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Identification
NameUrsodeoxycholic acid
Accession NumberDB01586
TypeSmall Molecule
GroupsApproved, Investigational
Description

Ursodeoxycholic acid is an epimer of chenodeoxycholic acid (DB06777). It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic. [PubChem]

Structure
Thumb
Synonyms
(3alpha,5beta,7beta)-3,7-dihydroxycholan-24-oic acid
(3α,5β,7β)-3,7-dihydroxycholan-24-oic acid
3alpha,7beta-Dihydroxy-5beta-cholan-24-oic acid
Acide ursodesoxycholique
Acido ursodeossicolico
Acido ursodeoxicolico
Acidum ursodeoxycholicum
Actigall
UDCA
Ursodeoxycholate
Ursodeoxycholic acid
Ursodiol
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Actigallcapsule300 mg/1oralActavis Pharma, Inc.1987-12-312016-04-05Us
Dom-ursodiol Ctablet500 mgoralDominion Pharmacal2006-08-17Not applicableCanada
Dom-ursodiol Ctablet250 mgoralDominion Pharmacal2006-08-17Not applicableCanada
Mint-ursodioltablet500 mgoralMint Pharmaceuticals IncNot applicableNot applicableCanada
Mint-ursodioltablet250 mgoralMint Pharmaceuticals IncNot applicableNot applicableCanada
Novo-ursodioltablet250 mgoralNovopharm LimitedNot applicableNot applicableCanada
Novo-ursodioltablet500 mgoralNovopharm LimitedNot applicableNot applicableCanada
Pendo-ursodiol Ctablet500 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
Pendo-ursodiol Ctablet250 mgoralPendopharm Division Of De Pharmascience IncNot applicableNot applicableCanada
PHL-ursodiol Ctablet500 mgoralPharmel Inc2006-08-17Not applicableCanada
PHL-ursodiol Ctablet250 mgoralPharmel Inc2006-08-17Not applicableCanada
PMS-ursodioltablet250 mgoralPharmascience IncNot applicableNot applicableCanada
PMS-ursodiol Ctablet250 mgoralPharmascience Inc2006-05-01Not applicableCanada
PMS-ursodiol Ctablet500 mgoralPharmascience Inc2006-05-01Not applicableCanada
Ursotablet250 mgoralAptalis Pharma Canada Inc1998-11-08Not applicableCanada
Ursotablet, film coated250 mg/1oralCardinal Health1997-12-102016-04-05Us
Urso 250tablet, film coated250 mg/1oralAptalis Pharma US, Inc.1997-12-102016-04-05Us
Urso DStablet500 mgoralAptalis Pharma Canada Inc2003-02-03Not applicableCanada
Urso Fortetablet, film coated500 mg/1oralAptalis Pharma US, Inc.1997-12-102016-04-05Us
Ursodiolcapsule300 mg/1oralCardinal Health2009-11-052016-04-05Us
Ursodioltablet250 mg/1oralActavis Pharma, Inc.1997-12-102016-04-23Us
Ursodiolcapsule300 mg/1oralCarilion Materials Management1987-12-312016-04-05Us
Ursodiolcapsule300 mg/1oralPhysicians Total Care, Inc.2004-03-292016-04-05Us
Ursodiolcapsule300 mg/1oralAmerican Health Packaging2009-11-052017-03-31Us
Ursodiolcapsule300 mg/1oralSTAT Rx USA LLC1987-12-312016-04-05Us
Ursodiolcapsule300 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1987-12-312016-04-23Us
Ursodiolcapsule300 mg/1oralActavis Pharma, Inc.1987-12-312016-04-23Us
Ursodioltablet500 mg/1oralActavis Pharma, Inc.1997-12-102016-04-23Us
Ursodiol Tablets, 250 mgtablet, film coated250 mg/1oralPrasco Laboratories2009-07-012016-04-05Us
Ursodiol Tablets, 500 mgtablet, film coated500 mg/1oralPrasco Laboratories2009-07-012016-04-05Us
Ursofalkcapsule250 mgoralAxcan Pharma Inc1991-12-312000-08-03Canada
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ursodiolcapsule300 mg/1oralAmerican Health Packaging2014-12-052016-04-05Us
Ursodiolcapsule300 mg/1oralMarlex Pharmaceuticals Inc2014-10-012016-04-05Us
Ursodioltablet, film coated250 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2011-12-232016-04-23Us
