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Identification
NameGlyburide
Accession NumberDB01016  (APRD00233)
TypeSmall Molecule
GroupsApproved
Description

Glyburide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in their dose, rate of absorption, duration of action, route of elimination and binding site on their target pancreatic β cell receptor. Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. The risk of hypoglycemia is increased in elderly, debilitated and malnourished individuals. Glyburide has been shown to decrease fasting plasma glucose, postprandial blood glucose and glycosolated hemoglobin (HbA1c) levels (reflective of the last 8-10 weeks of glucose control). Glyburide appears to be completely metabolized, likely in the liver. Although its metabolites exert a small hypoglycemic effect, their contribution to glyburide’s hypoglycemic effect is thought to be clinically unimportant. Glyburide metabolites are excreted in urine and feces in approximately equal proportions. The half-life of glyburide appears to be unaffected in those with a creatinine clearance of greater than 29 ml/min/1.73m2.

Structure
Thumb
Synonyms
1-((P-(2-(5-chloro-O-Anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea
1-(P-(2-(5-chloro-2-Methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexylurea
5-chloro-N-(2-(4-((((Cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxybenzamide
Diabeta
Glibenclamida
Glibenclamide
Glibenclamidum
Glyburide
Glynase
Micronase
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Ava-glyburidetablet2.5 mgoralAvanstra Inc2011-08-112014-08-21Canada
Ava-glyburidetablet5 mgoralAvanstra Inc2011-08-112014-08-21Canada
Diabetatablet5 mgoralSanofi Aventis Canada Inc1997-02-21Not applicableCanada
Diabetatablet1.25 mg/1oralSanofi Aventis U.S. Llc2009-06-01Not applicableUs
Diabetatablet2.5 mgoralSanofi Aventis Canada Inc1997-05-28Not applicableCanada
Diabetatablet5 mg/1oralSanofi Aventis U.S. Llc2009-06-01Not applicableUs
Diabetatablet2.5 mg/1oralSanofi Aventis U.S. Llc2009-06-01Not applicableUs
Diabeta 5mgtablet5 mgoralHoechst Canada Inc.1971-12-311996-09-09Canada
Diabeta Tab 2.5mgtablet2.5 mgoralHoechst Canada Inc.1978-12-311997-08-05Canada
Diabeta Tab 5mgtablet5 mgoralHoechst Roussel Canada Inc.1993-12-311999-08-11Canada
Diabeta Tablets 2.5mgtablet2.5 mgoralHoechst Roussel Canada Inc.1995-12-311999-08-11Canada
Dom-glyburidetablet5 mgoralDominion Pharmacal1998-03-20Not applicableCanada
Dom-glyburidetablet2.5 mgoralDominion Pharmacal1998-03-202010-02-16Canada
Euglucontablet5 mgoralPharmascience Inc1986-12-31Not applicableCanada
Euglucontablet2.5 mgoralPharmascience Inc1986-12-312009-10-14Canada
Glyburidetablet1.25 mg/1oralTeva Pharmaceuticals USA Inc1984-05-01Not applicableUs
Glyburidetablet5 mg/1oralAvera Mc Kennan Hospital2015-03-01Not applicableUs
Glyburidetablet2.5 mg/1oralTeva Pharmaceuticals USA Inc1984-05-01Not applicableUs
Glyburidetablet2.5 mg/1oralLegacy Pharmaceutical Packaging2010-05-18Not applicableUs
Glyburidetablet5 mg/1oralTeva Pharmaceuticals USA Inc1984-05-01Not applicableUs
Glyburidetablet2.5 mg/1oralPd Rx Pharmaceuticals, Inc.1984-05-01Not applicableUs
Glyburidetablet2.5 mgoralSanis Health Inc2010-05-12Not applicableCanada
Glyburidetablet1.25 mg/1oralAphena Pharma Solutions Tennessee, Llc1984-05-01Not applicableUs
Glyburidetablet2.5 mg/1oralAphena Pharma Solutions Tennessee, Llc1984-05-01Not applicableUs
Glyburidetablet5 mgoralSanis Health Inc2010-05-12Not applicableCanada
Glyburidetablet5 mg/1oralAphena Pharma Solutions Tennessee, Llc1984-05-01Not applicableUs
Glyburidetablet5 mg/1oralPd Rx Pharmaceuticals, Inc.1994-04-01Not applicableUs
Glyburide Tablets 2.5mgtablet2.5 mgoralPrempharm Inc1996-12-302005-08-05Canada
Glyburide Tablets 5mgtablet5 mgoralPrempharm Inc1996-12-302005-08-05Canada
Glyburide-2.5 Tab 2.5mgtablet2.5 mgoralPro Doc Limitee1992-12-31Not applicableCanada
Glyburide-5 Tab 5mgtablet5 mgoralPro Doc Limitee1992-12-312010-07-13Canada
Glynasetablet1.5 mg/1oralPharmacia and Upjohn Company1992-03-04Not applicableUs
Glynasetablet6 mg/1oralPharmacia and Upjohn Company1992-03-04Not applicableUs
Glynasetablet3 mg/1oralPharmacia and Upjohn Company1992-03-04Not applicableUs
Med Glybe Tab 2.5mgtablet2.5 mgoralMedican Pharma Incorporated1995-12-312011-03-29Canada
Med Glybe Tab 5mgtablet5 mgoralMedican Pharma Incorporated1994-12-312011-03-29Canada
Mylan-glybetablet5 mgoralMylan Pharmaceuticals Ulc1991-12-31Not applicableCanada
Mylan-glybetablet2.5 mgoralMylan Pharmaceuticals Ulc1991-12-31Not applicableCanada
Ntp-glyburidetablet5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Ntp-glyburidetablet2.5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Nu-glyburide Tab 2.5mgtablet2.5 mgoralNu Pharm Inc1993-12-312012-09-04Canada
Nu-glyburide Tab 5mgtablet5 mgoralNu Pharm Inc1993-12-312012-09-04Canada
Penta-glyburide - 2.5mgtablet2.5 mgoralPentapharm Ltd.1997-06-252004-07-30Canada
Penta-glyburide - 5mgtablet5 mgoralPentapharm Ltd.1997-06-252004-07-30Canada
PMS-glyburidetablet2.5 mgoralPharmascience Inc1998-01-292009-11-19Canada
PMS-glyburidetablet5 mgoralPharmascience Inc1998-01-29Not applicableCanada
Pro-glyburidetablet5 mgoralPro Doc Limitee2009-02-10Not applicableCanada
Ratio-glyburidetablet5 mgoralRatiopharm Inc Division Of Teva Canada Limited1990-12-312014-09-19Canada
Ratio-glyburidetablet2.5 mgoralRatiopharm Inc Division Of Teva Canada Limited1990-12-312014-09-19Canada
Riva-glyburidetablet5 mgoralPharmel Inc1998-06-04Not applicableCanada
Riva-glyburidetablet2.5 mgoralLaboratoire Riva Inc2000-05-232013-07-31Canada
Riva-glyburidetablet2.5 mgoralPharmel Inc1998-06-042010-02-16Canada
Riva-glyburidetablet5 mgoralLaboratoire Riva Inc2000-05-23Not applicableCanada
Sandoz Glyburidetablet5 mgoralSandoz Canada Incorporated2003-08-13Not applicableCanada
