin Intravenouspowder for solution25 mgintramuscular; intravenousPfizer Canada Inc1994-12-31Not applicableCanada
Premarin Tablets 0.3mgtablet0.3 mgoralAyerst Laboratories1951-12-311996-09-10Canada
Premarin Tablets 0.625mgtablet0.625 mgoralAyerst Laboratories1951-12-311996-09-10Canada
Premarin Tablets 0.9mgtablet0.9 mgoralWyeth Canada1993-12-312007-08-13Canada
Premarin Tablets 1.25mgtablet1.25 mgoralAyerst Laboratories1951-12-311996-09-10Canada
Premarin Tablets 2.5mgtablet2.5 mgoralWyeth Ayerst Canada Inc.1996-09-202000-08-02Canada
Premarin Tablets 2.5mgtablet2.5 mgoralAyerst Laboratories1951-12-311997-08-15Canada
Premarin Vaginalcream.625 mg/gvaginalWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.1978-11-01Not applicableUs
Premarin Vaginal Creamcream0.625 mgtopical; vaginalPfizer Canada Inc1994-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-conest Tab 0.3mgtablet0.3 mgoralApotex Inc1994-12-312009-10-09Canada
Apo-conest Tab 0.625mgtablet0.625 mgoralApotex Inc1994-12-312009-10-09Canada
Apo-conest Tab 0.9mgtablet0.9 mgoralApotex Inc1994-12-312009-10-09Canada
Apo-conest Tab 1.25mgtablet1.25 mgoralApotex Inc1994-12-312009-10-09Canada
Apo-conest Tab 2.5mgtablet2.5 mgoralApotex Inc1994-12-312009-10-09Canada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixtures
NameLabellerIngredients
DuaveeWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.
DuavivePfizer Canada Inc
Esterified Estrogens and MethyltestosteroneSeton Pharmaceuticals
PremphaseWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.
PremplusPfizer Canada Inc
Premplus CyclePfizer Canada Inc
PremproWyeth Pharmaceuticals Inc., a subsidiary of Pfizer Inc.
SaltsNot Available
Categories
UNII6K6FDA543A
CAS number438-67-5
WeightAverage: 372.411
Monoisotopic: 372.100739147
Chemical FormulaC18H21NaO5S
InChI KeyInChIKey=VUCAHVBMSFIGAI-ZFINNJDLSA-M
InChI
InChI=1S/C18H22O5S.Na/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19;/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22);/q;+1/p-1/t14-,15-,16+,18+;/m1./s1
IUPAC Name
sodium (1S,10R,11S,15S)-15-methyl-14-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2,4,6-trien-5-yl sulfate
SMILES
[Na+].[H][C@@]12CCC(=O)[C@@]1(C)CC[C@]1([H])C3=CC=C(OS([O-])(=O)=O)C=C3CC[C@@]21[H]
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as sulfated steroids. These are sterol lipids containing a sulfate group attached to the steroid skeleton.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassSulfated steroids
Direct ParentSulfated steroids
Alternative Parents
Substituents
  • Sulfated steroid
  • 3-sulfated steroid
  • Sulfated steroid skeleton
  • Oxosteroid
  • 17-oxosteroid
  • Estrane-skeleton
  • Phenanthrene
  • Tetralin
  • Sulfuric acid monoester
  • Benzenoid
  • Sulfuric acid ester
  • Sulfate-ester
  • Organic sulfuric acid or derivatives
  • Ketone
  • Hydrocarbon derivative
  • Organic alkali metal salt
  • Organic sodium salt
  • Organic salt
  • Organooxygen compound
  • Carbonyl group
  • Organic zwitterion
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of moderate to severe vasomotor symptoms associated with the menopause, atrophic vaginitis, osteoporosis, hypoestrogenism due to hypogonadism, castration, primary ovarian failure, breast cancer (for palliation only), and Advanced androgen-dependent carcinoma of the prostate (for palliation only)
PharmacodynamicsConjugated estrogens, a mixture of the water soluble salts of sulfate esters from estrone, equilin, 17 α-dihydroequilin, and other related steroids, may be derived from pregnant equine urine or yam and soy plants. Estrogens are important in the development and maintenance of the female reproductive system and secondary sex characteristics. They promote growth and development of the vagina, uterus, and fallopian tubes, and enlargement of the breasts. Indirectly, they contribute to the shaping of the skeleton, maintenance of tone and elasticity of urogenital structures, changes in the epiphyses of the long bones that allow for the pubertal growth spurt and its termination, growth of axillary and pubic hair, and pigmentation of the nipples and genitals. Decline of estrogenic activity at the end of the menstrual cycle can bring on menstruation, although the cessation of progesterone secretion is the most important factor in the mature ovulatory cycle. However, in the preovulatory or nonovulatory cycle, estrogen is the primary determinant in the onset of menstruation. Estrogens also affect the release of pituitary gonadotropins. The pharmacologic effects of conjugated estrogens are similar to those of endogenous estrogens.
