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Identification
NameProbenecid
Accession NumberDB01032  (APRD00167)
TypeSmall Molecule
GroupsApproved
Description

The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy. [PubChem]

Structure
Thumb
Synonyms
4-((Dipropylamino)sulfonyl)benzoic acid
4-(Di-N-propylsulfamoyl)benzoesaeure
4-(N,N-Dipropylsulfamoyl)benzoesaeure
P-(Dipropylsulfamoyl)benzoic acid
Probenecid acid
Probenecida
Probenecide
Probenecidum
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Benemid Tab 500mgtablet500 mgoralMerck Frosst Canada & Cie, Merck Frosst Canada & Co.1952-12-312000-08-03Canada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Benuryltablet500 mgoralValeant Canada Lp Valeant Canada S.E.C.1974-12-31Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Probenecidtablet, film coated500 mg/1oralMylan Pharmaceuticals Inc.1976-01-13Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralAmerican Health Packaging2015-03-31Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralPhysicians Total Care, Inc.1995-03-28Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralAphena Pharma Solutions Tennessee, Llc1976-07-29Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralHHS/Program Support Center/Supply Service Center1983-07-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralMarlex Pharmaceuticals Inc1976-07-29Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralWatson Laboratories, Inc.1983-07-01Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralLannett Company, Inc.1976-07-29Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Probenecidtablet, film coated500 mg/1oralCarilion Materials Management1976-01-13Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
BenecidNot Available
BenemidNot Available
ProbalanNot Available
ProbecidNot Available
ProbenNot Available
Brand mixtures
NameLabellerIngredients
Pro Biosan KitIcn Canada Ltd.
Probenecid and ColchicineWatson Laboratories, Inc.
SaltsNot Available
Categories
CAS number57-66-9
WeightAverage: 285.359
Monoisotopic: 285.103478791
Chemical FormulaC13H19NO4S
InChI KeyInChIKey=DBABZHXKTCFAPX-UHFFFAOYSA-N
InChI
InChI=1S/C13H19NO4S/c1-3-9-14(10-4-2)19(17,18)12-7-5-11(6-8-12)13(15)16/h5-8H,3-4,9-10H2,1-2H3,(H,15,16)
IUPAC Name
4-(dipropylsulfamoyl)benzoic acid
SMILES
CCCN(CCC)S(=O)(=O)C1=CC=C(C=C1)C(O)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzenesulfonamides
Direct ParentBenzenesulfonamides
Alternative Parents
Substituents
  • Benzenesulfonamide
  • Benzoic acid
  • Benzoic acid or derivatives
  • Benzoyl
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the reduction of serum uric acid concentrations in chronic gouty arthritis and tophaceous gout in patients with frequent disabling gout attacks. Has also been effectively used to promote uric acid excretion in hyperuricemia secondary to the administration of thiazide and related diuretics.
PharmacodynamicsProbenecid is a uricosuric and renal tubular blocking agent and is used in combination with colchicine to treat chronic gouty arthritis when complicated by frequent, recurrent acute attacks of gout. It inhibits the reabsorption of urate at the proximal convoluted tubule, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Effective uricosuria reduces the miscible urate pool, retards urate deposition, and promotes resorption of urate deposits. At the proximal and distal tubles, probenecid competitively inhibits the secretion of many weak organic acids including penicillins, most cephalosporins, and some other β-lactam antibiotics. This results in an increase in the plasma concentrations of acidic drugs eliminated principally by renal secretion, but only a slight increase if the drug is eliminated mainly by filtration. Thus, the drug can be used for therapeutic advantages to increase concentrations of certain β-lactam antibiotics in the treatment of gonorrhea, neurosyphilis, or pelvic inflammatory disease (PID).
Mechanism of actionProbenecid inhibits the tubular reabsorption of urate, thus increasing the urinary excretion of uric acid and decreasing serum urate levels. Probenecid may also reduce plasma binding of urate and inhibit renal secretion of uric acid at subtherapeutic concentrations. The mechanism by which probenecid inhibits renal tubular transport is not known, but the drug may inhibit transport enzymes that require a source of high energy phosphate bonds and/or nonspecifically interfere with substrate access to protein receptor sites on the kidney tubules.
AbsorptionNot Available
Volume of distributionNot Available
Protein binding75-95%
MetabolismNot Available
Route of eliminationExcreted principally in the urine as monoacyl glucuronide and unchanged drug. Alkalinization of urine increases renal probenecid excretion.
Half life6-12 hours
ClearanceNot Available
ToxicityNot Available
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+0.9972
Blood Brain Barrier+0.5486
Caco-2 permeable-0.6074
P-glycoprotein substrateNon-substrate0.626
P-glycoprotein inhibitor INon-inhibitor0.8323
P-glycoprotein inhibitor IINon-inhibitor0.9121