Sandoz Glyburidetablet2.5 mgoralSandoz Canada Incorporated2003-08-13Not applicableCanada
Teva-glyburidetablet5 mgoralTeva Canada Limited1991-12-31Not applicableCanada
Teva-glyburidetablet2.5 mgoralTeva Canada Limited1991-12-31Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Glyburide Tab 2.5mgtablet2.5 mgoralApotex Inc1991-12-31Not applicableCanada
Apo Glyburide Tab 5mgtablet5 mgoralApotex Inc1991-12-31Not applicableCanada
Glyburidetablet1.25 mg/1oralbryant ranch prepack2010-10-05Not applicableUs
Glyburidetablet6 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-28Not applicableUs
Glyburidetablet2.5 mg/1oralAidarex Pharmaceuticals LLC2010-10-05Not applicableUs
Glyburidetablet2.5 mg/1oralCore Pharma, Llc2002-08-062015-12-29Us
Glyburidetablet2.5 mg/1oralBlenheim Pharmacal, Inc.2013-11-15Not applicableUs
Glyburidetablet6 mg/1oralPhysicians Total Care, Inc.2003-07-02Not applicableUs
Glyburidetablet2.5 mg/1oralMylan Institutional Inc.1996-07-30Not applicableUs
Glyburidetablet5 mg/1oralMedsource Pharmaceuticals2010-10-05Not applicableUs
Glyburidetablet5 mg/1oralMajor Pharmaceuticals2002-08-06Not applicableUs
Glyburidetablet6 mg/1oralWest Ward Pharmaceuticals Corp2003-08-01Not applicableUs
Glyburidetablet1.5 mg/1oralTeva Pharmaceuticals USA Inc1999-05-11Not applicableUs
Glyburidetablet2.5 mg/1oralbryant ranch prepack1995-08-30Not applicableUs
Glyburidetablet5 mg/1oralClinical Solutions Wholesale1995-08-30Not applicableUs
Glyburidetablet5 mg/1oralMc Kesson Contract Packaging2012-01-09Not applicableUs
Glyburidetablet1.5 mg/1oralPhysicians Total Care, Inc.2006-12-07Not applicableUs
Glyburidetablet6 mg/1oralDispensing Solutions, Inc.1999-05-12Not applicableUs
Glyburidetablet5 mg/1oralUnit Dose Services2011-07-18Not applicableUs
Glyburidetablet2.5 mg/1oralMajor Pharmaceuticals2002-08-06Not applicableUs
Glyburidetablet3 mg/1oralWest Ward Pharmaceuticals Corp2003-08-01Not applicableUs
Glyburidetablet5 mg/1oralbryant ranch prepack1995-08-30Not applicableUs
Glyburidetablet2.5 mg/1oralClinical Solutions Wholesale1995-08-30Not applicableUs
Glyburidetablet5 mg/1oralPreferred Pharmaceuticals, Inc.2012-01-30Not applicableUs
Glyburidetablet2.5 mg/1oralDispensing Solutions, Inc.2010-10-05Not applicableUs
Glyburidetablet3 mg/1oralPd Rx Pharmaceuticals, Inc.2011-06-28Not applicableUs
Glyburidetablet5 mg/1oralAidarex Pharmaceuticals LLC2010-10-05Not applicableUs
Glyburidetablet3 mg/1oralPhysicians Total Care, Inc.1999-02-24Not applicableUs
Glyburidetablet1.25 mg/1oralMajor Pharmaceuticals2002-08-06Not applicableUs
Glyburidetablet1.5 mg/1oralWest Ward Pharmaceuticals Corp2003-08-01Not applicableUs
Glyburidetablet5 mg/1oralDIRECT RX2015-12-03Not applicableUs
Glyburidetablet5 mg/1oralCitron Pharma LLC2007-10-18Not applicableUs
Glyburidetablet5 mg/1oralPreferred Pharmaceuticals Inc.2015-08-27Not applicableUs
Glyburidetablet5 mg/1oralMed Vantx, Inc.2011-07-18Not applicableUs
Glyburidetablet5 mg/1oralAv Kare, Inc.2014-09-25Not applicableUs
Glyburidetablet5 mg/1oralA S Medication Solutions2007-10-18Not applicableUs
Glyburidetablet5 mg/1oralHeritage Pharmaceuticals Inc.2010-10-05Not applicableUs
Glyburidetablet1.25 mg/1oralPhysicians Total Care, Inc.1994-11-18Not applicableUs
Glyburidetablet2.5 mg/1oralUnit Dose Services2010-10-05Not applicableUs
Glyburidetablet2.5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1995-08-30Not applicableUs
Glyburidetablet5 mg/1oralTeva Pharmaceuticals USA Inc1995-08-30Not applicableUs
Glyburidetablet2.5 mg/1oralDIRECT RX2015-12-03Not applicableUs
Glyburidetablet2.5 mg/1oralCitron Pharma LLC2007-10-18Not applicableUs
Glyburidetablet5 mg/1oralAmerican Health Packaging2014-08-22Not applicableUs
Glyburidetablet5 mg/1oralAurobindo Pharma Limited2007-10-18Not applicableUs
Glyburidetablet2.5 mg/1oralAv Kare, Inc.2014-09-25Not applicableUs
Glyburidetablet5 mg/1oralProficient Rx LP2010-10-05Not applicableUs
Glyburidetablet2.5 mg/1oralHeritage Pharmaceuticals Inc.2010-10-05Not applicableUs
Glyburidetablet2.5 mg/1oralPhysicians Total Care, Inc.1994-08-26Not applicableUs
Glyburidetablet5 mg/1oralLake Erie Medical DBA Quality Care Products LLC2011-02-23Not applicableUs
Glyburidetablet2.5 mg/1oralREMEDYREPACK INC.2015-03-27Not applicableUs
Glyburidetablet1.25 mg/1oralCitron Pharma LLC2007-10-18Not applicableUs
Glyburidetablet6 mg/1oralDAVA Pharmaceuticals, Inc.1997-12-22Not applicableUs
Glyburidetablet2.5 mg/1oralAurobindo Pharma Limited2007-10-18Not applicableUs
Glyburidetablet6 mg/1oralRebel Distributors Corp1999-05-12Not applicableUs
Glyburidetablet2.5 mg/1oralProficient Rx LP2010-10-05Not applicableUs
Glyburidetablet1.25 mg/1oralHeritage Pharmaceuticals Inc.2010-10-05Not applicableUs
Glyburidetablet5 mg/1oralPhysicians Total Care, Inc.1994-04-26Not applicableUs
Glyburidetablet2.5 mg/1oralREMEDYREPACK INC.2011-08-23Not applicableUs
Glyburidetablet5 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1995-08-30Not applicableUs
Glyburidetablet2.5 mg/1oralTeva Pharmaceuticals USA Inc1995-08-30Not applicableUs
Glyburidetablet1.5 mg/1oralHikma Pharmaceutical2003-08-01Not applicableUs
Glyburidetablet5 mg/1oralPd Rx Pharmaceuticals, Inc.2002-08-06Not applicableUs
Glyburidetablet3 mg/1oralDAVA Pharmaceuticals, Inc.1997-12-22Not applicableUs
Glyburidetablet1.25 mg/1oralAurobindo Pharma Limited2007-10-18Not applicableUs
Glyburidetablet5 mg/1oralRebel Distributors Corp2010-10-05Not applicableUs
Glyburidetablet5 mg/1oralRebel Distributors Corp2002-08-06Not applicableUs
Glyburidetablet2.5 mg/1oralREMEDYREPACK INC.2013-07-01Not applicableUs
Glyburidetablet2.5 mg/1oralREMEDYREPACK INC.2011-07-08Not applicableUs
Glyburidetablet6 mg/1oralMylan Pharmaceuticals Inc.1999-09-17Not applicableUs
Glyburidetablet1.25 mg/1oralTeva Pharmaceuticals USA Inc1995-08-30Not applicableUs
Glyburidetablet3 mg/1oralHikma Pharmaceutical2003-08-01Not applicableUs
