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Identification
NameDiazepam
Accession NumberDB00829  (APRD00642, DB07699)
TypeSmall Molecule
GroupsApproved, Illicit, Vet Approved
Description

A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of gamma-aminobutyric acid activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589)

Structure
Thumb
Synonyms
7-chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one
Diazepam
Methyl diazepinone
Valium
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Bio-diazepamtablet5 mgoralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamtablet2 mgoralBiomed Pharma2003-04-23Not applicableCanada
Bio-diazepamtablet10 mgoralBiomed Pharma2003-04-23Not applicableCanada
Diastatgel10 mg/2mLrectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
Diastatgel2.5 mg/.5mLrectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
Diastatgel5 mgrectalValeant Pharmaceuticals North America LLC2000-01-28Not applicableCanada
Diastatgel20 mg/4mLrectalValeant Pharmaceuticals North America LLC1997-07-29Not applicableUs
Diazemulsemulsion5 mgintramuscular; intravenousActavis Group Ptc Ehf1995-12-312016-01-05Canada
Diazepamgel2.5 mg/.5mLrectalTeva Pharmaceuticals USA Inc2010-10-01Not applicableUs
Diazepamgel20 mg/4mLrectalTeva Pharmaceuticals USA Inc2010-09-03Not applicableUs
Diazepamgel10 mg/2mLrectalTeva Pharmaceuticals USA Inc2010-09-03Not applicableUs
Diazepam 10mg Tabletstablet10 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam 10tab 10mgtablet10 mgoralPro Doc Limitee1978-12-31Not applicableCanada
Diazepam 2mg Tabletstablet2 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam 2tab 2mgtablet2 mgoralPro Doc Limitee1978-12-312012-07-23Canada
Diazepam 5 Tabtablet5 mgoralPro Doc Limitee1974-12-31Not applicableCanada
Diazepam 5mg Tabletstablet5 mgoralLaboratoires Confab IncNot applicableNot applicableCanada
Diazepam Autoinjectorliquid5 mgintramuscularMeridian Medical Technologies Inc.2007-01-24Not applicableCanada
Diazepam Injection Sdzsolution5 mgintramuscular; intravenousSandoz Canada Incorporated2013-03-27Not applicableCanada
Diazepam Injection USPsolution5 mgintramuscular; intravenousAlveda Pharmaceuticals IncNot applicableNot applicableCanada
Diazepam Injection USPsolution5 mgintramuscular; intravenousSandoz Canada Incorporated1980-12-31Not applicableCanada
E Pam Tab 10mgtablet10 mgoralIcn Canada Ltd.1973-12-312005-04-26Canada
E Pam Tab 2mgtablet2 mgoralIcn Canada Ltd.1973-12-312005-04-26Canada
E Pam Tab 5mgtablet5 mgoralIcn Canada Ltd.1973-12-312005-04-26Canada
Meval 2tablet2 mgoralMedic Laboratory LtÉe1973-12-311996-09-09Canada
Meval 5tablet5 mgoralMedic Laboratory LtÉe1973-12-311996-09-09Canada
Novo-dipam Tab 10mgtablet10 mgoralNovopharm Limited1973-12-312015-10-26Canada
Novo-dipam Tab 2mgtablet2 mgoralNovopharm Limited1973-12-312015-10-26Canada
Novo-dipam Tab 5mgtablet5 mgoralNovopharm Limited1973-12-312015-10-26Canada
PMS-diazepamtablet10 mgoralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepamtablet5 mgoralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepamtablet2 mgoralPharmascience Inc2003-12-10Not applicableCanada
PMS-diazepam Solution 1mg/mlsolution1 mgoralPharmascience Inc1992-12-31Not applicableCanada
Valiumtablet10 mg/1oralGenentech, Inc.1963-11-15Not applicableUs
Valiumtablet5 mg/1oralPd Rx Pharmaceuticals, Inc.1963-11-15Not applicableUs