Mechanism of actionEstrogens enter the cells of responsive tissues (e.g., female organs, breasts, hypothalamus, pituitary) where they interact with a protein receptor, subsequently increasing the rate of synthesis of DNA, RNA, and some proteins. Estrogens decrease the secretion of gonadotropin-releasing hormone by the hypothalamus, reducing the secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary.
Related Articles
AbsorptionWell absorbed
Volume of distributionNot Available
Protein binding90% bound to plasma proteins
Metabolism

Hepatic

Route of eliminationEstradiol, estrone, and estriol are excreted in the urine, along with glucuronide and sulfate conjugates. Exogenous estrogens are metabolized in the same manner as endogenous estrogens.
Half life7.4 hours
ClearanceNot Available
ToxicityNausea and vomiting
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.997
Blood Brain Barrier+0.9486
Caco-2 permeable-0.8738
P-glycoprotein substrateNon-substrate0.5295
P-glycoprotein inhibitor INon-inhibitor0.5198
P-glycoprotein inhibitor IINon-inhibitor0.9431
Renal organic cation transporterNon-inhibitor0.8313
CYP450 2C9 substrateNon-substrate0.7886
CYP450 2D6 substrateNon-substrate0.8125
CYP450 3A4 substrateSubstrate0.6454
CYP450 1A2 substrateNon-inhibitor0.8152
CYP450 2C9 inhibitorNon-inhibitor0.8454
CYP450 2D6 inhibitorNon-inhibitor0.9026
CYP450 2C19 inhibitorNon-inhibitor0.8017
CYP450 3A4 inhibitorNon-inhibitor0.9204
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8461
Ames testNon AMES toxic0.5177
CarcinogenicityNon-carcinogens0.5338
BiodegradationNot ready biodegradable0.6303
Rat acute toxicity2.3418 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.6053
hERG inhibition (predictor II)Inhibitor0.7941
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Wyeth pharmaceuticals inc
  • Duramed research inc
  • Teva womens health inc
  • Roche palo alto llc
Packagers
Dosage forms
FormRouteStrength
Tabletoral0.3 mg
Tabletoral0.625 mg
Tabletoral0.9 mg
Tabletoral1.25 mg
Tabletoral2.5 mg
Tablet, film coatedoral
Tablet (immediate and extended release)oral
Tabletoral
Injection, powder, lyophilized, for solutionintramuscular; intravenous25 mg/5mL
Tablet (extended-release)oral0.3 mg
Tablet (extended-release)oral0.625 mg
Tablet (extended-release)oral1.25 mg
Tablet, film coatedoral.3 mg/1
Tablet, film coatedoral.45 mg/1
Tablet, film coatedoral.625 mg/1
Tablet, film coatedoral.9 mg/1
Tablet, film coatedoral1.25 mg/1
Creamtopical; vaginal.625 mg
Powder for solutionintramuscular; intravenous25 mg
Creamvaginal.625 mg/g
Creamtopical; vaginal0.625 mg
Kit
Kit; tabletoral
Tablet, sugar coatedoral
Prices
Unit descriptionCostUnit
Premarin 0.625 mg/gm Cream 42.5 gm Tube134.05USD tube
Premarin 25 mg vial107.54USD vial
Premphase 28 0.625-5 mg tablet Disp Pack69.99USD disp
Premarin vaginal cream-appl3.07USD g
Prempro 0.3 mg-1.5 mg tablet2.34USD tablet
Prempro 0.45-1.5 mg tablet2.34USD tablet
Prempro 0.625-2.5 mg tablet2.34USD tablet
Prempro 0.625-5 mg tablet2.34USD tablet
Premarin 0.45 mg tablet1.97USD tablet