Glyburidetablet5 mg/1oralCardinal Health2010-08-04Not applicableUs
Glyburidetablet1.5 mg/1oralDAVA Pharmaceuticals, Inc.1997-12-22Not applicableUs
Glyburidetablet5 mg/1oralTYA Pharmaceuticals2010-10-05Not applicableUs
Glyburidetablet1.25 mg/1oralLake Erie Medical DBA Quality Care Products LLC1995-08-30Not applicableUs
Glyburidetablet2.5 mg/1oralRebel Distributors Corp2002-08-06Not applicableUs
Glyburidetablet5 mg/1oralREMEDYREPACK INC.2013-05-28Not applicableUs
Glyburidetablet2.5 mg/1oralREMEDYREPACK INC.2011-04-18Not applicableUs
Glyburidetablet3 mg/1oralMylan Pharmaceuticals Inc.1999-09-17Not applicableUs
Glyburidetablet6 mg/1oralTeva Pharmaceuticals USA Inc1999-05-12Not applicableUs
Glyburidetablet6 mg/1oralHikma Pharmaceutical2003-08-01Not applicableUs
Glyburidetablet5 mg/1oralCardinal Health2011-05-13Not applicableUs
Glyburidetablet5 mg/1oralContract Pharmacy Services Pa2002-08-06Not applicableUs
Glyburidetablet5 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation1995-08-30Not applicableUs
Glyburidetablet2.5 mg/1oralLake Erie Medical DBA Quality Care Products LLC1995-08-30Not applicableUs
Glyburidetablet5 mg/1oralCore Pharma, Llc2002-08-062015-12-29Us
Glyburidetablet5 mg/1oralBlenheim Pharmacal, Inc.2013-10-01Not applicableUs
Glyburidetablet5 mg/1oralMylan Institutional Inc.1996-07-30Not applicableUs
Glyburidetablet5 mg/1oralREMEDYREPACK INC.2010-10-11Not applicableUs
Glyburidetablet1.5 mg/1oralMylan Pharmaceuticals Inc.1999-09-17Not applicableUs
Glyburidetablet3 mg/1oralTeva Pharmaceuticals USA Inc1999-05-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DaonilNot Available
DelmideNot Available
MicronaseNot Available
Novo-GlyburideNovopharm
Semi-DaonilNot Available
Brand mixtures
NameLabellerIngredients
GlucovanceBristol Myers Squibb Company
Glyburide (micronized) and Metformin HydrochlorideActavis Pharma Manufacturing Pvt. Ltd.
Glyburide and MetforminRebel Distributors Corp
Glyburide and Metformin HydrochlorideTeva Pharmaceuticals USA Inc
Glyburide-metformin HydrochlorideBlenheim Pharmacal, Inc.
SaltsNot Available
Categories
UNIISX6K58TVWC
CAS number10238-21-8
WeightAverage: 494.004
Monoisotopic: 493.143819418
Chemical FormulaC23H28ClN3O5S
InChI KeyInChIKey=ZNNLBTZKUZBEKO-UHFFFAOYSA-N
InChI
InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
IUPAC Name
5-chloro-N-[2-(4-{[(cyclohexylcarbamoyl)amino]sulfonyl}phenyl)ethyl]-2-methoxybenzamide
SMILES
COC1=C(C=C(Cl)C=C1)C(=O)NCCC1=CC=C(C=C1)S(=O)(=O)NC(=O)NC1CCCCC1
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
  • 3-halobenzoic acid or derivatives
  • Salicylamide
  • Benzenesulfonamide
  • Phenethylamine
  • Benzoic acid or derivatives
  • Benzamide
  • Methoxybenzene
  • Phenol ether
  • Benzoyl
  • Anisole
  • Sulfonylurea
  • Halobenzene
  • Cyclohexylamine
  • Chlorobenzene
  • Alkyl aryl ether
  • Aryl halide
  • Aryl chloride
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationIndicated as an adjunct to diet to lower the blood glucose in patients with NIDDM whose hyperglycemia cannot be satisfactorily controlled by diet alone.
PharmacodynamicsGlyburide, a second-generation sulfonylurea antidiabetic agent, lowers blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. With chronic administration in Type II diabetic patients, the blood glucose lowering effect persists despite a gradual decline in the insulin secretory response to the drug. Extrapancreatic effects may be involved in the mechanism of action of oral sulfonyl-urea hypoglycemic drugs. The combination of glibenclamide and metformin may have a synergistic effect, since both agents act to improve glucose tolerance by different but complementary mechanisms. In addition to its blood glucose lowering actions, glyburide produces a mild diuresis by enhancement of renal free water clearance. Glyburide is twice as potent as the related second-generation agent glipizide.
Mechanism of actionSulfonylureas such as glyburide bind to ATP-sensitive potassium channels on the pancreatic cell surface, reducing potassium conductance and causing depolarization of the membrane. Depolarization stimulates calcium ion influx through voltage-sensitive calcium channels, raising intracellular concentrations of calcium ions, which induces the secretion, or exocytosis, of insulin.
Related Articles
AbsorptionSignificant absorption within 1 hour and peak plasma levels are reached in 2 to 4 hours. Onset of action occurs within one hour.
Volume of distribution

Steady state Vd=0.125 L/kg; Vd during elimination phase=0.155 L/kg.

Protein bindingUnchanged drug is ~99% bound to serum proteins; 4-trans-hydroxyglyburide is greater than 97% bound to serum proteins. Protein binding is primarily nonionic making glyburide and is less likely to displace or be displaced by drugs that bind via an ionic mechanism.
Metabolism

Primarily hepatic (mainly cytochrome P450 3A4). The major metabolite is the 4-trans-hydroxy derivative. A second metabolite, the 3-cis-hydroxy derivative, also occurs. These metabolites do not contribute clinically significant hypoglycemic action in humans as they are only weakly active; however, retention of 4-trans-hydroxyglyburide may prolong the hypoglycemic effect of the agent in those with severe renal impairment.

SubstrateEnzymesProduct
Glyburide
2-trans-Hydroxycyclohexyl glyburideDetails
Glyburide
4-cis-Hydroxycyclohexyl glyburideDetails
Glyburide
4-trans-Hydroxycyclohexyl glyburideDetails
Glyburide
3-trans-Hydroxycyclohexyl glyburideDetails
Glyburide
3-cis-Hydroxycyclohexyl glyburideDetails
Route of eliminationGlyburide is excreted as metabolites in the bile and urine, approximately 50% by each route. This dual excretory pathway is qualitatively different from that of other sulfonylureas, which are excreted primarily in the urine.
