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Identification
NameClorazepate
Accession NumberDB00628  (APRD00881)
TypeSmall Molecule
GroupsApproved, Illicit
Description

A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. [PubChem]

Structure
Thumb
Synonyms
7-chloro-2,3-dihydro-2,2-Dihydroxy-5-phenyl-1H-1,4-benzodiazepine-3-carboxylic acid
Clorazepate
Clorazepic acid
External Identifiers
  • Abbott 35616
  • AH 3232
  • CB 4306
  • Ro 6-6616
  • TR 19119
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clorazepatecapsule7.5 mgoralAa Pharma Inc1990-12-31Not applicableCanada
Clorazepatecapsule3.75 mgoralAa Pharma Inc1990-12-31Not applicableCanada
Clorazepatecapsule15 mgoralAa Pharma Inc1990-12-31Not applicableCanada
Novo-clopate Cap 15mgcapsule15 mgoralNovopharm Limited1984-12-312015-10-26Canada
Novo-clopate Cap 3.75mgcapsule3.75 mgoralNovopharm Limited1984-12-312015-10-26Canada
Novo-clopate Cap 7.5mgcapsule7.5 mgoralNovopharm Limited1984-12-312015-10-26Canada
Tranxene Cap 15mgcapsule15 mgoralAbbott Laboratories, Limited1973-12-312003-08-01Canada
Tranxene Cap 3.75mgcapsule3.75 mgoralAbbott Laboratories, Limited1973-12-312003-08-01Canada
Tranxene Cap 7.5mgcapsule7.5 mgoralAbbott Laboratories, Limited1976-12-312003-08-01Canada
Tranxene T-tabtablet3.75 mg/1oralRECORDATI RARE DISEASES, INC.1972-06-23Not applicableUs
Tranxene T-tabtablet15 mg/1oralRECORDATI RARE DISEASES, INC.1972-06-23Not applicableUs
Tranxene T-tabtablet7.5 mg/1oralRECORDATI RARE DISEASES, INC.1972-06-23Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Clorazepate Dipotassiumtablet15 mg/1oralRanbaxy Pharmaceuticals Inc.2005-01-14Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralPd Rx Pharmaceuticals, Inc.2005-01-14Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralMylan Pharmaceuticals Inc.1987-07-17Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralbryant ranch prepack2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralRanbaxy Pharmaceuticals Inc.2005-01-14Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-29Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralRanbaxy Pharmaceuticals Inc.2005-01-14Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-29Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralA S Medication Solutions Llc2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralPd Rx Pharmaceuticals, Inc.2010-07-29Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralRebel Distributors Corp2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralAmerican Health Packaging2014-07-31Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralRebel Distributors Corp2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralContract Pharmacy Services Pa2011-03-29Not applicableUs
Clorazepate Dipotassiumtablet3.75 mg/1oralTaro Pharmaceuticals U.S.A., Inc.2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralMylan Pharmaceuticals Inc.1987-07-17Not applicableUs
Clorazepate Dipotassiumtablet15 mg/1oralbryant ranch prepack2000-04-27Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralbryant ranch prepack2005-01-14Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralREMEDYREPACK INC.2010-11-18Not applicableUs
Clorazepate Dipotassiumtablet7.5 mg/1oralMylan Pharmaceuticals Inc.1987-07-17Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AnksenSanovel
CalnerMedipharm
CloranxenTeva
Clorazepatumsanofi-aventis
ClozeneWeidar
DipotAsian
FluliumPharmasant
Gen-xeneAlra
JustumSandoz
ManotranMarch
MedipaxTecnifar
MendonAbbott Japan
PolizepPolipharm
TencilanFinadiet
TrancapT P Drug
Transenesanofi-aventis
Tranxensanofi-aventis
Tranxènesanofi-aventis
TranxeneLundbeck
Tranxilenesanofi-aventis
Tranxiliumsanofi-aventis
Zetran-5Masa Lab
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Clorazepate dipotassium
ThumbNot applicableDBSALT000953
Categories
UNIID51WO0G0L4
CAS number23887-31-2
WeightAverage: 314.723
Monoisotopic: 314.045819935
Chemical FormulaC16H11ClN2O3
InChI KeyInChIKey=XDDJGVMJFWAHJX-UHFFFAOYSA-N
InChI
InChI=1S/C16H11ClN2O3/c17-10-6-7-12-11(8-10)13(9-4-2-1-3-5-9)19-14(16(21)22)15(20)18-12/h1-8,14H,(H,18,20)(H,21,22)
IUPAC Name
7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine-3-carboxylic acid
SMILES
OC(=O)C1N=C(C2=CC=CC=C2)C2=C(NC1=O)C=CC(Cl)=C2
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
  • Alpha-amino acid or derivatives
  • Benzenoid
  • 1,3-dicarbonyl compound
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Secondary carboxylic acid amide
  • Lactam
  • Ketimine
  • Carboxamide group
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Also used as adjunctive therapy in the management of partial seizures and for the symptomatic relief of acute alcohol withdrawal.
PharmacodynamicsClorazepate is a member of the group of drugs called benzodiazepines. Pharmacologically, clorazepate has the characteristics of the benzodiazepines. It has depressant effects on the central nervous system. The primary metabolite, nordiazepam, quickly appears in the blood stream. Studies in healthy men have shown that clorazenate has depressant effects on the central nervous system. Since orally administered clorazepate dipotassium is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug.
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects 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 the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Related Articles
AbsorptionRapidly absorbed following oral administration (bioavailability is 91%).
Volume of distributionNot Available
Protein bindingThe protein binding of nordiazepam in plasma is high (97-98%).
Metabolism

