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Identification
NameMeprobamate
Accession NumberDB00371  (APRD01095)
TypeSmall Molecule
GroupsApproved, Illicit
Description

A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of anxiety disorders, and also for the short-term management of insomnia but has largely been superseded by the benzodiazepines. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) Meprobamate is a controlled substance in the U.S.

Structure
Thumb
Synonyms
Equanil
Meprobamat
Meprobamato
Meprobamatum
Meprobamic acid
Miltown
External Identifiers
  • DEA No. 2820
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Equanil Tablets 400mgtablet400 mgoralWyeth Ayerst Canada Inc.1994-12-312000-03-07Canada
Meditran 400mgtablet400 mgoralMedic Laboratory LtÉe1959-12-311996-09-09Canada
Meprobamate Tab 400mgtablet400 mgoralPro Doc Limitee1959-12-312001-10-15Canada
Meprobamate Tab 400mgtablet400 mgoralDuchesnay Inc1978-12-312001-10-15Canada
Novo-mepro 200mgtablet200 mgoralNovopharm Limited1967-12-312005-08-10Canada
Novo-mepro 400mgtablet400 mgoralNovopharm Limited1967-12-312005-08-10Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo Meprobamate Tab 400mgtablet400 mgoralApotex Inc1975-12-312001-10-09Canada
Meprobamatetablet400 mg/1oralWatson Laboratories, Inc.1973-05-03Not applicableUs
Meprobamatetablet200 mg/1oralTaro Pharmaceutical Industries Ltd.2011-05-23Not applicableUs
Meprobamatetablet200 mg/1oralAvera Mc Kennan Hospital2015-11-03Not applicableUs
Meprobamatetablet400 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2011-05-23Not applicableUs
Meprobamatetablet200 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2011-05-23Not applicableUs
Meprobamatetablet400 mg/1oralAlembic Pharmaceuticals Inc.2015-12-01Not applicableUs
Meprobamatetablet400 mg/1oralAlembic Pharmaceuticals Limited2013-07-23Not applicableUs
Meprobamatetablet200 mg/1oralAlembic Pharmaceuticals Inc.2015-12-01Not applicableUs
Meprobamatetablet200 mg/1oralAlembic Pharmaceuticals Limited2013-07-23Not applicableUs
Meprobamatetablet400 mg/1oralDr.Reddy's Laboratories Limited2008-01-03Not applicableUs
Meprobamatetablet400 mg/1oralHeritage Pharmaceuticals Inc.2009-05-01Not applicableUs
Meprobamatetablet200 mg/1oralDr.Reddy's Laboratories Limited2008-01-03Not applicableUs
Meprobamatetablet200 mg/1oralHeritage Pharmaceuticals Inc.2009-05-01Not applicableUs
Meprobamatetablet400 mg/1oralTaro Pharmaceutical Industries Ltd.2011-05-23Not applicableUs
Meprobamatetablet200 mg/1oralWatson Laboratories, Inc.1973-04-23Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
EquanilWyeth
MeprospanNot Available
MiltownWallace Laboratories
Brand mixtures
NameLabellerIngredients
282 Mep TabMerck Frosst Canada & Cie, Merck Frosst Canada & Co.
Equagesic TabletsWyeth Ayerst Canada Inc.
SaltsNot Available
Categories
UNII9I7LNY769Q
CAS number57-53-4
WeightAverage: 218.2502
Monoisotopic: 218.126657074
Chemical FormulaC9H18N2O4
InChI KeyInChIKey=NPPQSCRMBWNHMW-UHFFFAOYSA-N
InChI
InChI=1S/C9H18N2O4/c1-3-4-9(2,5-14-7(10)12)6-15-8(11)13/h3-6H2,1-2H3,(H2,10,12)(H2,11,13)
IUPAC Name
2-[(carbamoyloxy)methyl]-2-methylpentyl carbamate
SMILES
CCCC(C)(COC(N)=O)COC(N)=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as organooxygen compounds. These are organic compounds containing a bond between a carbon atom and an oxygen atom.
KingdomOrganic compounds
Super ClassOrganooxygen compounds
ClassNot Available
Sub ClassNot Available
Direct ParentOrganooxygen compounds
Alternative Parents
Substituents
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Aliphatic acyclic compound
Molecular FrameworkAliphatic acyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of anxiety disorders or for the short-term relief of the symptoms of anxiety.
PharmacodynamicsMeprobamate is an anxiolytic drug. It was the best selling minor tranquilizer for a time but has largely been replaced by benzodiazepines. Meprobamate has most of the pharmacological effects and dangers of the barbiturates (though it was marketed as being safer). However, it is less sedating at effective doses. It is reported to have some anticonvulsant properties against absence seizures, but can exacerbate generalized tonic-clonic seizures. It has also been used as a hypnotic (sleeping pill). However, its is currently only licensed as an anxiolytic and it is a third or fourth-order choice.
Mechanism of actionMeprobamate's mechanism of action is not known. It has been shown in animal studies to have effects at multiple sites in the central nervous system, including the thalamus and limbic system. Meprobamate binds to GABAA receptors which interrupt neuronal communication in the reticular formation and spinal cord, causing sedation and altered perception of pain.
Related Articles
AbsorptionWell absorbed from the gastrointestinal tract.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half lifePlasma half-life is about 10 hours.