Half life1.4-1.8 hours (unchanged drug only); 10 hours (metabolites included). Duration of effect is 12-24 hours.
Clearance

78 ml/hr/kg in healthy adults. Clearance may be substantially decreased in those with severe renal impairment.

ToxicityOral rat LD50: > 20,000 mg/kg. Oral mouse LD50: 3250 mg/kg.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Glibenclamide Action PathwayDrug actionSMP00460
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9701
Blood Brain Barrier-0.6707
Caco-2 permeable-0.6479
P-glycoprotein substrateNon-substrate0.5109
P-glycoprotein inhibitor INon-inhibitor0.7119
P-glycoprotein inhibitor IINon-inhibitor0.8185
Renal organic cation transporterNon-inhibitor0.7982
CYP450 2C9 substrateSubstrate0.6488
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5329
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorInhibitor0.8948
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8627
Ames testNon AMES toxic0.6996
CarcinogenicityNon-carcinogens0.7539
BiodegradationNot ready biodegradable0.8245
Rat acute toxicity1.4243 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7551
hERG inhibition (predictor II)Non-inhibitor0.8024
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Sanofi aventis us llc
  • Actavis totowa llc
  • Aurobindo pharma ltd
  • Corepharma llc
  • Teva pharmaceuticals usa inc
  • Dava pharmaceuticals inc
  • Hikma pharmaceuticals
  • Mylan pharmaceuticals inc
  • Sandoz inc
  • Pharmacia and upjohn co
Packagers
Dosage forms
FormRouteStrength
Tabletoral1.25 mg/1
Tabletoral2.5 mg/1
Tabletoral5 mg/1
Tabletoral5 mg
Tablet, film coatedoral
Tabletoral
Tabletoral1.5 mg/1
Tabletoral3 mg/1
Tabletoral6 mg/1
Tabletoral2.5 mg
Prices
Unit descriptionCostUnit
Glynase 6 mg tablet2.28USD tablet
Glynase 6 mg prestab2.19USD tablet
Glynase 3 mg tablet1.45USD tablet
Glynase 3 mg prestab1.39USD tablet
Diabeta 5 mg tablet1.36USD tablet
Micronase 5 mg tablet1.36USD tablet
Diabeta 2.5 mg tablet0.91USD tablet
Glynase 1.5 mg tablet0.83USD tablet
Glynase 1.5 mg prestab0.82USD tablet
Micronase 2.5 mg tablet0.8USD tablet
Diabeta 1.25 mg tablet0.5USD tablet
Micronase 1.25 mg tablet0.48USD tablet
Diabeta 5 mg Tablet0.26USD tablet
Diabeta 2.5 mg Tablet0.14USD tablet
Apo-Glyburide 5 mg Tablet0.07USD tablet
Euglucon 5 mg Tablet0.07USD tablet
Mylan-Glybe 5 mg Tablet0.07USD tablet
Novo-Glyburide 5 mg Tablet0.07USD tablet
Nu-Glyburide 5 mg Tablet0.07USD tablet
Pms-Glyburide 5 mg Tablet0.07USD tablet
Ratio-Glyburide 5 mg Tablet0.07USD tablet
Sandoz Glyburide 5 mg Tablet0.07USD tablet
Apo-Glyburide 2.5 mg Tablet0.04USD tablet
Euglucon 2.5 mg Tablet0.04USD tablet
Mylan-Glybe 2.5 mg Tablet0.04USD tablet
Novo-Glyburide 2.5 mg Tablet0.04USD tablet
Nu-Glyburide 2.5 mg Tablet0.04USD tablet
Pms-Glyburide 2.5 mg Tablet0.04USD tablet
Ratio-Glyburide 2.5 mg Tablet0.04USD tablet
Sandoz Glyburide 2.5 mg Tablet0.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6303146 Yes2000-01-142020-01-14Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point169 °CPhysProp
water solubility4 mg/L (at 27 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.7Not Available
logS-5.09ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.00206 mg/mLALOGPS
logP3.78ALOGPS
logP3.79ChemAxon
logS-5.4ALOGPS
pKa (Strongest Acidic)4.32ChemAxon
pKa (Strongest Basic)-1.2ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area113.6 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity126.98 m3·mol-1ChemAxon
Polarizability51.75 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Suresh Gidwani, “Solid oral dosage form of metformin and glyburide and the method of preparation thereof.” U.S. Patent US20040175421, issued September 09, 2004.

US20040175421
General References
  1. Monami M, Luzzi C, Lamanna C, Chiasserini V, Addante F, Desideri CM, Masotti G, Marchionni N, Mannucci E: Three-year mortality in diabetic patients treated with different combinations of insulin secretagogues and metformin. Diabetes Metab Res Rev. 2006 Nov-Dec;22(6):477-82. [PubMed:16634115 ]
External Links
ATC CodesA10BB01
AHFS Codes
  • 68:20.20
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (36.9 KB)
Interactions
Drug Interactions
Drug
AcetohexamideAcetohexamide may increase the hypoglycemic activities of Glyburide.
Acetylsalicylic acidAcetylsalicylic acid may increase the hypoglycemic activities of Glyburide.
AlogliptinAlogliptin may increase the hypoglycemic activities of Glyburide.
AmitriptylineAmitriptyline may increase the hypoglycemic activities of Glyburide.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Glyburide.
AripiprazoleThe therapeutic efficacy of Glyburide can be decreased when used in combination with Aripiprazole.
Arsenic trioxideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Arsenic trioxide.
ArticaineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Articaine.
AsenapineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Asenapine.
AtazanavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Atazanavir.
BendroflumethiazideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Bendroflumethiazide.
BetamethasoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Betamethasone.
BosentanGlyburide may increase the hepatotoxic activities of Bosentan.
BrexpiprazoleThe therapeutic efficacy of Glyburide can be decreased when used in combination with Brexpiprazole.
BumetanideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Bumetanide.
BuserelinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Buserelin.
CanagliflozinCanagliflozin may increase the hypoglycemic activities of Glyburide.
CarbocisteineThe risk or severity of adverse effects can be increased when Glyburide is combined with Carbocisteine.
CeritinibThe serum concentration of Glyburide can be increased when it is combined with Ceritinib.
ChloramphenicolThe metabolism of Glyburide can be decreased when combined with Chloramphenicol.
ChlorothiazideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Chlorothiazide.
ChlorpropamideGlyburide may increase the hypoglycemic activities of Chlorpropamide.
ChlorthalidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Chlorthalidone.
Cholic AcidGlyburide may decrease the excretion rate of Cholic Acid which could result in a lower serum level and potentially a reduction in efficacy.
CimetidineThe serum concentration of Glyburide can be increased when it is combined with Cimetidine.
ClarithromycinThe serum concentration of Glyburide can be increased when it is combined with Clarithromycin.
ClozapineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Clozapine.
ColesevelamThe serum concentration of Glyburide can be decreased when it is combined with Colesevelam.
CorticotropinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Corticotropin.
Cortisone acetateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Cortisone acetate.
CyclosporineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Cyclosporine.
Cyproterone acetateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Cyproterone acetate.
DabrafenibThe therapeutic efficacy of Glyburide can be decreased when used in combination with Dabrafenib.
DanazolThe therapeutic efficacy of Glyburide can be decreased when used in combination with Danazol.
DarunavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Darunavir.
DesogestrelThe therapeutic efficacy of Glyburide can be decreased when used in combination with Desogestrel.
DexamethasoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Dexamethasone.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Glyburide.
DiazoxideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Diazoxide.
DicoumarolGlyburide may increase the anticoagulant activities of Dicoumarol.
DienogestThe therapeutic efficacy of Glyburide can be decreased when used in combination with Dienogest.
DihydrotestosteroneDihydrotestosterone may increase the hypoglycemic activities of Glyburide.
DisopyramideGlyburide may increase the hypoglycemic activities of Disopyramide.
DrospirenoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Drospirenone.
EpinephrineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Epinephrine.
ErythromycinGlyburide may increase the hypoglycemic activities of Erythromycin.
EstradiolThe therapeutic efficacy of Glyburide can be decreased when used in combination with Estradiol.
Estrone sulfateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Estropipate.
Etacrynic acidThe therapeutic efficacy of Glyburide can be decreased when used in combination with Ethacrynic acid.
EthanolThe risk or severity of adverse effects can be increased when Glyburide is combined with Ethanol.
Ethinyl EstradiolThe therapeutic efficacy of Glyburide can be decreased when used in combination with Ethinyl Estradiol.
Ethynodiol diacetateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Ethynodiol.
EtonogestrelThe therapeutic efficacy of Glyburide can be decreased when used in combination with Etonogestrel.
EverolimusThe therapeutic efficacy of Glyburide can be decreased when used in combination with Everolimus.
ExenatideExenatide may increase the hypoglycemic activities of Glyburide.
FenofibrateFenofibrate may increase the hypoglycemic activities of Glyburide.
FloxuridineThe metabolism of Glyburide can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Glyburide can be decreased when combined with Fluconazole.
FludrocortisoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Fludrocortisone.
FosamprenavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Fosamprenavir.
FurosemideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Furosemide.
GliclazideGliclazide may increase the hypoglycemic activities of Glyburide.
GlimepirideGlyburide may increase the hypoglycemic activities of Glimepiride.
GlipizideGlyburide may increase the hypoglycemic activities of Glipizide.
GliquidoneGliquidone may increase the hypoglycemic activities of Glyburide.
GoserelinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Goserelin.
HistrelinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Histrelin.
HydrochlorothiazideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Hydrochlorothiazide.
HydrocortisoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Hydrocortisone.
Hydroxyprogesterone caproateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Hydroxyprogesterone caproate.
IloperidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Iloperidone.
IndapamideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Indapamide.
IndinavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Indinavir.
Insulin AspartInsulin Aspart may increase the hypoglycemic activities of Glyburide.
Insulin DegludecGlyburide may increase the hypoglycemic activities of Insulin degludec.
Insulin DetemirInsulin Detemir may increase the hypoglycemic activities of Glyburide.
Insulin GlargineGlyburide may increase the hypoglycemic activities of Insulin Glargine.
Insulin GlulisineInsulin Glulisine may increase the hypoglycemic activities of Glyburide.
Insulin HumanGlyburide may increase the hypoglycemic activities of Insulin Regular.
Insulin LisproGlyburide may increase the hypoglycemic activities of Insulin Lispro.
LanreotideGlyburide may increase the hypoglycemic activities of Lanreotide.
LeuprolideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Leuprolide.
LevonorgestrelThe therapeutic efficacy of Glyburide can be decreased when used in combination with Levonorgestrel.
LinagliptinLinagliptin may increase the hypoglycemic activities of Glyburide.
Lipoic AcidLipoic Acid may increase the hypoglycemic activities of Glyburide.
LopinavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Lopinavir.
LumacaftorThe serum concentration of Glyburide can be decreased when it is combined with Lumacaftor.
LurasidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Lurasidone.
MecamylamineThe risk or severity of adverse effects can be increased when Glyburide is combined with Mecamylamine.
MecaserminGlyburide may increase the hypoglycemic activities of Mecasermin.
Medroxyprogesterone acetateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Medroxyprogesterone Acetate.
Megestrol acetateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Megestrol acetate.
MestranolThe therapeutic efficacy of Glyburide can be decreased when used in combination with Mestranol.
MetforminMetformin may increase the hypoglycemic activities of Glyburide.
MethotrimeprazineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Methotrimeprazine.
MethyclothiazideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Methyclothiazide.
MethylprednisoloneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Methylprednisolone.
MetolazoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Metolazone.
MetreleptinMetreleptin may increase the hypoglycemic activities of Glyburide.
MiconazoleMiconazole may increase the hypoglycemic activities of Glyburide.
MifepristoneThe serum concentration of Glyburide can be increased when it is combined with Mifepristone.
NadololNadolol may increase the hypoglycemic activities of Glyburide.
NateglinideGlyburide may increase the hypoglycemic activities of Nateglinide.
NelfinavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Nelfinavir.
NiacinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Niacin.
NilotinibThe therapeutic efficacy of Glyburide can be decreased when used in combination with Nilotinib.
NorethisteroneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Norethindrone.
NorgestimateThe therapeutic efficacy of Glyburide can be decreased when used in combination with Norgestimate.
OctreotideGlyburide may increase the hypoglycemic activities of Octreotide.
OlanzapineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Olanzapine.
OxandroloneOxandrolone may increase the hypoglycemic activities of Glyburide.
PaliperidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Paliperidone.
ParoxetineParoxetine may increase the hypoglycemic activities of Glyburide.
PasireotideGlyburide may increase the hypoglycemic activities of Pasireotide.
PegvisomantPegvisomant may increase the hypoglycemic activities of Glyburide.
PentamidineGlyburide may increase the hypoglycemic activities of Pentamidine.
PhenelzinePhenelzine may increase the hypoglycemic activities of Glyburide.
PhenytoinThe metabolism of Glyburide can be increased when combined with Phenytoin.
PipotiazineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Pipotiazine.
PorfimerGlyburide may increase the photosensitizing activities of Porfimer.
PrednisoloneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Prednisolone.
PrednisoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Prednisone.
ProbenecidThe protein binding of Glyburide can be decreased when combined with Probenecid.
ProgesteroneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Progesterone.
QuetiapineThe therapeutic efficacy of Glyburide can be decreased when used in combination with Quetiapine.
QuinineGlyburide may increase the hypoglycemic activities of Quinine.
RanitidineThe serum concentration of Glyburide can be increased when it is combined with Ranitidine.
RepaglinideGlyburide may increase the hypoglycemic activities of Repaglinide.
Repository corticotropinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Repository corticotropin.
RifampicinThe serum concentration of Glyburide can be decreased when it is combined with Rifampicin.
RisperidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Risperidone.
RitonavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Ritonavir.
SaquinavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Saquinavir.
SaxagliptinSaxagliptin may increase the hypoglycemic activities of Glyburide.
SecobarbitalThe metabolism of Glyburide can be increased when combined with Secobarbital.
SirolimusThe therapeutic efficacy of Glyburide can be decreased when used in combination with Sirolimus.