Ursodioltablet, film coated250 mg/1oralBlue Point Laboratories2014-02-272016-04-05Us
Ursodiolcapsule300 mg/1oralGolden State Medical Supply, Inc.2010-07-162016-04-05Us
Ursodiolcapsule300 mg/1oralMajor Pharmaceuticals2015-05-052016-04-05Us
Ursodiolcapsule300 mg/1oralTAGI Pharma, Inc.2011-04-152016-04-05Us
Ursodiolcapsule300 mg/1oralMajor Pharmaceuticals2011-04-012016-04-05Us
Ursodiolcapsule300 mg/1oralMylan Institutional Inc.2016-01-252016-04-05Us
Ursodiolcapsule300 mg/1oralAv Pak2012-07-252016-04-05Us
Ursodioltablet, film coated500 mg/1oralActavis Pharma, Inc.2011-12-232016-04-23Us
Ursodioltablet, film coated250 mg/1oralAvera Mc Kennan Hospital2015-08-182016-04-05Us
Ursodioltablet, film coated500 mg/1oralPar Pharmaceutical Companies, Inc.2013-08-012016-04-05Us
Ursodioltablet, film coated250 mg/1oralActavis Pharma, Inc.2011-12-232016-04-23Us
Ursodioltablet500 mg/1oralGlenmark Pharmaceuticals Inc., Usa2011-07-122016-04-05Us
Ursodioltablet, film coated250 mg/1oralPar Pharmaceutical Companies, Inc.2013-08-012016-04-05Us
Ursodiolcapsule300 mg/1oralLannett Company, Inc.2009-01-012016-04-23Us
Ursodioltablet250 mg/1oralGlenmark Pharmaceuticals Inc., Usa2011-07-122016-04-05Us
Ursodiolcapsule300 mg/1oralEpic Pharma, LLC2010-07-162016-04-05Us
Ursodiolcapsule300 mg/1oralMylan Pharmaceuticals Inc.2012-05-072016-04-23Us
Ursodioltablet, film coated250 mg/1oralAmerican Health Packaging2014-12-152016-04-05Us
Ursodiolcapsule300 mg/1oralAv Kare, Inc.2010-07-162016-04-05Us
Ursodioltablet, film coated500 mg/1oralGlobal Pharmaceuticals, Division of Impax Laboratories, Inc.2011-12-232016-04-23Us
Ursodioltablet, film coated500 mg/1oralBlue Point Laboratories2014-02-272016-04-05Us
Over the Counter ProductsNot Available
International Brands
NameCompany
Cholit-ursanNot Available
DelursanNot Available
DestolitNot Available
DeursilNot Available
LitursolNot Available
SolutratNot Available
UrsacolNot Available
UrsocholNot Available
UrsolvanNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII724L30Y2QR
CAS number128-13-2
WeightAverage: 392.572
Monoisotopic: 392.292659768
Chemical FormulaC24H40O4
InChI KeyInChIKey=RUDATBOHQWOJDD-UZVSRGJWSA-N
InChI
InChI=1S/C24H40O4/c1-14(4-7-21(27)28)17-5-6-18-22-19(9-11-24(17,18)3)23(2)10-8-16(25)12-15(23)13-20(22)26/h14-20,22,25-26H,4-13H2,1-3H3,(H,27,28)/t14-,15+,16-,17-,18+,19+,20+,22+,23+,24-/m1/s1
IUPAC Name
(4R)-4-[(1S,2S,5R,7S,9S,10R,11S,14R,15R)-5,9-dihydroxy-2,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadecan-14-yl]pentanoic acid
SMILES
[H][C@@]1(CC[C@@]2([H])[C@]3([H])[C@@H](O)C[C@]4([H])C[[email protected]](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)[[email protected]](C)CCC(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dihydroxy bile acids, alcohols and derivatives. These are compounds containing or derived from a bile acid or alcohol, and which bears exactly two carboxylic acid groups.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassBile acids, alcohols and derivatives
Direct ParentDihydroxy bile acids, alcohols and derivatives
Alternative Parents
Substituents
  • Dihydroxy bile acid, alcohol, or derivatives
  • 7-hydroxysteroid
  • 3-alpha-hydroxysteroid
  • Hydroxysteroid
  • 3-hydroxysteroid
  • Cyclic alcohol
  • Secondary alcohol
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Alcohol
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationThe drug reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones in patients who want an alternative to surgery.