Premarin 0.9 mg tablet1.97USD tablet
Premarin 2.5 mg tablet1.83USD tablet
Premarin 2.5 mg Tabs1.82USD tablet
Premarin 0.3 mg tablet1.42USD tablet
Premarin 0.625 mg tablet1.42USD tablet
Premarin 1.25 mg tablet1.42USD tablet
Premarin 0.625 mg/g Cream0.69USD g
C.E.S. 0.625 mg Tablet0.11USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5547948 No1995-01-172015-01-17Us
US5908638 No1995-07-262015-07-26Us
US5998402 No1997-04-042017-04-04Us
US6479535 No1999-05-062019-05-06Us
US7138392 No1997-04-042017-04-04Us
US7683051 No2007-03-102027-03-10Us
US8815934 No1999-05-062019-05-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point173 °CNot Available
water solubility0.0036 mg/mlNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0045 mg/mLALOGPS
logP2.75ALOGPS
logP3.83ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)-1.7ChemAxon
pKa (Strongest Basic)-7.5ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area83.5 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity87.95 m3·mol-1ChemAxon
Polarizability36.47 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Vallapa Soong, “Process for the preparation of conjugated estrogens from pregnant mare urine.” U.S. Patent US20020156303, issued October 24, 2002.

US20020156303
General ReferencesNot Available
External Links
ATC CodesG03CA57G03CC07
AHFS Codes
  • 68:16.04
PDB EntriesNot Available
FDA labelDownload (167 KB)
MSDSDownload (34.7 KB)
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Molecular Weight:
66215.45 Da
References
  1. Ropero AB, Eghbali M, Minosyan TY, Tang G, Toro L, Stefani E: Heart estrogen receptor alpha: distinct membrane and nuclear distribution patterns and regulation by estrogen. J Mol Cell Cardiol. 2006 Sep;41(3):496-510. Epub 2006 Jul 28. [PubMed:16876190 ]
  2. Stroud FC, Appt SE, Wilson ME, Franke AA, Adams MR, Kaplan JR: Concentrations of isoflavones in macaques consuming standard laboratory monkey diet. J Am Assoc Lab Anim Sci. 2006 Jul;45(4):20-3. [PubMed:16884174 ]
  3. Hou NN, Zhu YM, Huang HF: [The expression of estrogen receptor alpha and beta in the intervention of different estrogens in rat bone metabolism]. Fen Zi Xi Bao Sheng Wu Xue Bao. 2006 Aug;39(4):289-96. [PubMed:16955786 ]
  4. Gouva L, Tsatsoulis A: The role of estrogens in cardiovascular disease in the aftermath of clinical trials. Hormones (Athens). 2004 Jul-Sep;3(3):171-83. [PubMed:16982590 ]
  5. Smith MR: Selective estrogen receptor modulators to prevent treatment-related osteoporosis. Rev Urol. 2005;7 Suppl 3:S30-5. [PubMed:16985877 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
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. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M: Substrate inhibition kinetics for cytochrome P450-catalyzed reactions. Drug Metab Dispos. 2001 Apr;29(4 Pt 1):368-74. [PubMed:11259318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
O-methyltransferase activity
Specific Function:
Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOPA, alpha-methyl DOPA and isoproterenol.