SitagliptinSitagliptin may increase the hypoglycemic activities of Glyburide.
SparfloxacinSparfloxacin may increase the hypoglycemic activities of Glyburide.
SulfadiazineGlyburide may increase the hypoglycemic activities of Sulfadiazine.
SulfamethoxazoleGlyburide may increase the hypoglycemic activities of Sulfamethoxazole.
SulfisoxazoleGlyburide may increase the hypoglycemic activities of Sulfisoxazole.
SunitinibGlyburide may increase the hypoglycemic activities of Sunitinib.
TacrolimusThe therapeutic efficacy of Glyburide can be decreased when used in combination with Tacrolimus.
TemsirolimusThe therapeutic efficacy of Glyburide can be decreased when used in combination with Temsirolimus.
TestosteroneTestosterone may increase the hypoglycemic activities of Glyburide.
TipranavirThe therapeutic efficacy of Glyburide can be decreased when used in combination with Tipranavir.
TolazamideGlyburide may increase the hypoglycemic activities of Tolazamide.
TolbutamideTolbutamide may increase the hypoglycemic activities of Glyburide.
TorasemideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Torasemide.
TranylcypromineTranylcypromine may increase the hypoglycemic activities of Glyburide.
TriamcinoloneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Triamcinolone.
TrichlormethiazideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Trichlormethiazide.
TrimethoprimGlyburide may increase the hypoglycemic activities of Trimethoprim.
TriptorelinThe therapeutic efficacy of Glyburide can be decreased when used in combination with Triptorelin.
TroglitazoneTroglitazone may increase the hypoglycemic activities of Glyburide.
VerteporfinGlyburide may increase the photosensitizing activities of Verteporfin.
VildagliptinVildagliptin may increase the hypoglycemic activities of Glyburide.
VoriconazoleThe serum concentration of Glyburide can be increased when it is combined with Voriconazole.
VorinostatThe therapeutic efficacy of Glyburide can be decreased when used in combination with Vorinostat.
ZiprasidoneThe therapeutic efficacy of Glyburide can be decreased when used in combination with Ziprasidone.
Food Interactions
  • Avoid alcohol.
  • Take 30-60 minutes before breakfast.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
modulator
General Function:
Sulfonylurea receptor activity
Specific Function:
Subunit of the beta-cell ATP-sensitive potassium channel (KATP). Regulator of ATP-sensitive K(+) channels and insulin release.
Gene Name:
ABCC8
Uniprot ID:
Q09428
Molecular Weight:
176990.36 Da
References
  1. Dabrowski M, Ashcroft FM, Ashfield R, Lebrun P, Pirotte B, Egebjerg J, Bondo Hansen J, Wahl P: The novel diazoxide analog 3-isopropylamino-7-methoxy-4H-1,2,4-benzothiadiazine 1,1-dioxide is a selective Kir6.2/SUR1 channel opener. Diabetes. 2002 Jun;51(6):1896-906. [PubMed:12031979 ]
  2. Hambrock A, Preisig-Muller R, Russ U, Piehl A, Hanley PJ, Ray J, Daut J, Quast U, Derst C: Four novel splice variants of sulfonylurea receptor 1. Am J Physiol Cell Physiol. 2002 Aug;283(2):C587-98. [PubMed:12107069 ]
  3. Hambrock A, Loffler-Walz C, Quast U: Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. Br J Pharmacol. 2002 Aug;136(7):995-1004. [PubMed:12145099 ]
  4. Nielsen FE, Bodvarsdottir TB, Worsaae A, MacKay P, Stidsen CE, Boonen HC, Pridal L, Arkhammar PO, Wahl P, Ynddal L, Junager F, Dragsted N, Tagmose TM, Mogensen JP, Koch A, Treppendahl SP, Hansen JB: 6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells. J Med Chem. 2002 Sep 12;45(19):4171-87. [PubMed:12213059 ]
  5. Babenko AP, Bryan J: SUR-dependent modulation of KATP channels by an N-terminal KIR6.2 peptide. Defining intersubunit gating interactions. J Biol Chem. 2002 Nov 15;277(46):43997-4004. Epub 2002 Sep 3. [PubMed:12213829 ]
  6. Ueda K, Komine J, Matsuo M, Seino S, Amachi T: Cooperative binding of ATP and MgADP in the sulfonylurea receptor is modulated by glibenclamide. Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1268-72. [PubMed:9990013 ]
  7. Serrano-Martin X, Payares G, Mendoza-Leon A: Glibenclamide, a blocker of K+(ATP) channels, shows antileishmanial activity in experimental murine cutaneous leishmaniasis. Antimicrob Agents Chemother. 2006 Dec;50(12):4214-6. Epub 2006 Oct 2. [PubMed:17015627 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Phosphatidylinositol-4,5-bisphosphate binding
Specific Function:
In the kidney, probably plays a major role in potassium homeostasis. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive vol...
Gene Name:
KCNJ1
Uniprot ID:
P48048
Molecular Weight:
44794.6 Da
References
  1. Pondugula SR, Raveendran NN, Ergonul Z, Deng Y, Chen J, Sanneman JD, Palmer LG, Marcus DC: Glucocorticoid regulation of genes in the amiloride-sensitive sodium transport pathway by semicircular canal duct epithelium of neonatal rat. Physiol Genomics. 2006 Jan 12;24(2):114-23. Epub 2005 Nov 1. [PubMed:16263802 ]
  2. Lu M, Leng Q, Egan ME, Caplan MJ, Boulpaep EL, Giebisch GH, Hebert SC: CFTR is required for PKA-regulated ATP sensitivity of Kir1.1 potassium channels in mouse kidney. J Clin Invest. 2006 Mar;116(3):797-807. Epub 2006 Feb 9. [PubMed:16470247 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
G-protein activated inward rectifier potassium channel activity
Specific Function:
This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward...
Gene Name:
KCNJ5
Uniprot ID:
P48544
Molecular Weight:
47667.3 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
modulator
General Function:
Transporter activity
Specific Function:
Subunit of ATP-sensitive potassium channels (KATP). Can form cardiac and smooth muscle-type KATP channels with KCNJ11. KCNJ11 forms the channel pore while ABCC9 is required for activation and regulation.