Valiumtablet5 mg/1oralGenentech, Inc.1963-11-15Not applicableUs
Valiumtablet10 mg/1oralCardinal Health1963-11-15Not applicableUs
Valiumtablet2 mg/1oralGenentech, Inc.1963-11-15Not applicableUs
Valiumtablet5 mg/1oralCardinal Health1963-11-15Not applicableUs
Valiumtablet5 mg/1oralREMEDYREPACK INC.2012-11-28Not applicableUs
Valium 10 Tabtablet10 mgoralHoffmann La Roche Limited1978-12-312001-07-19Canada
Valium 5 Tabtablet5 mgoralHoffmann La Roche Limited1978-12-31Not applicableCanada
Valium Inj Roche 5mg/mlliquid10 mgintramuscular; intravenousHoffmann La Roche Limited1968-12-312000-07-27Canada
Vivoltablet5 mgAxxess Pharma Inc.1970-12-312011-07-22Canada
Vivoltablet2 mgoralCarter Horner Corp.1970-12-312004-07-09Canada
Vivoltablet10 mgAxxess Pharma Inc.1970-12-312011-07-22Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Diazepam Tab 10mgtablet10 mgoralApotex Inc1979-12-31Not applicableCanada
Apo Diazepam Tab 2mgtablet2 mgoralApotex Inc1979-12-31Not applicableCanada
Apo Diazepam Tab 5mgtablet5 mgoralApotex Inc1977-12-31Not applicableCanada
Diazepamtablet5 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousCardinal Health1988-12-20Not applicableUs
Diazepamtablet10 mg/1oralbryant ranch prepack2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralPreferred Pharmaceuticals, Inc.2012-01-17Not applicableUs
Diazepamsolution, concentrate5 mg/mLoralLannett Company, Inc.2014-04-14Not applicableUs
Diazepamtablet5 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-29Not applicableUs
Diazepamtablet2 mg/1oralRebel Distributors Corp.2009-11-09Not applicableUs
Diazepamtablet10 mg/1oralRebel Distributors Corp.2009-11-09Not applicableUs
Diazepamtablet10 mg/1oralActavis Pharma, Inc.1987-02-03Not applicableUs
Diazepamtablet10 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousA S Medication Solutions Llc1987-10-13Not applicableUs
Diazepamtablet5 mg/1oralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
Diazepamtablet2 mg/1oralTYA Pharmaceuticals1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralMc Kesson Contract Packaging2011-10-13Not applicableUs
Diazepamtablet10 mg/1oralUnit Dose Services2006-03-31Not applicableUs
Diazepamsolution5 mg/5mLoralCardinal Health2012-02-22Not applicableUs
Diazepamtablet10 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diazepamtablet5 mg/1oralContract Pharmacy Services Pa2011-08-01Not applicableUs
Diazepamtablet2 mg/1oralAvera Mc Kennan Hospital2015-05-05Not applicableUs
Diazepamtablet5 mg/1oralKAISER FOUNDATION HOSPITALS2002-01-29Not applicableUs
Diazepamtablet10 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1987-02-03Not applicableUs
Diazepamtablet10 mg/1oralBlenheim Pharmacal, Inc.2010-04-13Not applicableUs
Diazepamtablet2 mg/1oralA S Medication Solutions Llc1986-12-10Not applicableUs
Diazepamtablet10 mg/1oralCardinal Health2009-11-09Not applicableUs
Diazepamtablet2 mg/1oralbryant ranch prepack1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralPreferred Pharmaceuticals, Inc.2011-11-09Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousHospira, Inc.1987-10-13Not applicableUs
Diazepamtablet2 mg/1oralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
Diazepamsolution5 mg/5mLoralAtlantic Biologicals Corps1987-04-03Not applicableUs
Diazepamtablet5 mg/1oralUnit Dose Services1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralCardinal Health2006-11-15Not applicableUs