The drug is metabolized in the liver and excreted primarily in the urine. The primary metabolite, nordiazepam, is further metabolized by hydroxylation. The major urinary metabolite is conjugated oxazepam (3-hydroxynordiazepam), and smaller amounts of conjugated p-hydroxynordiazepam and nordiazepam are also found in the urine.

SubstrateEnzymesProduct
Clorazepate
Not Available
OxazepamDetails
Clorazepate
Not Available
3-hydroxynordiazepamDetails
Clorazepate
NordiazepamDetails
Clorazepate
Not Available
p-HydroxynordiazepamDetails
Route of eliminationThe drug is metabolized in the liver and excreted primarily in the urine.
Half lifeThe serum half-life is about 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours.
ClearanceNot Available
ToxicityOral LD50 in rats is 1320 mg/kg. In monkeys, oral LD50 exceed 1600 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
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+0.9285
Blood Brain Barrier+0.8373
Caco-2 permeable+0.5909
P-glycoprotein substrateNon-substrate0.5597
P-glycoprotein inhibitor INon-inhibitor0.9328
P-glycoprotein inhibitor IINon-inhibitor0.9386
Renal organic cation transporterNon-inhibitor0.9049
CYP450 2C9 substrateNon-substrate0.7365
CYP450 2D6 substrateNon-substrate0.8745
CYP450 3A4 substrateNon-substrate0.5798
CYP450 1A2 substrateInhibitor0.7086
CYP450 2C9 inhibitorNon-inhibitor0.756
CYP450 2D6 inhibitorNon-inhibitor0.819
CYP450 2C19 inhibitorNon-inhibitor0.7451
CYP450 3A4 inhibitorNon-inhibitor0.8333
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8165
Ames testNon AMES toxic0.8311
CarcinogenicityNon-carcinogens0.659
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9282 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9987
hERG inhibition (predictor II)Non-inhibitor0.9207
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Able laboratories inc
  • American therapeutics inc
  • Clonmel healthcare ltd
  • Gd searle llc
  • Mylan pharmaceuticals inc
  • Purepac pharmaceutical co
  • Quantum pharmics ltd
  • Sandoz inc
  • Usl pharma inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
  • Lundbeck inc
  • Lederle laboratories div american cyanamid co
  • Ranbaxy laboratories ltd
  • Taro pharmaceuticals usa inc
  • Alra laboratories inc
Packagers
Dosage forms
FormRouteStrength
Capsuleoral15 mg
Capsuleoral3.75 mg
Capsuleoral7.5 mg
Tabletoral15 mg/1
Tabletoral3.75 mg/1
Tabletoral7.5 mg/1
Prices
Unit descriptionCostUnit
Tranxene t-tablet 15 mg5.41USD tablet
Tranxene-T 15 mg tablet5.08USD tablet
Tranxene t-tablet 7.5 mg3.99USD tablet
Tranxene-T 7.5 mg tablet3.6USD tablet
Tranxene t-tablet 3.75 mg3.21USD tablet
Tranxene-T 3.75 mg tablet3.04USD tablet
Clorazepate 15 mg tablet2.17USD tablet
Clorazepate Dipotassium 15 mg tablet1.27USD tablet
Clorazepate Dipotassium 7.5 mg tablet0.93USD tablet
Clorazepate 7.5 mg tablet0.79USD tablet
Clorazepate Dipotassium 3.75 mg tablet0.76USD tablet
Clorazepate 3.75 mg tablet0.73USD tablet
Apo-Clorazepate 15 mg Capsule0.4USD capsule
Apo-Clorazepate 7.5 mg Capsule0.2USD capsule
Apo-Clorazepate 3.75 mg Capsule0.15USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityVery solubleNot Available
logP3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0248 mg/mLALOGPS
logP2.68ALOGPS
logP3.21ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)3.32ChemAxon
pKa (Strongest Basic)-0.64ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.76 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity82.68 m3·mol-1ChemAxon
Polarizability30.63 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

Schmitt, J.; U.S. Patent 3,516,988; June 23, 1970.