Gene Name:
COMT
Uniprot ID:
P21964
Molecular Weight:
30036.77 Da
References
  1. Zhu BT, Wu KY, Wang P, Cai MX, Conney AH: O-methylation of catechol estrogens by human placental catechol-o-methyltransferase: interindividual differences in sensitivity to heat inactivation and to inhibition by dietary polyphenols. Drug Metab Dispos. 2010 Oct;38(10):1892-9. doi: 10.1124/dmd.110.033548. Epub 2010 Jul 6. [PubMed:20606002 ]
  2. Jobe SO, Ramadoss J, Koch JM, Jiang Y, Zheng J, Magness RR: Estradiol-17beta and its cytochrome P450- and catechol-O-methyltransferase-derived metabolites stimulate proliferation in uterine artery endothelial cells: role of estrogen receptor-alpha versus estrogen receptor-beta. Hypertension. 2010 Apr;55(4):1005-11. doi: 10.1161/HYPERTENSIONAHA.109.146399. Epub 2010 Mar 8. [PubMed:20212268 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Hirohashi T, Suzuki H, Sugiyama Y: Characterization of the transport properties of cloned rat multidrug resistance-associated protein 3 (MRP3). J Biol Chem. 1999 May 21;274(21):15181-5. [PubMed:10329726 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
May be an organic anion pump relevant to cellular detoxification.
Gene Name:
ABCC4
Uniprot ID:
O15439
Molecular Weight:
149525.33 Da
References
  1. Zelcer N, Reid G, Wielinga P, Kuil A, van der Heijden I, Schuetz JD, Borst P: Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7. [PubMed:12523936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Qian YM, Song WC, Cui H, Cole SP, Deeley RG: Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1. J Biol Chem. 2001 Mar 2;276(9):6404-11. Epub 2000 Dec 1. [PubMed:11102445 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [PubMed:10871297 ]
  2. Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. [PubMed:9539145 ]
  3. Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [PubMed:8779894 ]
  4. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566 ]
  5. Kontaxi M, Echkardt U, Hagenbuch B, Stieger B, Meier PJ, Petzinger E: Uptake of the mycotoxin ochratoxin A in liver cells occurs via the cloned organic anion transporting polypeptide. J Pharmacol Exp Ther. 1996 Dec;279(3):1507-13. [PubMed:8968376 ]
  6. Pang KS, Wang PJ, Chung AY, Wolkoff AW: The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein. Hepatology. 1998 Nov;28(5):1341-6. [PubMed:9794920 ]
  7. Bossuyt X, Muller M, Meier PJ: Multispecific amphipathic substrate transport by an organic anion transporter of human liver. J Hepatol. 1996 Nov;25(5):733-8. [PubMed:8938553 ]
  8. Hagenbuch B, Adler ID, Schmid TE: Molecular cloning and functional characterization of the mouse organic-anion-transporting polypeptide 1 (Oatp1) and mapping of the gene to chromosome X. Biochem J. 2000 Jan 1;345 Pt 1:115-20. [PubMed:10600646 ]
  9. Lee TK, Koh AS, Cui Z, Pierce RH, Ballatori N: N-glycosylation controls functional activity of Oatp1, an organic anion transporter. Am J Physiol Gastrointest Liver Physiol. 2003 Aug;285(2):G371-81. Epub 2003 Apr 17. [PubMed:12702494 ]
  10. Kouzuki H, Suzuki H, Ito K, Ohashi R, Sugiyama Y: Contribution of organic anion transporting polypeptide to uptake of its possible substrates into rat hepatocytes. J Pharmacol Exp Ther. 1999 Feb;288(2):627-34. [PubMed:9918568 ]
  11. Eckhardt U, Schroeder A, Stieger B, Hochli M, Landmann L, Tynes R, Meier PJ, Hagenbuch B: Polyspecific substrate uptake by the hepatic organic anion transporter Oatp1 in stably transfected CHO cells. Am J Physiol. 1999 Apr;276(4 Pt 1):G1037-42. [PubMed:10198348 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Virus receptor activity
Specific Function:
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.(Microbial infection) Acts as a receptor for hepatitis B virus.
Gene Name:
SLC10A1
Uniprot ID:
Q14973
Molecular Weight:
38118.64 Da
References
  1. Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. [PubMed:9486191 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Not Available
Gene Name:
SLC22A10
Uniprot ID:
Q63ZE4
Molecular Weight:
60256.57 Da
References
  1. Youngblood GL, Sweet DH: Identification and functional assessment of the novel murine organic anion transporter Oat5 (Slc22a19) expressed in kidney. Am J Physiol Renal Physiol. 2004 Aug;287(2):F236-44. Epub 2004 Apr 6. [PubMed:15068970 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
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).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. 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:14762099 ]
  2. 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:12679720 ]
  3. Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol. 2002 May;61(5):982-8. [PubMed:11961115 ]
  4. 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:11306713 ]
  5. Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [PubMed:12011098 ]
  6. Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. [PubMed:15100168 ]
  7. 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:10224140 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol, estrone-3-sulfate and sulfobromophthalein (BSP) are transported with much lower efficiency. May play a signifiant role in regulating T4 flux into and out of the brain (By similarity).