Diazepamtablet5 mg/1oralDIRECT RX2014-01-01Not applicableUs
Diazepamtablet2 mg/1oralDispensing Solutions, Inc.1987-02-03Not applicableUs
Diazepamtablet10 mg/1oralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC1987-02-03Not applicableUs
Diazepamtablet5 mg/1oralMajor Pharmaceuticals2008-06-05Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousHospira, Inc.1988-12-20Not applicableUs
Diazepamtablet5 mg/1oralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralSTAT Rx USA LLC2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralCardinal Health2009-11-09Not applicableUs
Diazepamtablet10 mg/1oralbryant ranch prepack2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralPreferred Pharmaceuticals, Inc.2011-11-09Not applicableUs
Diazepamtablet5 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepamtablet2 mg/1oralPhysicians Total Care, Inc.2008-07-23Not applicableUs
Diazepamtablet2 mg/1oralREMEDYREPACK INC.2015-07-22Not applicableUs
Diazepamtablet5 mg/1oralDispensing Solutions, Inc.2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
Diazepamtablet2 mg/1oralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralQualitest Pharmaceuticals2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
Diazepamtablet5 mg/1oralSTAT Rx USA LLC2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralREMEDYREPACK INC.2013-07-03Not applicableUs
Diazepamtablet2 mg/1oralCardinal Health2009-11-20Not applicableUs
Diazepamtablet5 mg/1oralbryant ranch prepack1986-12-10Not applicableUs
Diazepamsolution5 mg/5mLoralPrecision Dose Inc.2012-02-22Not applicableUs
Diazepamtablet10 mg/1oralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
Diazepamtablet10 mg/1oralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralQualitest Pharmaceuticals2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralPhysicians Total Care, Inc.2004-06-03Not applicableUs
Diazepamtablet2 mg/1oralLake Erie Medical DBA Quality Care Products LLC1986-12-10Not applicableUs
Diazepamtablet10 mg/1oralDispensing Solutions, Inc.2006-03-31Not applicableUs
Diazepamtablet2 mg/1oralIVAX Pharmaceuticals, Inc.1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralSTAT Rx USA LLC2009-11-20Not applicableUs
Diazepamtablet2 mg/1oralSTAT Rx USA LLC2006-03-31Not applicableUs
Diazepamtablet10 mg/1oralMylan Institutional Inc.1997-10-31Not applicableUs
Diazepamtablet5 mg/1oralCardinal Health2009-11-20Not applicableUs
Diazepamtablet10 mg/1oralProficient Rx LP1986-12-10Not applicableUs
Diazepamtablet10 mg/1oralAphena Pharma Solutions Tennessee, Llc2006-03-31Not applicableUs
Diazepaminjection5 mg/mLintramuscular; intravenousGENERAL INJECTABLES AND VACCINES, INC.2010-06-01Not applicableUs
Diazepamtablet5 mg/1oralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
Diazepamtablet5 mg/1oralAidarex Pharmaceuticals LLC2006-03-31Not applicableUs
Diazepamtablet2 mg/1oralQualitest Pharmaceuticals2006-03-31Not applicableUs
Diazepamtablet2 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousPhysicians Total Care, Inc.2002-02-13Not applicableUs
Diazepamtablet2 mg/1oralPd Rx Pharmaceuticals, Inc.1987-02-03Not applicableUs
Diazepamtablet10 mg/1oralTYA Pharmaceuticals1987-02-03Not applicableUs
Diazepamtablet5 mg/1oralAmerican Health Packaging2009-10-132015-12-29Us