Renal organic cation transporterNon-inhibitor0.8253
CYP450 2C9 substrateNon-substrate0.7012
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6485
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8962
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9318
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.6999
BiodegradationNot ready biodegradable0.863
Rat acute toxicity2.2821 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8521
hERG inhibition (predictor II)Non-inhibitor0.7885
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral500 mg
Capsule; tabletoral
Tablet, film coatedoral500 mg/1
Tabletoral
Prices
Unit descriptionCostUnit
Probenecid 500 mg tablet1.37USD tablet
Colchicine-Probenecid 0.5-500 mg tablet0.87USD tablet
Benuryl 500 mg Tablet0.21USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point195 °CPhysProp
water solubility27.1 mg/LNot Available
logP3.21HANSCH,C ET AL. (1995)
pKa3.4SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.425 mg/mLALOGPS
logP1.52ALOGPS
logP2.44ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)3.53ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area74.68 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity73.81 m3·mol-1ChemAxon
Polarizability29.96 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.48 KB)
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. Butler D: Wartime tactic doubles power of scarce bird-flu drug. Nature. 2005 Nov 3;438(7064):6. Pubmed
External Links
ATC CodesM04AB01
AHFS Codes
  • 40:40.00
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (36.9 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Probenecid.
Acetylsalicylic acidThe therapeutic efficacy of Probenecid can be decreased when used in combination with Acetylsalicylic acid.
AmdinocillinThe serum concentration of Amdinocillin can be increased when it is combined with Probenecid.
Aminosalicylic AcidThe therapeutic efficacy of Probenecid can be decreased when used in combination with Aminosalicylic Acid.
AmoxicillinThe serum concentration of Amoxicillin can be increased when it is combined with Probenecid.
AmpicillinThe serum concentration of Ampicillin can be increased when it is combined with Probenecid.
AvibactamThe serum concentration of Avibactam can be increased when it is combined with Probenecid.
AzidocillinThe serum concentration of Azidocillin can be increased when it is combined with Probenecid.
AzlocillinThe serum concentration of Azlocillin can be increased when it is combined with Probenecid.
BacampicillinThe serum concentration of Bacampicillin can be increased when it is combined with Probenecid.
Benzathine benzylpenicillinThe serum concentration of Benzathine benzylpenicillin can be increased when it is combined with Probenecid.
Benzoic AcidThe serum concentration of Benzoic Acid can be increased when it is combined with Probenecid.
BenzylpenicillinThe serum concentration of Benzylpenicillin can be increased when it is combined with Probenecid.
Bismuth SubsalicylateThe therapeutic efficacy of Probenecid can be decreased when used in combination with Bismuth Subsalicylate.
BumetanideThe risk or severity of adverse effects can be increased when Probenecid is combined with Bumetanide.
CarbenicillinThe serum concentration of Carbenicillin can be increased when it is combined with Probenecid.
CefacetrileThe serum concentration of Cefacetrile can be increased when it is combined with Probenecid.
CefaclorThe serum concentration of Cefaclor can be increased when it is combined with Probenecid.
CefadroxilThe serum concentration of Cefadroxil can be increased when it is combined with Probenecid.
CefalotinThe serum concentration of Cefalotin can be increased when it is combined with Probenecid.
CefamandoleThe serum concentration of Cefamandole can be increased when it is combined with Probenecid.
CefapirinThe serum concentration of Cefapirin can be increased when it is combined with Probenecid.
CefazolinThe serum concentration of Cefazolin can be increased when it is combined with Probenecid.
CefdinirThe serum concentration of Cefdinir can be increased when it is combined with Probenecid.
CefditorenThe serum concentration of Cefditoren can be increased when it is combined with Probenecid.
CefepimeThe serum concentration of Cefepime can be increased when it is combined with Probenecid.
CefiximeThe serum concentration of Cefixime can be increased when it is combined with Probenecid.
CefmenoximeThe serum concentration of Cefmenoxime can be increased when it is combined with Probenecid.
CefmetazoleThe serum concentration of Cefmetazole can be increased when it is combined with Probenecid.
CefonicidThe serum concentration of Cefonicid can be increased when it is combined with Probenecid.
CefoperazoneThe serum concentration of Cefoperazone can be increased when it is combined with Probenecid.
CeforanideThe serum concentration of Ceforanide can be increased when it is combined with Probenecid.
CefotaximeThe serum concentration of Cefotaxime can be increased when it is combined with Probenecid.