PharmacodynamicsUrsodiol (also known as ursodeoxycholic acid) is one of the secondary bile acids, which are metabolic byproducts of intestinal bacteria. Primary bile acids are produced by the liver and stored in the gall bladder. When secreted into the colon, primary bile acids can be metabolized into secondary bile acids by intestinal bacteria. Primary and secondary bile acids help the body digest fats. Ursodeoxycholic acid helps regulate cholesterol by reducing the rate at which the intestine absorbs cholesterol molecules while breaking up micelles containing cholesterol. Because of this property, ursodeoxycholic acid is used to treat gall stones non-surgically.
Mechanism of actionUrsodeoxycholic acid reduces elevated liver enzyme levels by facilitating bile flow through the liver and protecting liver cells. The main mechanism if anticholelithic. Although the exact process of ursodiol's anticholelithic action is not completely understood, it is thought that the drug is concentrated in bile and decreases biliary cholesterol by suppressing hepatic synthesis and secretion of cholesterol and by inhibiting its intestinal absorption. The reduced cholesterol saturation permits the gradual solubilization of cholesterol from gallstones, resulting in their eventual dissolution.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationOnly small quantities of ursodiol appear in the systemic circulation and very small amounts are excreted into urine. Eighty percent of lithocholic acid formed in the small bowel is excreted in the feces, but the 20% that is absorbed is sulfated at the 3-hydroxyl group in the liver to relatively insoluble lithocholyl conjugates which are excreted into bile and lost in feces.
Half lifeNot Available
ClearanceNot Available
ToxicityNeither accidental nor intentional overdosing with ursodeoxycholic acid has been reported. Doses of ursodeoxycholic acid in the range of 16-20 mg/kg/day have been tolerated for 6-37 months without symptoms by 7 patients. The LD50 for ursodeoxycholic acid in rats is over 5000 mg/kg given over 7-10 days and over 7500 mg/kg for mice. The most likely manifestation of severe overdose with ursodeoxycholic acid would probably be diarrhea, which should be treated symptomatically.
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+0.9766
Blood Brain Barrier+0.9288
Caco-2 permeable+0.73
P-glycoprotein substrateSubstrate0.6648
P-glycoprotein inhibitor INon-inhibitor0.8737
P-glycoprotein inhibitor IIInhibitor0.5368
Renal organic cation transporterNon-inhibitor0.8537
CYP450 2C9 substrateNon-substrate0.7818
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9456
CYP450 2D6 inhibitorNon-inhibitor0.9781
CYP450 2C19 inhibitorNon-inhibitor0.9707
CYP450 3A4 inhibitorNon-inhibitor0.8405
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9563
Ames testNon AMES toxic0.8794
CarcinogenicityNon-carcinogens0.9329
BiodegradationNot ready biodegradable0.992
Rat acute toxicity2.5624 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9622
hERG inhibition (predictor II)Non-inhibitor0.7246
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral250 mg
Tabletoral500 mg
Capsuleoral300 mg/1
Tabletoral250 mg/1
Tabletoral500 mg/1
Tablet, film coatedoral250 mg/1
Tablet, film coatedoral500 mg/1
Capsuleoral250 mg
Prices
Unit descriptionCostUnit
Urso forte 500 mg tablet6.3USD tablet
Actigall 300 mg capsule5.52USD capsule
Ursodiol 500 mg tablet4.75USD tablet
Urso 250 mg tablet4.41USD tablet
Urso 250 250 mg tablet3.55USD tablet
Urso Ds 500 mg Tablet2.69USD tablet
Ursodiol 250 mg tablet2.68USD tablet
Pms-Ursodiol C 500 mg Tablet1.75USD tablet
Urso 250 mg Tablet1.42USD tablet
Pms-Ursodiol C 250 mg Tablet0.92USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point203 °CPhysProp
water solubility20 mg/L (at 20 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP3.00RODA,A ET AL. (1990)
Predicted Properties
PropertyValueSource
Water Solubility0.0197 mg/mLALOGPS
logP3.01ALOGPS
logP3.71ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)4.6ChemAxon
pKa (Strongest Basic)-0.54ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area77.76 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity109.27 m3·mol-1ChemAxon
Polarizability46.33 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

Antonio Bonaldi, Egidio Molinari, “Process for preparing high purity ursodeoxycholic acid.” U.S. Patent US4379093, issued July, 1980.