Diazepamsolution5 mg/5mLoralRoxane Laboratories, Inc1990-06-14Not applicableUs
Diazepamtablet10 mg/1oralSTAT Rx USA LLC2009-11-20Not applicableUs
Diazepamtablet10 mg/1oralApotheca, Inc.2009-01-15Not applicableUs
Diazepamtablet5 mg/1oralMylan Institutional Inc.1997-11-04Not applicableUs
Diazepamtablet10 mg/1oralCardinal Health2009-11-20Not applicableUs
Diazepamtablet5 mg/1oralProficient Rx LP1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralRed Pharm Drug Inc.2006-05-01Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousGENERAL INJECTABLES AND VACCINES, INC.2010-05-01Not applicableUs
Diazepamtablet2 mg/1oralMylan Pharmaceuticals Inc.1985-09-04Not applicableUs
Diazepamtablet10 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousCardinal Health1987-10-13Not applicableUs
Diazepamtablet5 mg/1oralMc Kesson Packaging Services Business Unit Of Mc Kesson Corporation2006-11-15Not applicableUs
Diazepamtablet5 mg/1oralPreferred Pharmaceuticals, Inc.2012-01-17Not applicableUs
Diazepamtablet5 mg/1oralActavis Pharma, Inc.1987-02-03Not applicableUs
Diazepamtablet10 mg/1oralA S Medication Solutions Llc2006-03-31Not applicableUs
Diazepamtablet5 mg/1oralRebel Distributors Corp.2009-11-09Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscular; intravenousRebel Distributors Corp1987-10-13Not applicableUs
Diazepamtablet2 mg/1oralActavis Pharma, Inc.1987-02-03Not applicableUs
Diazepamtablet2 mg/1oralA S Medication Solutions Llc1986-12-10Not applicableUs
Diazepamtablet5 mg/1oralPhysicians Total Care, Inc.2008-08-19Not applicableUs
Diazepamtablet10 mg/1oralPd Rx Pharmaceuticals, Inc.2009-11-20Not applicableUs
Diazepamtablet5 mg/1oralTYA Pharmaceuticals1986-12-10Not applicableUs
Diazepamtablet10 mg/1oralMc Kesson Contract Packaging2009-11-09Not applicableUs
Diazepamsolution5 mg/5mLoralRoxane Laboratories, Inc1987-04-03Not applicableUs
Diazepamtablet5 mg/1oralApotheca, Inc.2009-12-09Not applicableUs
Diazepamtablet2 mg/1oralMylan Institutional Inc.1997-10-31Not applicableUs
Diazepamtablet5 mg/1oralCardinal Health2009-10-13Not applicableUs
Diazepamtablet5 mg/1oralDIRECT RX2015-01-01Not applicableUs
Diazepamtablet10 mg/1oralContract Pharmacy Services Pa2011-03-29Not applicableUs
Diazepaminjection, solution5 mg/mLintramuscularREMEDYREPACK INC.2016-03-07Not applicableUs
Diazepamtablet10 mg/1oralKAISER FOUNDATION HOSPITALS2002-01-29Not applicableUs
Diazepamtablet10 mg/1oralLake Erie Medical DBA Quality Care Products LLC1986-12-10Not applicableUs
Diazepam Intensolsolution, concentrate5 mg/mLoralRoxane Laboratories, Inc1987-04-03Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
DiapamOrion
NerviumSaba
RelaniumGlaxoSmithKline
Brand mixtures
NameLabellerIngredients
Gabavale-5Physician Therapeutics Llc
SaltsNot Available
Categories
UNIIQ3JTX2Q7TU
CAS number439-14-5
WeightAverage: 284.74
Monoisotopic: 284.071640755
Chemical FormulaC16H13ClN2O
InChI KeyInChIKey=AAOVKJBEBIDNHE-UHFFFAOYSA-N
InChI
InChI=1S/C16H13ClN2O/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
IUPAC Name
7-chloro-1-methyl-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub Class1,4-benzodiazepines
Direct Parent1,4-benzodiazepines
Alternative Parents
Substituents
  • 1,4-benzodiazepine
  • Chlorobenzene
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Lactam
  • Ketimine
  • Carboxamide group
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome.