ClearanceNot Available
ToxicitySymptoms of overdose include coma, drowsiness, loss of muscle control, severely impaired breathing, shock, sluggishness, and unresponsiveness. Death has been reported with ingestion of as little as 12 g meprobamate and survival with as much as 40 g.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Capecitabine Metabolism PathwayDrug metabolismSMP00607
Capecitabine Action PathwayDrug actionSMP00469
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9534
Blood Brain Barrier+0.9864
Caco-2 permeable-0.5731
P-glycoprotein substrateNon-substrate0.5282
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.9033
Renal organic cation transporterNon-inhibitor0.945
CYP450 2C9 substrateNon-substrate0.9108
CYP450 2D6 substrateNon-substrate0.8961
CYP450 3A4 substrateNon-substrate0.7032
CYP450 1A2 substrateNon-inhibitor0.8381
CYP450 2C9 inhibitorNon-inhibitor0.8799
CYP450 2D6 inhibitorNon-inhibitor0.8764
CYP450 2C19 inhibitorNon-inhibitor0.8754
CYP450 3A4 inhibitorNon-inhibitor0.8735
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8914
Ames testNon AMES toxic0.8706
CarcinogenicityNon-carcinogens0.7304
BiodegradationNot ready biodegradable0.965
Rat acute toxicity2.4075 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9943
hERG inhibition (predictor II)Non-inhibitor0.9322
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Glaxosmithkline llc
  • Medpointe pharmaceuticals medpointe healthcare inc
  • Wyeth ayerst laboratories
  • Ferndale laboratories inc
  • Alra laboratories inc
  • Teva pharmaceuticals usa inc
  • Alembic ltd
  • Barr laboratories inc
  • Elkins sinn div ah robins co inc
  • Heather drug co inc
  • Impax laboratories inc
  • Invagen pharmaceuticals inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Ivc industries inc dba inverness medical nutritionals group
  • Lannett co inc
  • Lederle laboratories div american cyanamid co
  • Km lee laboratories inc
  • Mallard inc
  • Mk laboratories inc
  • Mutual pharmaceutical co inc
  • Mylan pharmaceuticals inc
  • Nexgen pharma inc
  • Parke davis div warner lambert co
  • L perrigo co
  • Pharmavite pharmaceuticals
  • Purepac pharmaceutical co
  • Private formulations inc
  • Roxane laboratories inc
  • Sandoz inc
  • Scherer laboratories inc
  • Solvay pharmaceuticals
  • Stanlabs pharmaceutical co sub simpak corp
  • Tablicaps inc
  • Usl pharma inc
  • Valeant pharmaceuticals international
  • Vangard laboratories inc div midway medical co
  • Watson laboratories inc
  • West ward pharmaceutical corp
  • Whiteworth towne paulsen inc
  • Halsey drug co inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Tabletoral400 mg
Tabletoral200 mg/1
Tabletoral400 mg/1
Tabletoral200 mg
Prices
Unit descriptionCostUnit
Mepron 750 mg/5ml Suspension5.41USD ml
Mepron 750 mg/5 ml suspension4.95USD ml
Meprobamate 200 mg tablet1.42USD tablet
Meprobamate 400 mg tablet0.84USD tablet
Meprozine 50-25 mg capsule0.78USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1336266 No1995-07-112012-07-11Canada
CA2152615 No2001-10-162013-12-23Canada
US4981874 No1992-08-152009-08-15Us
US6649659 No1997-01-102017-01-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point105 °CPhysProp
water solubility4700 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP0.70HANSCH,C ET AL. (1995)
logS-1.67ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility2.47 mg/mLALOGPS
logP1.06ALOGPS
logP0.93ChemAxon
logS-1.9ALOGPS
pKa (Strongest Acidic)15.17ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area104.64 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity53.04 m3·mol-1ChemAxon
Polarizability22.65 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (10.1 KB)
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05BC01N05BC51N05CX01
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (52.6 KB)
Interactions
Drug Interactions
Drug
AzelastineMeprobamate 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 Meprobamate.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
BuprenorphineMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
EthanolMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
HydrocodoneMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Meprobamate.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
MefloquineThe therapeutic efficacy of Meprobamate can be decreased when used in combination with Mefloquine.
MethotrimeprazineMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineMeprobamate may increase the sedative activities of Metyrosine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
MirtazapineMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
OrlistatThe serum concentration of Meprobamate can be decreased when it is combined with Orlistat.
OrphenadrineMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Meprobamate is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
PramipexoleMeprobamate may increase the sedative activities of Pramipexole.
RopiniroleMeprobamate may increase the sedative activities of Ropinirole.
RotigotineMeprobamate may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Meprobamate.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
SuvorexantMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Meprobamate.
ThalidomideMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
YohimbineThe therapeutic efficacy of Meprobamate can be decreased when used in combination with Yohimbine.
ZolpidemMeprobamate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Take without regard to meals. Avoid alcohol.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
  3. 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
yes
Actions
agonist
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. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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:
GABRA4
Uniprot ID:
P48169
Molecular Weight:
61622.645 Da
References
  1. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
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:
GABRA6
Uniprot ID:
Q16445
Molecular Weight:
51023.69 Da
References
  1. Rho JM, Donevan SD, Rogawski MA: Barbiturate-like actions of the propanediol dicarbamates felbamate and meprobamate. J Pharmacol Exp Ther. 1997 Mar;280(3):1383-91. [PubMed:9067327 ]
  2. Gonzalez LA, Gatch MB, Taylor CM, Bell-Horner CL, Forster MJ, Dillon GH: Carisoprodol-mediated modulation of GABAA receptors: in vitro and in vivo studies. J Pharmacol Exp Ther. 2009 May;329(2):827-37. doi: 10.1124/jpet.109.151142. Epub 2009 Feb 24. [PubMed:19244096 ]
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
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. 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:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
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. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, Polli JW: Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther. 2002 Dec;303(3):1029-37. [PubMed:12438524 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:10