US4379093
General References
  1. Akare S, Jean-Louis S, Chen W, Wood DJ, Powell AA, Martinez JD: Ursodeoxycholic acid modulates histone acetylation and induces differentiation and senescence. Int J Cancer. 2006 Dec 15;119(12):2958-69. [PubMed:17019713 ]
  2. Smith T, Befeler AS: High-dose ursodeoxycholic acid for the treatment of primary sclerosing cholangitis. Curr Gastroenterol Rep. 2007 Mar;9(1):54-9. [PubMed:17335678 ]
  3. Jackson H, Solaymani-Dodaran M, Card TR, Aithal GP, Logan R, West J: Influence of ursodeoxycholic acid on the mortality and malignancy associated with primary biliary cirrhosis: a population-based cohort study. Hepatology. 2007 Oct;46(4):1131-7. [PubMed:17685473 ]
External Links
ATC CodesA05AA02
AHFS Codes
  • 56:14.00
PDB Entries
FDA labelDownload (233 KB)
MSDSDownload (73.3 KB)
Interactions
Drug Interactions
Drug
Aluminum hydroxideThe serum concentration of Ursodeoxycholic acid can be decreased when it is combined with Aluminum hydroxide.
BezafibrateThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Bezafibrate.
ChlorotrianiseneThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Chlorotrianisene.
CholestyramineThe serum concentration of Ursodeoxycholic acid can be decreased when it is combined with Cholestyramine.
Choline fenofibrateThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Choline fenofibrate.
ColesevelamThe serum concentration of Ursodeoxycholic acid can be decreased when it is combined with Colesevelam.
ColestipolThe serum concentration of Ursodeoxycholic acid can be decreased when it is combined with Colestipol.
EstradiolThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Estradiol.
EstropipateThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Estropipate.
FenofibrateThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Fenofibrate.
GemfibrozilThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Gemfibrozil.
NitrendipineUrsodeoxycholic acid can cause a decrease in the absorption of Nitrendipine resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inducer
General Function:
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function:
Works in concert with the 5-alpha/5-beta-steroid reductases to convert steroid hormones into the 3-alpha/5-alpha and 3-alpha/5-beta-tetrahydrosteroids. Catalyzes the inactivation of the most potent androgen 5-alpha-dihydrotestosterone (5-alpha-DHT) to 5-alpha-androstane-3-alpha,17-beta-diol (3-alpha-diol). Has a high bile-binding ability.
Gene Name:
AKR1C2
Uniprot ID:
P52895
Molecular Weight:
36734.97 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Amaral JD, Sola S, Steer CJ, Rodrigues CM: Role of nuclear steroid receptors in apoptosis. Curr Med Chem. 2009;16(29):3886-902. [PubMed:19747134 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
General Function:
Transporter activity
Specific Function:
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name:
ABCB11
Uniprot ID:
O95342
Molecular Weight:
146405.83 Da
References
  1. Schuetz EG, Strom S, Yasuda K, Lecureur V, Assem M, Brimer C, Lamba J, Kim RB, Ramachandran V, Komoroski BJ, Venkataramanan R, Cai H, Sinal CJ, Gonzalez FJ, Schuetz JD: Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters, and cytochrome P450. J Biol Chem. 2001 Oct 19;276(42):39411-8. Epub 2001 Aug 16. [PubMed:11509573 ]
  2. Green RM, Hoda F, Ward KL: Molecular cloning and characterization of the murine bile salt export pump. Gene. 2000 Jan 4;241(1):117-23. [PubMed:10607905 ]
  3. Mita S, Suzuki H, Akita H, Stieger B, Meier PJ, Hofmann AF, Sugiyama Y: Vectorial transport of bile salts across MDCK cells expressing both rat Na+-taurocholate cotransporting polypeptide and rat bile salt export pump. Am J Physiol Gastrointest Liver Physiol. 2005 Jan;288(1):G159-67. Epub 2004 Aug 5. [PubMed:15297262 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitorinducer
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. Fickert P, Zollner G, Fuchsbichler A, Stumptner C, Pojer C, Zenz R, Lammert F, Stieger B, Meier PJ, Zatloukal K, Denk H, Trauner M: Effects of ursodeoxycholic and cholic acid feeding on hepatocellular transporter expression in mouse liver. Gastroenterology. 2001 Jul;121(1):170-83. [PubMed:11438506 ]
  2. Kullak-Ublick GA, Hagenbuch B, Stieger B, Schteingart CD, Hofmann AF, Wolkoff AW, Meier PJ: Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995 Oct;109(4):1274-82. [PubMed:7557095 ]
  3. Kullak-Ublick GA, Hagenbuch B, Stieger B, Wolkoff AW, Meier PJ: Functional characterization of the basolateral rat liver organic anion transporting polypeptide. Hepatology. 1994 Aug;20(2):411-6. [PubMed:8045503 ]
  4. Hata S, Wang P, Eftychiou N, Ananthanarayanan M, Batta A, Salen G, Pang KS, Wolkoff AW: Substrate specificities of rat oatp1 and ntcp: implications for hepatic organic anion uptake. Am J Physiol Gastrointest Liver Physiol. 2003 Nov;285(5):G829-39. Epub 2003 Jul 3. [PubMed:12842829 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Kast HR, Goodwin B, Tarr PT, Jones SA, Anisfeld AM, Stoltz CM, Tontonoz P, Kliewer S, Willson TM, Edwards PA: Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. J Biol Chem. 2002 Jan 25;277(4):2908-15. Epub 2001 Nov 12. [PubMed:11706036 ]
  2. Fickert P, Zollner G, Fuchsbichler A, Stumptner C, Pojer C, Zenz R, Lammert F, Stieger B, Meier PJ, Zatloukal K, Denk H, Trauner M: Effects of ursodeoxycholic and cholic acid feeding on hepatocellular transporter expression in mouse liver. Gastroenterology. 2001 Jul;121(1):170-83. [PubMed:11438506 ]
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. Rius M, Nies AT, Hummel-Eisenbeiss J, Jedlitschky G, Keppler D: Cotransport of reduced glutathione with bile salts by MRP4 (ABCC4) localized to the basolateral hepatocyte membrane. Hepatology. 2003 Aug;38(2):374-84. [PubMed:12883481 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Bile acid:sodium symporter activity
Specific Function:
Plays a critical role in the sodium-dependent reabsorption of bile acids from the lumen of the small intestine. Plays a key role in cholesterol metabolism.
Gene Name:
SLC10A2
Uniprot ID:
Q12908
Molecular Weight:
37713.405 Da
References
  1. Craddock AL, Love MW, Daniel RW, Kirby LC, Walters HC, Wong MH, Dawson PA: Expression and transport properties of the human ileal and renal sodium-dependent bile acid transporter. Am J Physiol. 1998 Jan;274(1 Pt 1):G157-69. [PubMed:9458785 ]
  2. Saeki T, Matoba K, Furukawa H, Kirifuji K, Kanamoto R, Iwami K: Characterization, cDNA cloning, and functional expression of mouse ileal sodium-dependent bile acid transporter. J Biochem. 1999 Apr;125(4):846-51. [PubMed:10101301 ]
  3. Saeki T, Takahashi N, Kanamoto R, Iwami K: Characterization of cloned mouse Na+/taurocholate cotransporting polypeptide by transient expression in COS-7 cells. Biosci Biotechnol Biochem. 2002 May;66(5):1116-8. [PubMed:12092825 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Boyer JL, Ng OC, Ananthanarayanan M, Hofmann AF, Schteingart CD, Hagenbuch B, Stieger B, Meier PJ: Expression and characterization of a functional rat liver Na+ bile acid cotransport system in COS-7 cells. Am J Physiol. 1994 Mar;266(3 Pt 1):G382-7. [PubMed:8166278 ]
  2. Mita S, Suzuki H, Akita H, Stieger B, Meier PJ, Hofmann AF, Sugiyama Y: Vectorial transport of bile salts across MDCK cells expressing both rat Na+-taurocholate cotransporting polypeptide and rat bile salt export pump. Am J Physiol Gastrointest Liver Physiol. 2005 Jan;288(1):G159-67. Epub 2004 Aug 5. [PubMed:15297262 ]
Comments
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Drug created on August 29, 2007 08:57 / Updated on January 11, 2014 20:13