CefotetanThe serum concentration of Cefotetan can be increased when it is combined with Probenecid.
CefotiamThe serum concentration of Cefotiam can be increased when it is combined with Probenecid.
CefoxitinThe serum concentration of Cefoxitin can be increased when it is combined with Probenecid.
CefpiramideThe serum concentration of Cefpiramide can be increased when it is combined with Probenecid.
CefpodoximeThe serum concentration of Cefpodoxime can be increased when it is combined with Probenecid.
CefprozilThe serum concentration of Cefprozil can be increased when it is combined with Probenecid.
CefradineThe serum concentration of Cefradine can be increased when it is combined with Probenecid.
Ceftaroline fosamilThe serum concentration of Ceftaroline fosamil can be increased when it is combined with Probenecid.
CeftazidimeThe serum concentration of Ceftazidime can be increased when it is combined with Probenecid.
CeftibutenThe serum concentration of Ceftibuten can be increased when it is combined with Probenecid.
CeftizoximeThe serum concentration of Ceftizoxime can be increased when it is combined with Probenecid.
CeftobiproleThe serum concentration of Ceftobiprole can be increased when it is combined with Probenecid.
CeftriaxoneThe serum concentration of Ceftriaxone can be increased when it is combined with Probenecid.
CefuroximeThe serum concentration of Cefuroxime can be increased when it is combined with Probenecid.
CelecoxibThe serum concentration of Celecoxib can be increased when it is combined with Probenecid.
CephalexinThe serum concentration of Cephalexin can be increased when it is combined with Probenecid.
CephaloglycinThe serum concentration of Cephaloglycin can be increased when it is combined with Probenecid.
ChlorpropamideThe protein binding of Chlorpropamide can be decreased when combined with Probenecid.
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Probenecid.
CloxacillinThe serum concentration of Cloxacillin can be increased when it is combined with Probenecid.
CyclacillinThe serum concentration of Cyclacillin can be increased when it is combined with Probenecid.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Probenecid.
DeferiproneThe serum concentration of Deferiprone can be increased when it is combined with Probenecid.
DexketoprofenThe serum concentration of Dexketoprofen can be increased when it is combined with Probenecid.
DiclofenacThe serum concentration of Diclofenac can be increased when it is combined with Probenecid.
DicloxacillinThe serum concentration of Dicloxacillin can be increased when it is combined with Probenecid.
DiflunisalThe serum concentration of Diflunisal can be increased when it is combined with Probenecid.
DoripenemThe serum concentration of doripenem can be increased when it is combined with Probenecid.
DyphyllineThe serum concentration of Dyphylline can be increased when it is combined with Probenecid.
ErtapenemThe serum concentration of Ertapenem can be increased when it is combined with Probenecid.
Ethacrynic acidThe risk or severity of adverse effects can be increased when Probenecid is combined with Ethacrynic acid.
EtodolacThe serum concentration of Etodolac can be increased when it is combined with Probenecid.
FenoprofenThe serum concentration of Fenoprofen can be increased when it is combined with Probenecid.
FloctafenineThe serum concentration of Floctafenine can be increased when it is combined with Probenecid.
FlucloxacillinThe serum concentration of Flucloxacillin can be increased when it is combined with Probenecid.
FlurbiprofenThe serum concentration of Flurbiprofen can be increased when it is combined with Probenecid.
FurosemideThe risk or severity of adverse effects can be increased when Probenecid is combined with Furosemide.
GanciclovirThe serum concentration of Ganciclovir can be increased when it is combined with Probenecid.
GemifloxacinProbenecid may decrease the excretion rate of Gemifloxacin which could result in a lower serum level and potentially a reduction in efficacy.
GliclazideThe protein binding of Gliclazide can be decreased when combined with Probenecid.
GlimepirideThe protein binding of Glimepiride can be decreased when combined with Probenecid.
GlipizideThe protein binding of Glipizide can be decreased when combined with Probenecid.
GlyburideThe protein binding of Glyburide can be decreased when combined with Probenecid.
Glycerol PhenylbutyrateThe serum concentration of the active metabolites of Glycerol Phenylbutyrate can be increased when Glycerol Phenylbutyrate is used in combination with Probenecid.
HetacillinThe serum concentration of Hetacillin can be increased when it is combined with Probenecid.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Probenecid.
ImipenemThe serum concentration of Imipenem can be increased when it is combined with Probenecid.
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Probenecid.
InfliximabThe serum concentration of Infliximab can be increased when it is combined with Probenecid.