PharmacodynamicsDiazepam, a benzodiazepine, generates the same active metabolite as chlordiazepoxide and clorazepate. In animals, diazepam appears to act on parts of the limbic system, the thalamus and hypothalamus, and induces calming effects. Diazepam, unlike chlorpromazine and reserpine, has no demonstrable peripheral autonomic blocking action, nor does it produce extrapyramidal side effects; however, animals treated with diazepam do have a transient ataxia at higher doses. Diazepam was found to have transient cardiovascular depressor effects in dogs. Long-term experiments in rats revealed no disturbances of endocrine function. Injections into animals have produced localized irritation of tissue surrounding injection sites and some thickening of veins after intravenous use.
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors which mediate sleep, affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Related Articles
AbsorptionEssentially complete, with a bioavailability of 93%.
Volume of distribution
  • 0.8 to 1.0 L/kg [young healthy males]
Protein binding98.5%
Metabolism

Hepatic via the Cytochrome P450 enzyme system. The main active metabolite is desmethyldiazepam, in addition to minor active metabolites including temazepam and oxazepam.

SubstrateEnzymesProduct
Diazepam
NordiazepamDetails
Diazepam
TemazepamDetails
Diazepam
OxazepamDetails
Diazepam
Not Available
desmethyldiazepamDetails
Nordiazepam
OxazepamDetails
Temazepam
OxazepamDetails
Nordiazepam
Not Available
Nordiazepam O-glucuronideDetails
Route of eliminationDiazepam and its metabolites are excreted mainly in the urine, predominantly as their glucuronide conjugates.
Half lifeBiphasic 1-2 days and 2-5 days, active metabolites with long half lives.
Clearance
  • 20-30 mL/min
ToxicitySymptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
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+0.9948
Blood Brain Barrier+0.9934
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.661
P-glycoprotein inhibitor INon-inhibitor0.5557
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterInhibitor0.6152
CYP450 2C9 substrateNon-substrate0.6699
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.8177
CYP450 1A2 substrateInhibitor0.8175
CYP450 2C9 inhibitorNon-inhibitor0.5562
CYP450 2D6 inhibitorNon-inhibitor0.858
CYP450 2C19 inhibitorInhibitor0.5221
CYP450 3A4 inhibitorInhibitor0.6423
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5693
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8312
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5946 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9948
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Hoffmann la roche inc
  • Roxane laboratories inc
  • Valeant pharmaceuticals international
  • Abraxis pharmaceutical products
  • Baxter healthcare corp anesthesia and critical care
  • Hospira inc
  • Marsam pharmaceuticals llc
  • Parenta pharmaceuticals inc
  • Us army medical research materiel command
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Pharmacia and upjohn co
  • Actavis elizabeth llc
  • Barr laboratories inc
  • Dava pharmaceuticals inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Ferndale laboratories inc
  • Halsey drug co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Martec usa llc
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Vintage pharmaceuticals inc
  • Quantum pharmics ltd
Packagers
Dosage forms
FormRouteStrength
Tabletoral2 mg
Gelrectal5 mg
Emulsionintramuscular; intravenous5 mg
Gelrectal10 mg/2mL
Gelrectal2.5 mg/.5mL
Gelrectal20 mg/4mL
Injectionintramuscular; intravenous5 mg/mL
Injection, solutionintramuscular5 mg/mL
Injection, solutionintramuscular; intravenous5 mg/mL
Solutionoral5 mg/5mL
Tabletoral10 mg
Tabletoral5 mg
Liquidintramuscular5 mg
Solutionintramuscular; intravenous5 mg
Solution, concentrateoral5 mg/mL
Kit
Solutionoral1 mg
Tabletoral10 mg/1