Gene Name:
ABCC9
Uniprot ID:
O60706
Molecular Weight:
174221.7 Da
References
  1. Hambrock A, Loffler-Walz C, Quast U: Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. Br J Pharmacol. 2002 Aug;136(7):995-1004. [PubMed:12145099 ]
  2. Rainbow RD, James M, Hudman D, Al Johi M, Singh H, Watson PJ, Ashmole I, Davies NW, Lodwick D, Norman RI: Proximal C-terminal domain of sulphonylurea receptor 2A interacts with pore-forming Kir6 subunits in KATP channels. Biochem J. 2004 Apr 1;379(Pt 1):173-81. [PubMed:14672537 ]
  3. Felsch H, Lange U, Hambrock A, Loffler-Walz C, Russ U, Carroll WA, Gopalakrishnan M, Quast U: Interaction of a novel dihydropyridine K+ channel opener, A-312110, with recombinant sulphonylurea receptors and KATP channels: comparison with the cyanoguanidine P1075. Br J Pharmacol. 2004 Apr;141(7):1098-105. Epub 2004 Mar 15. [PubMed:15023854 ]
  4. Zhao JL, Yang YJ, You SJ, Jing ZC, Wu YJ, Cheng JL, Gao RL: Pretreatment with fosinopril or valsartan reduces myocardial no-reflow after acute myocardial infarction and reperfusion. Coron Artery Dis. 2006 Aug;17(5):463-9. [PubMed:16845255 ]
  5. Wang YH, Zheng HY, Qin NL, Yu SB, Liu SY: Involvement of ATP-sensitive potassium channels in proliferation and differentiation of rat preadipocytes. Sheng Li Xue Bao. 2007 Feb 25;59(1):8-12. [PubMed:17294036 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Byrne JA, Strautnieks SS, Mieli-Vergani G, Higgins CF, Linton KJ, Thompson RJ: The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology. 2002 Nov;123(5):1649-58. [PubMed:12404239 ]
  2. Kemp DC, Brouwer KL: Viability assessment in sandwich-cultured rat hepatocytes after xenobiotic exposure. Toxicol In Vitro. 2004 Dec;18(6):869-77. [PubMed:15465654 ]
  3. Horikawa M, Kato Y, Tyson CA, Sugiyama Y: Potential cholestatic activity of various therapeutic agents assessed by bile canalicular membrane vesicles isolated from rats and humans. Drug Metab Pharmacokinet. 2003;18(1):16-22. [PubMed:15618715 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Syntaxin binding
Specific Function:
cAMP-dependent and sulfonylurea-sensitive anion transporter. Key gatekeeper influencing intracellular cholesterol transport.
Gene Name:
ABCA1
Uniprot ID:
O95477
Molecular Weight:
254299.89 Da
References
  1. Reddy ST, Hama S, Ng C, Grijalva V, Navab M, Fogelman AM: ATP-binding cassette transporter 1 participates in LDL oxidation by artery wall cells. Arterioscler Thromb Vasc Biol. 2002 Nov 1;22(11):1877-83. [PubMed:12426219 ]
  2. Muhl H, Hofler S, Pfeilschifter J: Inhibition of lipopolysaccharide/ATP-induced release of interleukin-18 by KN-62 and glyburide. Eur J Pharmacol. 2003 Dec 15;482(1-3):325-8. [PubMed:14660039 ]
  3. Agassandian M, Mathur SN, Zhou J, Field FJ, Mallampalli RK: Oxysterols trigger ABCA1-mediated basolateral surfactant efflux. Am J Respir Cell Mol Biol. 2004 Aug;31(2):227-33. Epub 2004 Mar 23. [PubMed:15039140 ]
  4. Nieland TJ, Chroni A, Fitzgerald ML, Maliga Z, Zannis VI, Kirchhausen T, Krieger M: Cross-inhibition of SR-BI- and ABCA1-mediated cholesterol transport by the small molecules BLT-4 and glyburide. J Lipid Res. 2004 Jul;45(7):1256-65. Epub 2004 Apr 21. [PubMed:15102890 ]
  5. Alder-Baerens N, Muller P, Pohl A, Korte T, Hamon Y, Chimini G, Pomorski T, Herrmann A: Headgroup-specific exposure of phospholipids in ABCA1-expressing cells. J Biol Chem. 2005 Jul 15;280(28):26321-9. Epub 2005 May 19. [PubMed:15905177 ]
  6. Lamkanfi M, Mueller JL, Vitari AC, Misaghi S, Fedorova A, Deshayes K, Lee WP, Hoffman HM, Dixit VM: Glyburide inhibits the Cryopyrin/Nalp3 inflammasome. J Cell Biol. 2009 Oct 5;187(1):61-70. doi: 10.1083/jcb.200903124. [PubMed:19805629 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Pdz domain binding
Specific Function:
Involved in the transport of chloride ions. May regulate bicarbonate secretion and salvage in epithelial cells by regulating the SLC4A7 transporter. Can inhibit the chloride channel activity of ANO1. Plays a role in the chloride and bicarbonate homeostasis during sperm epididymal maturation and capacitation.
Gene Name:
CFTR
Uniprot ID:
P13569
Molecular Weight:
168139.895 Da
References
  1. Reddy MM, Quinton PM: Effect of anion transport blockers on CFTR in the human sweat duct. J Membr Biol. 2002 Sep 1;189(1):15-25. [PubMed:12202948 ]
  2. Jiang J, Song Y, Bai C, Koller BH, Matthay MA, Verkman AS: Pleural surface fluorescence measurement of Na+ and Cl- transport across the air space-capillary barrier. J Appl Physiol (1985). 2003 Jan;94(1):343-52. Epub 2002 Aug 30. [PubMed:12391048 ]
  3. Zhou Z, Hu S, Hwang TC: Probing an open CFTR pore with organic anion blockers. J Gen Physiol. 2002 Nov;120(5):647-62. [PubMed:12407077 ]
  4. Larsen EH, Amstrup J, Willumsen NJ: Beta-adrenergic receptors couple to CFTR chloride channels of intercalated mitochondria-rich cells in the heterocellular toad skin epithelium. Biochim Biophys Acta. 2003 Dec 30;1618(2):140-52. [PubMed:14729151 ]
  5. Lee SY, Lee CO: Inhibition of Na+-K+ pump and L-type Ca2+ channel by glibenclamide in Guinea pig ventricular myocytes. J Pharmacol Exp Ther. 2005 Jan;312(1):61-8. Epub 2004 Sep 13. [PubMed:15365090 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
modulator
General Function:
Voltage-gated potassium channel activity
Specific Function:
This receptor is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectific...
Gene Name:
KCNJ11
Uniprot ID:
Q14654
Molecular Weight:
43540.375 Da
References
  1. Hambrock A, Loffler-Walz C, Quast U: Glibenclamide binding to sulphonylurea receptor subtypes: dependence on adenine nucleotides. Br J Pharmacol. 2002 Aug;136(7):995-1004. [PubMed:12145099 ]
  2. Nielsen FE, Bodvarsdottir TB, Worsaae A, MacKay P, Stidsen CE, Boonen HC, Pridal L, Arkhammar PO, Wahl P, Ynddal L, Junager F, Dragsted N, Tagmose TM, Mogensen JP, Koch A, Treppendahl SP, Hansen JB: 6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells. J Med Chem. 2002 Sep 12;45(19):4171-87. [PubMed:12213059 ]
  3. Gojkovic-Bukarica L, Hambrock A, Loffler-Walz C, Quast U, Russ U: Mg2+ sensitizes KATP channels to inhibition by DIDS: dependence on the sulphonylurea receptor subunit. Br J Pharmacol. 2002 Oct;137(4):429-40. [PubMed:12359624 ]
  4. Ball AJ, McCluskey JT, Flatt PR, McClenaghan NH: Chronic exposure to tolbutamide and glibenclamide impairs insulin secretion but not transcription of K(ATP) channel components. Pharmacol Res. 2004 Jul;50(1):41-6. [PubMed:15082027 ]
  5. Lim JG, Lee HY, Yun JE, Kim SP, Park JW, Suh SI, Jang BC, Cho CH, Bae JH, Kim SS, Han J, Park MJ, Song DK: Taurine block of cloned ATP-sensitive K+ channels with different sulfonylurea receptor subunits expressed in Xenopus laevis oocytes. Biochem Pharmacol. 2004 Sep 1;68(5):901-10. [PubMed:15294453 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated potassium channel activity
Specific Function:
This receptor is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. Can be blocked by extracellular barium (By similarity). Subunit of ATP-sensitive potassium channels (KATP). Can form cardiac and smooth muscle-type KATP channels with ABCC9. KCNJ11 forms the channel pore while ABCC9 is required for activation and regulation.