KetoprofenThe serum concentration of Ketoprofen can be increased when it is combined with Probenecid.
KetorolacThe serum concentration of Ketorolac can be increased when it is combined with Probenecid.
LatamoxefThe serum concentration of Latamoxef can be increased when it is combined with Probenecid.
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Probenecid.
LorazepamThe serum concentration of Lorazepam can be increased when it is combined with Probenecid.
Magnesium salicylateThe therapeutic efficacy of Probenecid can be decreased when used in combination with Magnesium salicylate.
Mefenamic acidThe serum concentration of Mefenamic acid can be increased when it is combined with Probenecid.
MeloxicamThe serum concentration of Meloxicam can be increased when it is combined with Probenecid.
MeropenemThe serum concentration of Meropenem can be increased when it is combined with Probenecid.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Probenecid.
MeticillinThe serum concentration of Meticillin can be increased when it is combined with Probenecid.
MezlocillinThe serum concentration of Mezlocillin can be increased when it is combined with Probenecid.
MinoxidilThe serum concentration of Minoxidil can be increased when it is combined with Probenecid.
MoxifloxacinThe serum concentration of Moxifloxacin can be increased when it is combined with Probenecid.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Probenecid.
Mycophenolic acidThe serum concentration of Mycophenolic acid can be increased when it is combined with Probenecid.
NabumetoneThe serum concentration of Nabumetone can be increased when it is combined with Probenecid.
NafcillinThe serum concentration of Nafcillin can be increased when it is combined with Probenecid.
NaproxenThe serum concentration of Naproxen can be increased when it is combined with Probenecid.
NitrofurantoinThe serum concentration of Nitrofurantoin can be increased when it is combined with Probenecid.
NorfloxacinThe serum concentration of Norfloxacin can be increased when it is combined with Probenecid.
OfloxacinThe serum concentration of Ofloxacin can be increased when it is combined with Probenecid.
OseltamivirThe serum concentration of the active metabolites of Oseltamivir can be increased when Oseltamivir is used in combination with Probenecid.
OxacillinThe serum concentration of Oxacillin can be increased when it is combined with Probenecid.
OxaprozinThe serum concentration of Oxaprozin can be increased when it is combined with Probenecid.
PegloticaseThe risk or severity of adverse effects can be increased when Probenecid is combined with Pegloticase.
PhenoxymethylpenicillinThe serum concentration of Phenoxymethylpenicillin can be increased when it is combined with Probenecid.
Phenylacetic acidThe serum concentration of Phenylacetic acid can be increased when it is combined with Probenecid.
PiperacillinThe serum concentration of Piperacillin can be increased when it is combined with Probenecid.
PiroxicamThe serum concentration of Piroxicam can be increased when it is combined with Probenecid.
PivampicillinThe serum concentration of Pivampicillin can be increased when it is combined with Probenecid.
PivmecillinamThe serum concentration of Pivmecillinam can be increased when it is combined with Probenecid.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Probenecid.
Procaine benzylpenicillinThe serum concentration of Procaine benzylpenicillin can be increased when it is combined with Probenecid.
PropacetamolThe serum concentration of the active metabolites of Propacetamol can be increased when Propacetamol is used in combination with Probenecid.
Salicylate-sodiumThe therapeutic efficacy of Probenecid can be decreased when used in combination with Salicylate-sodium.
SalsalateThe therapeutic efficacy of Probenecid can be decreased when used in combination with Salsalate.
Sodium phenylbutyrateThe serum concentration of the active metabolites of Sodium phenylbutyrate can be increased when Sodium phenylbutyrate is used in combination with Probenecid.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Probenecid.
SulindacThe serum concentration of Sulindac can be increased when it is combined with Probenecid.
Tiaprofenic acidThe serum concentration of Tiaprofenic acid can be increased when it is combined with Probenecid.
TicarcillinThe serum concentration of Ticarcillin can be increased when it is combined with Probenecid.
TolazamideThe protein binding of Tolazamide can be decreased when combined with Probenecid.
TolbutamideThe protein binding of Tolbutamide can be decreased when combined with Probenecid.
TolmetinThe serum concentration of Tolmetin can be increased when it is combined with Probenecid.
TorasemideThe risk or severity of adverse effects can be increased when Probenecid is combined with Torasemide.
ValganciclovirThe serum concentration of Valganciclovir can be increased when it is combined with Probenecid.
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Probenecid.
Food Interactions
  • Increase liquid intake, avoid alcohol.
  • Take with food to reduce irritation.