Tabletoral2 mg/1
Tabletoral5 mg/1
Liquidintramuscular; intravenous10 mg
Tablet10 mg
Tablet5 mg
Prices
Unit descriptionCostUnit
Diastat acudial 12.5-15-20 mg429.58USD each
Diastat acudial 5-7.5-10 mg kit429.58USD kit
Diastat AcuDial 10 mg Gel 1 Box Contains Two 10 mg Syringes423.95USD box
Diastat AcuDial 20 mg Gel 1 Box Contains Two 20 mg Syringes413.6USD box
Diastat 2.5 mg pedi system362.12USD each
Valium 10 mg tablet6.06USD tablet
Diazepam powder3.99USD g
Valium 5 mg tablet2.55USD tablet
Valium 2 mg tablet2.43USD tablet
Diazemuls 5 mg/ml Emulsion1.23USD ml
Diazepam 5 mg/ml0.69USD ml
Diazepam 10 mg tablet0.38USD tablet
Diazepam 5 mg tablet0.3USD tablet
Diazepam 2 mg tablet0.26USD tablet
Diazepam 5 mg/ml vial0.17USD ml
Apo-Diazepam 10 mg Tablet0.09USD tablet
Apo-Diazepam 5 mg Tablet0.07USD tablet
Apo-Diazepam 2 mg Tablet0.05USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2171627 No2006-01-312014-09-12Canada
US5462740 No1993-09-172013-09-17Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point125-126Chase, G.; U.S. Patent 3,102,116; August 27, 1963; assigned to Hoffmann-La Roche Inc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,109,843; November 5, 1963; assigned to Hoffmann-La Roche lnc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,136,815; June 9, 1964; assigned to Hoffmann- La Roche Inc. Reeder, E. and Sternbach, L.H.; US. Patent 3,371,085; February 27, 1968; assigned to Hoffmann-La Roche Inc.
water solubility50 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.82SANGSTER (1994)
Caco2 permeability-4.32ADME Research, USCD
pKa3.4MERCK INDEX (1996)
Predicted Properties
PropertyValueSource
Water Solubility0.0122 mg/mLALOGPS
logP2.63ALOGPS
logP3.08ChemAxon
logS-4.4ALOGPS
pKa (Strongest Basic)2.92ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.67 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity79.81 m3·mol-1ChemAxon
Polarizability29.39 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.4 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0a59-2490000000-41352db33c43d0b96876View in MoNA
References
Synthesis Reference

Chase, G.; U.S. Patent 3,102,116; August 27, 1963; assigned to Hoffmann-La Roche Inc. Reeder, E. and Sternbach, L.H.; U.S. Patent 3,109,843; November 5, 1963; assigned to
Hoffmann-La Roche lnc.
Reeder, E. and Sternbach, L.H.; U.S. Patent 3,136,815; June 9, 1964; assigned to Hoffmann-
La Roche Inc.
Reeder, E. and Sternbach, L.H.; US. Patent 3,371,085; February 27, 1968; assigned to
Hoffmann-La Roche Inc.

General References
  1. Mant A, Whicker SD, McManus P, Birkett DJ, Edmonds D, Dumbrell D: Benzodiazepine utilisation in Australia: report from a new pharmacoepidemiological database. Aust J Public Health. 1993 Dec;17(4):345-9. [PubMed:7911332 ]
  2. Earley JV, Fryer RI, Ning RY: Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci. 1979 Jul;68(7):845-50. [PubMed:458601 ]
  3. Usami N, Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A: Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5. [PubMed:11995921 ]
  4. Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. [PubMed:3089825 ]
  5. McLean MJ, Macdonald RL: Benzodiazepines, but not beta carbolines, limit high frequency repetitive firing of action potentials of spinal cord neurons in cell culture. J Pharmacol Exp Ther. 1988 Feb;244(2):789-95. [PubMed:2450203 ]
External Links
ATC CodesN05BA01
AHFS Codes
  • 28:24.08
PDB EntriesNot Available
FDA labelDownload (260 KB)
MSDSDownload (53.1 KB)
Interactions
Drug Interactions
Drug
AlfentanilDiazepam may increase the central nervous system depressant (CNS depressant) activities of Alfentanil.
AprepitantThe serum concentration of Diazepam can be increased when it is combined with Aprepitant.
AzelastineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Diazepam.
BexaroteneThe serum concentration of Diazepam can be decreased when it is combined with Bexarotene.