Components:
NameUniProt IDDetails
ATP-sensitive inward rectifier potassium channel 11Q14654 Details
ATP-sensitive inward rectifier potassium channel 8Q15842 Details
References
  1. Jaburek M, Yarov-Yarovoy V, Paucek P, Garlid KD: State-dependent inhibition of the mitochondrial KATP channel by glyburide and 5-hydroxydecanoate. J Biol Chem. 1998 May 29;273(22):13578-82. [PubMed:9593694 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Carnitine o-palmitoyltransferase activity
Specific Function:
Catalyzes the transfer of the acyl group of long-chain fatty acid-CoA conjugates onto carnitine, an essential step for the mitochondrial uptake of long-chain fatty acids and their subsequent beta-oxidation in the mitochondrion. Plays an important role in triglyceride metabolism.
Gene Name:
CPT1A
Uniprot ID:
P50416
Molecular Weight:
88366.92 Da
References
  1. Patel TB: Effect of sulfonylureas on hepatic fatty acid oxidation. Am J Physiol. 1986 Aug;251(2 Pt 1):E241-6. [PubMed:3090894 ]
  2. Cook GA: The hypoglycemic sulfonylureas glyburide and tolbutamide inhibit fatty acid oxidation by inhibiting carnitine palmitoyltransferase. J Biol Chem. 1987 Apr 15;262(11):4968-72. [PubMed:3104327 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid 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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Crooks MJ, Brown KF: The binding of sulphonylureas to serum albumin. J Pharm Pharmacol. 1974 May;26(5):304-11. [PubMed:4153105 ]
  2. Hsu PL, Ma JK, Luzzi LA: Interactions of sulfonylureas with plasma proteins. J Pharm Sci. 1974 Apr;63(4):570-3. [PubMed:4208196 ]
  3. Brown KF, Crooks MJ: Displacement of tolbutamide, glibencalmide and chlorpropamide from serum albumin by anionic drugs. Biochem Pharmacol. 1976 May 15;25(10):1175-8. [PubMed:820348 ]

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. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. [PubMed:16460798 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Byrne JA, Strautnieks SS, Mieli-Vergani G, Higgins CF, Linton KJ, Thompson RJ: The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology. 2002 Nov;123(5):1649-58. [PubMed:12404239 ]
  2. Wang EJ, Casciano CN, Clement RP, Johnson WW: Fluorescent substrates of sister-P-glycoprotein (BSEP) evaluated as markers of active transport and inhibition: evidence for contingent unequal binding sites. Pharm Res. 2003 Apr;20(4):537-44. [PubMed:12739759 ]
  3. Noe J, Hagenbuch B, Meier PJ, St-Pierre MV: Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. Hepatology. 2001 May;33(5):1223-31. [PubMed:11343252 ]
  4. Funk C, Pantze M, Jehle L, Ponelle C, Scheuermann G, Lazendic M, Gasser R: Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt export pump (Bsep) by troglitazone and troglitazone sulfate. Toxicology. 2001 Oct 5;167(1):83-98. [PubMed:11557132 ]
  5. Stieger B, Fattinger K, Madon J, Kullak-Ublick GA, Meier PJ: Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver. Gastroenterology. 2000 Feb;118(2):422-30. [PubMed:10648470 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Golstein PE, Boom A, van Geffel J, Jacobs P, Masereel B, Beauwens R: P-glycoprotein inhibition by glibenclamide and related compounds. Pflugers Arch. 1999 Apr;437(5):652-60. [PubMed:10087141 ]
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. Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells. Br J Pharmacol. 2001 Feb;132(3):778-84. [PubMed:11159731 ]
  2. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. [PubMed:16460798 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Proton-dependent oligopeptide secondary active transmembrane transporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides. May constitute a major route for the absorption of protein digestion end-products.
Gene Name:
SLC15A1
Uniprot ID:
P46059
Molecular Weight:
78805.265 Da
References
  1. Sawada K, Terada T, Saito H, Hashimoto Y, Inui K: Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2. Br J Pharmacol. 1999 Nov;128(6):1159-64. [PubMed:10578127 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Shitara Y, Sugiyama D, Kusuhara H, Kato Y, Abe T, Meier PJ, Itoh T, Sugiyama Y: Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport. Pharm Res. 2002 Feb;19(2):147-53. [PubMed:11883641 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Peptide:proton symporter activity
Specific Function:
Proton-coupled intake of oligopeptides of 2 to 4 amino acids with a preference for dipeptides.
Gene Name:
SLC15A2
Uniprot ID:
Q16348
Molecular Weight:
81782.77 Da
References
  1. Sawada K, Terada T, Saito H, Hashimoto Y, Inui K: Effects of glibenclamide on glycylsarcosine transport by the rat peptide transporters PEPT1 and PEPT2. Br J Pharmacol. 1999 Nov;128(6):1159-64. [PubMed:10578127 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Uwai Y, Saito H, Hashimoto Y, Inui K: Inhibitory effect of anti-diabetic agents on rat organic anion transporter rOAT1. Eur J Pharmacol. 2000 Jun 16;398(2):193-7. [PubMed:10854830 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. [PubMed:16460798 ]
  2. Payen L, Delugin L, Courtois A, Trinquart Y, Guillouzo A, Fardel O: The sulphonylurea glibenclamide inhibits multidrug resistance protein (MRP1) activity in human lung cancer cells. Br J Pharmacol. 2001 Feb;132(3):778-84. [PubMed:11159731 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. Gedeon C, Behravan J, Koren G, Piquette-Miller M: Transport of glyburide by placental ABC transporters: implications in fetal drug exposure. Placenta. 2006 Nov-Dec;27(11-12):1096-102. Epub 2006 Feb 3. [PubMed:16460798 ]
  2. Pollex EK, Anger G, Hutson J, Koren G, Piquette-Miller M: Breast cancer resistance protein (BCRP)-mediated glyburide transport: effect of the C421A/Q141K BCRP single-nucleotide polymorphism. Drug Metab Dispos. 2010 May;38(5):740-4. doi: 10.1124/dmd.109.030791. Epub 2010 Feb 16. [PubMed:20159988 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulfate, allopurinol, 5-fluorouracil, paclitaxel, L-ascorbic acid, salicylate, ethotrexate, and alpha-ketoglutarate.
Gene Name:
SLC22A7
Uniprot ID:
Q9Y694
Molecular Weight:
60025.025 Da
References
  1. Morita N, Kusuhara H, Sekine T, Endou H, Sugiyama Y: Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. J Pharmacol Exp Ther. 2001 Sep;298(3):1179-84. [PubMed:11504818 ]
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. 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 ]
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Drug created on June 13, 2005 07:24 / Updated on July 01, 2016 03:05