Targets

1. Solute carrier family 22 member 6

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

References:

  1. Takeda M, Narikawa S, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. Eur J Pharmacol. 2001 May 11;419(2-3):113-20. 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. Hashimoto T, Narikawa S, Huang XL, Minematsu T, Usui T, Kamimura H, Endou H: Characterization of the renal tubular transport of zonampanel, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, by human organic anion transporters. Drug Metab Dispos. 2004 Oct;32(10):1096-102. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Solute carrier family 22 member 11

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Enomoto A, Takeda M, Shimoda M, Narikawa S, Kobayashi Y, Kobayashi Y, Yamamoto T, Sekine T, Cha SH, Niwa T, Endou H: Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. J Pharmacol Exp Ther. 2002 Jun;301(3):797-802. Pubmed
  2. 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
  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. Hashimoto T, Narikawa S, Huang XL, Minematsu T, Usui T, Kamimura H, Endou H: Characterization of the renal tubular transport of zonampanel, a novel alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid receptor antagonist, by human organic anion transporters. Drug Metab Dispos. 2004 Oct;32(10):1096-102. Pubmed

3. Solute carrier family 22 member 8

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

References:

  1. 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
  2. Takeda M, Narikawa S, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. Eur J Pharmacol. 2001 May 11;419(2-3):113-20. Pubmed
  3. 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
  4. 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
  5. Sweet DH, Chan LM, Walden R, Yang XP, Miller DS, Pritchard JB: Organic anion transporter 3 (Slc22a8) is a dicarboxylate exchanger indirectly coupled to the Na+ gradient. Am J Physiol Renal Physiol. 2003 Apr;284(4):F763-9. Epub 2002 Dec 17. Pubmed
  6. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed

4. Pannexin-1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Pannexin-1 Q96RD7 Details

References:

  1. Silverman W, Locovei S, Dahl G: Probenecid, a gout remedy, inhibits pannexin 1 channels. Am J Physiol Cell Physiol. 2008 Sep;295(3):C761-7. Epub 2008 Jul 2. Pubmed
  2. Ransford GA, Fregien N, Qiu F, Dahl G, Conner GE, Salathe M: Pannexin 1 contributes to ATP release in airway epithelia. Am J Respir Cell Mol Biol. 2009 Nov;41(5):525-34. Epub 2009 Feb 12. Pubmed
  3. Ma W, Hui H, Pelegrin P, Surprenant A: Pharmacological characterization of pannexin-1 currents expressed in mammalian cells. J Pharmacol Exp Ther. 2009 Feb;328(2):409-18. Epub 2008 Nov 20. Pubmed
  4. Silverman WR, de Rivero Vaccari JP, Locovei S, Qiu F, Carlsson SK, Scemes E, Keane RW, Dahl G: The pannexin 1 channel activates the inflammasome in neurons and astrocytes. J Biol Chem. 2009 Jul 3;284(27):18143-51. Epub 2009 May 5. Pubmed
  5. Bunse S, Locovei S, Schmidt M, Qiu F, Zoidl G, Dahl G, Dermietzel R: The potassium channel subunit Kvbeta3 interacts with pannexin 1 and attenuates its sensitivity to changes in redox potentials. FEBS J. 2009 Nov;276(21):6258-70. Epub 2009 Sep 24. Pubmed

Enzymes

1. Cytochrome P450 2C9

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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. Epub 2009 Nov 24. Pubmed

2. Cytochrome P450 2C19

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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. Epub 2009 Nov 24. Pubmed

3. Cytochrome P450 2C8

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

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. Epub 2009 Nov 24. Pubmed

4. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inducer

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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. Epub 2009 Nov 24. Pubmed

Carriers

1. Serum albumin

Kind: Protein

Organism: Human

Pharmacological action: no

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. Dundee JW, Halliday NJ, McMurray TJ: Aspirin and probenecid pretreatment influences the potency of thiopentone and the onset of action of midazolam. Eur J Anaesthesiol. 1986 May;3(3):247-51. Pubmed
  2. Gewirtz DA, Holt SA: Protein binding as a component of drug interaction in cellular pharmacokinetic studies. Effects of probenecid on transport and accumulation of methotrexate in Ehrlich ascites tumor cells in vitro. Biochem Pharmacol. 1985 Mar 15;34(6):747-54. Pubmed
  3. Hansen-Moller J, Schmit U: Rapid high-performance liquid chromatographic assay for the simultaneous determination of probenecid and its glucuronide in urine. Irreversible binding of probenecid to serum albumin. J Pharm Biomed Anal. 1991;9(1):65-73. Pubmed