BortezomibThe metabolism of Diazepam can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Diazepam can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
BuprenorphineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClozapineThe risk or severity of adverse effects can be increased when Diazepam is combined with Clozapine.
ConivaptanThe serum concentration of Diazepam can be increased when it is combined with Conivaptan.
CosyntropinCosyntropin may increase the hepatotoxic activities of Diazepam.
DabrafenibThe serum concentration of Diazepam can be decreased when it is combined with Dabrafenib.
DasatinibThe serum concentration of Diazepam can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Diazepam can be decreased when it is combined with Deferasirox.
DisulfiramThe serum concentration of Diazepam can be increased when it is combined with Disulfiram.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
EthanolDiazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EtravirineThe serum concentration of Diazepam can be decreased when it is combined with Etravirine.
FluconazoleThe metabolism of Diazepam can be decreased when combined with Fluconazole.
FluvoxamineThe metabolism of Diazepam can be decreased when combined with Fluvoxamine.
FosamprenavirThe serum concentration of Diazepam can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Diazepam can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Diazepam can be increased when it is combined with Fusidic Acid.
HydrocodoneDiazepam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
IdelalisibThe serum concentration of Diazepam can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Diazepam can be increased when it is combined with Ivacaftor.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Diazepam.
LuliconazoleThe serum concentration of Diazepam can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
MefloquineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Mefloquine.
MethadoneDiazepam may increase the central nervous system depressant (CNS depressant) activities of Methadone.
MethotrimeprazineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineDiazepam may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Diazepam can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
MirtazapineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Diazepam can be decreased when it is combined with Mitotane.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
NelfinavirThe metabolism of Diazepam can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Diazepam can be increased when it is combined with Netupitant.
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Diazepam.
OrlistatThe serum concentration of Diazepam can be decreased when it is combined with Orlistat.
OrphenadrineDiazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Diazepam can be increased when it is combined with Palbociclib.
ParaldehydeDiazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Diazepam is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
PhenytoinThe metabolism of Diazepam can be increased when combined with Phenytoin.
PramipexoleDiazepam may increase the sedative activities of Pramipexole.
RitonavirThe serum concentration of Diazepam can be increased when it is combined with Ritonavir.
RopiniroleDiazepam may increase the sedative activities of Ropinirole.
RotigotineDiazepam may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Diazepam.
SaquinavirThe serum concentration of Diazepam can be increased when it is combined with Saquinavir.
SiltuximabThe serum concentration of Diazepam can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Diazepam can be increased when it is combined with Simeprevir.
Sodium oxybateDiazepam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
St. John's WortThe serum concentration of Diazepam can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Diazepam can be increased when it is combined with Stiripentol.
SuvorexantDiazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Diazepam.
TeduglutideThe serum concentration of Diazepam can be increased when it is combined with Teduglutide.
ThalidomideDiazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Theophylline.
TocilizumabThe serum concentration of Diazepam can be decreased when it is combined with Tocilizumab.
YohimbineThe therapeutic efficacy of Diazepam can be decreased when used in combination with Yohimbine.
ZolpidemDiazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (caffeine).
  • Avoid taking with grapefruit or grapefruit juice as grapefruit can significantly increase serum levels of this product.
  • Take with food.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA2
Uniprot ID:
P47869
Molecular Weight:
51325.85 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA3
Uniprot ID:
P34903
Molecular Weight:
55164.055 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Transporter activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA5
Uniprot ID:
P31644
Molecular Weight:
52145.645 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
  3. Derry JM, Dunn SM, Davies M: Identification of a residue in the gamma-aminobutyric acid type A receptor alpha subunit that differentially affects diazepam-sensitive and -insensitive benzodiazepine site binding. J Neurochem. 2004 Mar;88(6):1431-8. [PubMed:15009644 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRB1
Uniprot ID:
P18505
Molecular Weight:
54234.085 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB2
Uniprot ID:
P47870
Molecular Weight:
59149.895 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-gated chloride ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRB3
Uniprot ID:
P28472
Molecular Weight:
54115.04 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRG1
Uniprot ID:
Q8N1C3
Molecular Weight:
53594.49 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
Gene Name:
GABRG2
Uniprot ID:
P18507
Molecular Weight:
54161.78 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRG3
Uniprot ID:
Q99928
Molecular Weight:
54288.16 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-a receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRD
Uniprot ID:
O14764
Molecular Weight:
50707.835 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRE
Uniprot ID:
P78334
Molecular Weight:
57971.175 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-a receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to ...