Gene Name:
SLCO1C1
Uniprot ID:
Q9NYB5
Molecular Weight:
78695.625 Da
References
  1. Tohyama K, Kusuhara H, Sugiyama Y: Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier. Endocrinology. 2004 Sep;145(9):4384-91. Epub 2004 May 27. [PubMed:15166123 ]
  2. Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake 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. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238 ]
  2. Nozawa T, Tamai I, Sai Y, Nezu J, Tsuji A: Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin. J Pharm Pharmacol. 2003 Jul;55(7):1013-20. [PubMed:12906759 ]
  3. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001 ]
  4. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445 ]
  5. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862 ]
  6. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800 ]
  7. van Montfoort JE, Schmid TE, Adler ID, Meier PJ, Hagenbuch B: Functional characterization of the mouse organic-anion-transporting polypeptide 2. Biochim Biophys Acta. 2002 Aug 19;1564(1):183-8. [PubMed:12101011 ]
  8. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
  2. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238 ]
  3. Kobayashi D, Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther. 2003 Aug;306(2):703-8. Epub 2003 Apr 30. [PubMed:12724351 ]
  4. Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45. Epub 2003 Nov 10. [PubMed:14610227 ]
  5. Satoh H, Yamashita F, Tsujimoto M, Murakami H, Koyabu N, Ohtani H, Sawada Y: Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos. 2005 Apr;33(4):518-23. Epub 2005 Jan 7. [PubMed:15640378 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [PubMed:12011098 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficiently transports the major species of bile acids.
Gene Name:
SLC51A
Uniprot ID:
Q86UW1
Molecular Weight:
37734.575 Da
References
  1. Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficiently transports the major species of bile acids. Modulates SLC51A glycosylation, membrane trafficking and stability activities.
Gene Name:
SLC51B
Uniprot ID:
Q86UW2
Molecular Weight:
14346.195 Da
References
  1. Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [PubMed:12719432 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Spears KJ, Ross J, Stenhouse A, Ward CJ, Goh LB, Wolf CR, Morgan P, Ayrton A, Friedberg TH: Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochem Pharmacol. 2005 Feb 1;69(3):415-23. Epub 2004 Dec 22. [PubMed:15652233 ]
  2. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name:
SLCO4A1
Uniprot ID:
Q96BD0
Molecular Weight:
77192.505 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Purine nucleotide transmembrane transporter activity
Specific Function:
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...
Gene Name:
ABCC11
Uniprot ID:
Q96J66
Molecular Weight:
154299.625 Da
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:15537867 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [PubMed:11134001 ]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
  3. Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [PubMed:15159445 ]
  4. Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [PubMed:14977862 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name:
SLC22A11
Uniprot ID:
Q9NSA0
Molecular Weight:
59970.945 Da
References
  1. 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:10660625 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as estrone-3-sulfate (PubMed:10873595). Mediates transport of prostaglandins (PG) E1 and E2, thyroxine (T4), deltorphin II, BQ-123 and vasopressin, but not DPDPE (a derivative of enkephalin lacking an N-terminal tyrosine residue), estrone-3-sulfate, taurocholate, digoxin nor DHEAS (PubMed:16971491).
Gene Name:
SLCO3A1
Uniprot ID:
Q9UIG8
Molecular Weight:
76552.135 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800 ]
  2. Suzuki M, Suzuki H, Sugimoto Y, Sugiyama Y: ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9. Epub 2003 Apr 7. [PubMed:12682043 ]
  3. Imai Y, Asada S, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Breast cancer resistance protein exports sulfated estrogens but not free estrogens. Mol Pharmacol. 2003 Sep;64(3):610-8. [PubMed:12920197 ]
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Drug created on June 13, 2005 07:24 / Updated on July 29, 2016 01:53