Transporters

1. Solute carrier family 22 member 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 2 O15244 Details

References:

  1. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. Pubmed

2. Solute carrier family 22 member 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 1 O15245 Details

References:

  1. Arndt P, Volk C, Gorboulev V, Budiman T, Popp C, Ulzheimer-Teuber I, Akhoundova A, Koppatz S, Bamberg E, Nagel G, Koepsell H: Interaction of cations, anions, and weak base quinine with rat renal cation transporter rOCT2 compared with rOCT1. Am J Physiol Renal Physiol. 2001 Sep;281(3):F454-68. Pubmed

3. Canalicular multispecific organic anion transporter 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 2 O15438 Details

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. Zeng H, Chen ZS, Belinsky MG, Rea PA, Kruh GD: Transport of methotrexate (MTX) and folates by multidrug resistance protein (MRP) 3 and MRP1: effect of polyglutamylation on MTX transport. Cancer Res. 2001 Oct 1;61(19):7225-32. Pubmed
  3. Zamek-Gliszczynski MJ, Xiong H, Patel NJ, Turncliff RZ, Pollack GM, Brouwer KL: Pharmacokinetics of 5 (and 6)-carboxy-2’,7’-dichlorofluorescein and its diacetate promoiety in the liver. J Pharmacol Exp Ther. 2003 Feb;304(2):801-9. Pubmed

4. Multidrug resistance-associated protein 4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 4 O15439 Details

References:

  1. van Aubel RA, Smeets PH, Peters JG, Bindels RJ, Russel FG: The MRP4/ABCC4 gene encodes a novel apical organic anion transporter in human kidney proximal tubules: putative efflux pump for urinary cAMP and cGMP. J Am Soc Nephrol. 2002 Mar;13(3):595-603. Pubmed
  2. Chen ZS, Lee K, Walther S, Raftogianis RB, Kuwano M, Zeng H, Kruh GD: Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res. 2002 Jun 1;62(11):3144-50. Pubmed
  3. 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

5. Multidrug resistance-associated protein 5

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 5 O15440 Details

References:

  1. Jedlitschky G, Burchell B, Keppler D: The multidrug resistance protein 5 functions as an ATP-dependent export pump for cyclic nucleotides. J Biol Chem. 2000 Sep 29;275(39):30069-74. Pubmed

6. Monocarboxylate transporter 2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Monocarboxylate transporter 2 O60669 Details

References:

  1. Broer S, Broer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW: Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes. Biochem J. 1999 Aug 1;341 ( Pt 3):529-35. Pubmed

7. Solute carrier family 22 member 5

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 5 O76082 Details

References:

  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. Pubmed

8. Multidrug resistance-associated protein 6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 6 O95255 Details

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

9. Multidrug resistance protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Gao J, Murase O, Schowen RL, Aube J, Borchardt RT: A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells. Pharm Res. 2001 Feb;18(2):171-6. Pubmed
  2. Honda Y, Ushigome F, Koyabu N, Morimoto S, Shoyama Y, Uchiumi T, Kuwano M, Ohtani H, Sawada Y: Effects of grapefruit juice and orange juice components on P-glycoprotein- and MRP2-mediated drug efflux. Br J Pharmacol. 2004 Dec;143(7):856-64. Epub 2004 Oct 25. Pubmed
  3. Minderman H, Brooks TA, O’Loughlin KL, Ojima I, Bernacki RJ, Baer MR: Broad-spectrum modulation of ATP-binding cassette transport proteins by the taxane derivatives ortataxel (IDN-5109, BAY 59-8862) and tRA96023. Cancer Chemother Pharmacol. 2004 May;53(5):363-9. Epub 2004 Jan 27. Pubmed

10. Multidrug resistance-associated protein 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 1 P33527 Details

References:

  1. 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
  2. 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
  3. Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: Reversal of MRP-mediated multidrug resistance in human lung cancer cells by the antiprogestatin drug RU486. Biochem Biophys Res Commun. 1999 May 19;258(3):513-8. Pubmed
  4. Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B: Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. Pubmed
  5. Hooijberg JH, Broxterman HJ, Kool M, Assaraf YG, Peters GJ, Noordhuis P, Scheper RJ, Borst P, Pinedo HM, Jansen G: Antifolate resistance mediated by the multidrug resistance proteins MRP1 and MRP2. Cancer Res. 1999 Jun 1;59(11):2532-5. Pubmed
  6. Legrand O, Simonin G, Beauchamp-Nicoud A, Zittoun R, Marie JP: Simultaneous activity of MRP1 and Pgp is correlated with in vitro resistance to daunorubicin and with in vivo resistance in adult acute myeloid leukemia. Blood. 1999 Aug 1;94(3):1046-56. Pubmed
  7. Legrand O, Simonin G, Perrot JY, Zittoun R, Marie JP: Both Pgp and MRP1 activities using calcein-AM contribute to drug resistance in AML. Adv Exp Med Biol. 1999;457:161-75. Pubmed
  8. 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
  9. Issandou M, Grand-Perret T: Multidrug resistance P-glycoprotein is not involved in cholesterol esterification. Biochem Biophys Res Commun. 2000 Dec 20;279(2):369-77. Pubmed

11. Solute carrier organic anion transporter family member 1A2

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

References:

  1. Sugiyama D, Kusuhara H, Shitara Y, Abe T, Meier PJ, Sekine T, Endou H, Suzuki H, Sugiyama Y: Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier. J Pharmacol Exp Ther. 2001 Jul;298(1):316-22. Pubmed
  2. 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

12. Monocarboxylate transporter 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Monocarboxylate transporter 1 P53985 Details

References:

  1. Broer S, Broer A, Schneider HP, Stegen C, Halestrap AP, Deitmer JW: Characterization of the high-affinity monocarboxylate transporter MCT2 in Xenopus laevis oocytes. Biochem J. 1999 Aug 1;341 ( Pt 3):529-35. Pubmed

13. Sodium/bile acid cotransporter

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Sodium/bile acid cotransporter Q14973 Details

References:

  1. Hagenbuch B, Stieger B, Foguet M, Lubbert H, Meier PJ: Functional expression cloning and characterization of the hepatocyte Na+/bile acid cotransport system. Proc Natl Acad Sci U S A. 1991 Dec 1;88(23):10629-33. Pubmed

14. Solute carrier family 22 member 6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 6 Q4U2R8 Details

References:

  1. Cihlar T, Ho ES: Fluorescence-based assay for the interaction of small molecules with the human renal organic anion transporter 1. Anal Biochem. 2000 Jul 15;283(1):49-55. Pubmed
  2. 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
  3. Takeda M, Narikawa S, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. Eur J Pharmacol. 2001 May 11;419(2-3):113-20. Pubmed
  4. 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
  5. Ichida K, Hosoyamada M, Kimura H, Takeda M, Utsunomiya Y, Hosoya T, Endou H: Urate transport via human PAH transporter hOAT1 and its gene structure. Kidney Int. 2003 Jan;63(1):143-55. Pubmed
  6. 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
  7. 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
  8. Race JE, Grassl SM, Williams WJ, Holtzman EJ: Molecular cloning and characterization of two novel human renal organic anion transporters (hOAT1 and hOAT3). Biochem Biophys Res Commun. 1999 Feb 16;255(2):508-14. Pubmed
  9. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed
  10. 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
  11. 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
  12. Tsuda M, Sekine T, Takeda M, Cha SH, Kanai Y, Kimura M, Endou H: Transport of ochratoxin A by renal multispecific organic anion transporter 1. J Pharmacol Exp Ther. 1999 Jun;289(3):1301-5. Pubmed
  13. Takeda M, Tojo A, Sekine T, Hosoyamada M, Kanai Y, Endou H: Role of organic anion transporter 1 (OAT1) in cephaloridine (CER)-induced nephrotoxicity. Kidney Int. 1999 Dec;56(6):2128-36. Pubmed
  14. Sugiyama D, Kusuhara H, Shitara Y, Abe T, Meier PJ, Sekine T, Endou H, Suzuki H, Sugiyama Y: Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier. J Pharmacol Exp Ther. 2001 Jul;298(1):316-22. Pubmed
  15. Uwai Y, Iwamoto K: Transport of aminopterin by human organic anion transporters hOAT1 and hOAT3: Comparison with methotrexate. Drug Metab Pharmacokinet. 2010;25(2):163-9. Pubmed