Gene Name:
GABRP
Uniprot ID:
O00591
Molecular Weight:
50639.735 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-a receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-1 GABA receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR1
Uniprot ID:
P24046
Molecular Weight:
55882.91 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-a receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Rho-2 GABA receptor could play a role in retinal neurotransmission.
Gene Name:
GABRR2
Uniprot ID:
P28476
Molecular Weight:
54150.41 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Gaba-a receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRR3
Uniprot ID:
A8MPY1
Molecular Weight:
54271.1 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Transmembrane signaling receptor activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRQ
Uniprot ID:
Q9UN88
Molecular Weight:
72020.875 Da
References
  1. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [PubMed:11752090 ]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [PubMed:18384456 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
potentiator
General Function:
Cholesterol binding
Specific Function:
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benz...
Gene Name:
TSPO
Uniprot ID:
P30536
Molecular Weight:
18827.81 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 ]
  2. Falchi AM, Battetta B, Sanna F, Piludu M, Sogos V, Serra M, Melis M, Putzolu M, Diaz G: Intracellular cholesterol changes induced by translocator protein (18 kDa) TSPO/PBR ligands. Neuropharmacology. 2007 Aug;53(2):318-29. Epub 2007 Jun 2. [PubMed:17631921 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
positive allosteric modulator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. ChEMBL Compound Report Card [Link]

Enzymes

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 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 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
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 ]
  3. Jung F, Richardson TH, Raucy JL, Johnson EF: Diazepam metabolism by cDNA-expressed human 2C P450s: identification of P4502C18 and P4502C19 as low K(M) diazepam N-demethylases. Drug Metab Dispos. 1997 Feb;25(2):133-9. [PubMed:9029042 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Jung F, Richardson TH, Raucy JL, Johnson EF: Diazepam metabolism by cDNA-expressed human 2C P450s: identification of P4502C18 and P4502C19 as low K(M) diazepam N-demethylases. Drug Metab Dispos. 1997 Feb;25(2):133-9. [PubMed:9029042 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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. Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M: Substrate inhibition kinetics for cytochrome P450-catalyzed reactions. Drug Metab Dispos. 2001 Apr;29(4 Pt 1):368-74. [PubMed:11259318 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. 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 ]
  2. Source [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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.
Gene Name:
CYP2C18
Uniprot ID:
P33260
Molecular Weight:
55710.075 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 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 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Tassaneeyakul W, Birkett DJ, Miners JO: Inhibition of human hepatic cytochrome P4502E1 by azole antifungals, CNS-active drugs and non-steroidal anti-inflammatory agents. Xenobiotica. 1998 Mar;28(3):293-301. [PubMed:9574817 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
no
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. Bertucci C, Wainer IW: Improved chromatographic performance of a modified human albumin based stationary phase. Chirality. 1997;9(4):335-40. [PubMed:9275312 ]
  2. Brodersen R, Honore B: Drug binding properties of neonatal albumin. Acta Paediatr Scand. 1989 May;78(3):342-6. [PubMed:2545072 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M, Lin JH: In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther. 2001 Mar;296(3):723-35. [PubMed:11181899 ]
  2. Adachi Y, Suzuki H, Sugiyama Y: Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8. [PubMed:11785684 ]
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Drug created on June 13, 2005 07:24 / Updated on April 11, 2014 14:50