15. Solute carrier family 22 member 10

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 10 Q63ZE4 Details

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

16. Solute carrier family 22 member 8

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

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. Takeda M, Narikawa S, Hosoyamada M, Cha SH, Sekine T, Endou H: Characterization of organic anion transport inhibitors using cells stably expressing human organic anion transporters. Eur J Pharmacol. 2001 May 11;419(2-3):113-20. Pubmed
  3. 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
  4. 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
  5. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed
  6. 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
  7. 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
  8. 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. Sugiyama D, Kusuhara H, Shitara Y, Abe T, Meier PJ, Sekine T, Endou H, Suzuki H, Sugiyama Y: Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier. J Pharmacol Exp Ther. 2001 Jul;298(1):316-22. Pubmed
  10. 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
  11. Uwai Y, Iwamoto K: Transport of aminopterin by human organic anion transporters hOAT1 and hOAT3: Comparison with methotrexate. Drug Metab Pharmacokinet. 2010;25(2):163-9. Pubmed
  12. Lai Y, Sampson KE, Balogh LM, Brayman TG, Cox SR, Adams WJ, Kumar V, Stevens JC: Preclinical and clinical evidence for the collaborative transport and renal secretion of an oxazolidinone antibiotic by organic anion transporter 3 (OAT3/SLC22A8) and multidrug and toxin extrusion protein 1 (MATE1/SLC47A1). J Pharmacol Exp Ther. 2010 Sep 1;334(3):936-44. Epub 2010 Jun 2. Pubmed

17. Canalicular multispecific organic anion transporter 1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Canalicular multispecific organic anion transporter 1 Q92887 Details

References:

  1. 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
  2. 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
  3. Bakos E, Evers R, Sinko E, Varadi A, Borst P, Sarkadi B: Interactions of the human multidrug resistance proteins MRP1 and MRP2 with organic anions. Mol Pharmacol. 2000 Apr;57(4):760-8. Pubmed
  4. Horikawa M, Kato Y, Tyson CA, Sugiyama Y: The potential for an interaction between MRP2 (ABCC2) and various therapeutic agents: probenecid as a candidate inhibitor of the biliary excretion of irinotecan metabolites. Drug Metab Pharmacokinet. 2002;17(1):23-33. Pubmed
  5. Zamek-Gliszczynski MJ, Xiong H, Patel NJ, Turncliff RZ, Pollack GM, Brouwer KL: Pharmacokinetics of 5 (and 6)-carboxy-2’,7’-dichlorofluorescein and its diacetate promoiety in the liver. J Pharmacol Exp Ther. 2003 Feb;304(2):801-9. Pubmed
  6. 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
  7. Chen C, Scott D, Hanson E, Franco J, Berryman E, Volberg M, Liu X: Impact of Mrp2 on the biliary excretion and intestinal absorption of furosemide, probenecid, and methotrexate using Eisai hyperbilirubinemic rats. Pharm Res. 2003 Jan;20(1):31-7. Pubmed

18. ATP-binding cassette sub-family C member 11

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
ATP-binding cassette sub-family C member 11 Q96J66 Details

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

19. Solute carrier family 22 member 11

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

References:

  1. Enomoto A, Takeda M, Shimoda M, Narikawa S, Kobayashi Y, Kobayashi Y, Yamamoto T, Sekine T, Cha SH, Niwa T, Endou H: Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. J Pharmacol Exp Ther. 2002 Jun;301(3):797-802. Pubmed
  2. 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
  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. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed

20. Solute carrier organic anion transporter family member 1C1

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1C1 Q9NYB5 Details

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

21. Solute carrier family 22 member 7

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 7 Q9Y694 Details

References:

  1. Enomoto A, Takeda M, Shimoda M, Narikawa S, Kobayashi Y, Kobayashi Y, Yamamoto T, Sekine T, Cha SH, Niwa T, Endou H: Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors. J Pharmacol Exp Ther. 2002 Jun;301(3):797-802. Pubmed
  2. Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. Pubmed

22. Solute carrier family 22 member 12

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 12 Q96S37 Details

References:

  1. Shin HJ, Takeda M, Enomoto A, Fujimura M, Miyazaki H, Anzai N, Endou H: Interactions of urate transporter URAT1 in human kidney with uricosuric drugs. Nephrology (Carlton). 2011 Feb;16(2):156-62. doi: 10.1111/j.1440-1797.2010.01368.×. Pubmed

23. Solute carrier family 2, facilitated glucose transporter member 9

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 2, facilitated glucose transporter member 9 Q9NRM0 Details

References:

  1. http://www.pharmgkb.org/pathway/PA165980774

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:13