General References
  1. Authors unspecified: Systematic review of the benzodiazepines. Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Committee on the Review of Medicines. Br Med J. 1980 Mar 29;280(6218):910-2. [PubMed:7388368 ]
  2. McElhatton PR: The effects of benzodiazepine use during pregnancy and lactation. Reprod Toxicol. 1994 Nov-Dec;8(6):461-75. [PubMed:7881198 ]
External Links
ATC CodesNot Available
AHFS Codes
  • 28:24.08
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AprepitantThe serum concentration of Clorazepate can be increased when it is combined with Aprepitant.
AzelastineClorazepate 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 Clorazepate.
BexaroteneThe serum concentration of Clorazepate can be decreased when it is combined with Bexarotene.
BosentanThe serum concentration of Clorazepate can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
BuprenorphineClorazepate may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ClozapineThe risk or severity of adverse effects can be increased when Clorazepate is combined with Clozapine.
ConivaptanThe serum concentration of Clorazepate can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Clorazepate can be decreased when it is combined with Dabrafenib.
DasatinibThe serum concentration of Clorazepate can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Clorazepate can be decreased when it is combined with Deferasirox.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
EthanolClorazepate may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FluconazoleThe metabolism of Clorazepate can be decreased when combined with Fluconazole.
FosamprenavirThe serum concentration of Clorazepate can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Clorazepate can be increased when it is combined with Fosaprepitant.
Fusidic AcidThe serum concentration of Clorazepate can be increased when it is combined with Fusidic Acid.
HydrocodoneClorazepate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
IdelalisibThe serum concentration of Clorazepate can be increased when it is combined with Idelalisib.
IvacaftorThe serum concentration of Clorazepate can be increased when it is combined with Ivacaftor.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Clorazepate.
LuliconazoleThe serum concentration of Clorazepate can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
MethadoneClorazepate may increase the central nervous system depressant (CNS depressant) activities of Methadone.
MethotrimeprazineClorazepate may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineClorazepate may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Clorazepate can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
MirtazapineClorazepate may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Clorazepate can be decreased when it is combined with Mitotane.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
NelfinavirThe metabolism of Clorazepate can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Clorazepate can be increased when it is combined with Netupitant.
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Clorazepate.
OrphenadrineClorazepate may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Clorazepate can be increased when it is combined with Palbociclib.
ParaldehydeClorazepate may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Clorazepate is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Clorazepate.
PhenytoinThe metabolism of Clorazepate can be increased when combined with Phenytoin.
PramipexoleClorazepate may increase the sedative activities of Pramipexole.
RitonavirThe serum concentration of Clorazepate can be increased when it is combined with Ritonavir.
RopiniroleClorazepate may increase the sedative activities of Ropinirole.
RotigotineClorazepate may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Clorazepate.
SaquinavirThe serum concentration of Clorazepate can be increased when it is combined with Saquinavir.
SiltuximabThe serum concentration of Clorazepate can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Clorazepate can be increased when it is combined with Simeprevir.
Sodium oxybateClorazepate may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
St. John's WortThe serum concentration of Clorazepate can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Clorazepate can be increased when it is combined with Stiripentol.
SuvorexantClorazepate may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Clorazepate.
TeduglutideThe serum concentration of Clorazepate can be increased when it is combined with Teduglutide.
ThalidomideClorazepate may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Theophylline.
TocilizumabThe serum concentration of Clorazepate can be decreased when it is combined with Tocilizumab.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Clorazepate.
YohimbineThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Yohimbine.
ZolpidemClorazepate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

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. 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
agonist
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. Park CH, Carboni E, Wood PL, Gee KW: Characterization of peripheral benzodiazepine type sites in a cultured murine BV-2 microglial cell line. Glia. 1996 Jan;16(1):65-70. [PubMed:8787774 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Dresser GK, Spence JD, Bailey DG: Pharmacokinetic-pharmacodynamic consequences and clinical relevance of cytochrome P450 3A4 inhibition. Clin Pharmacokinet. 2000 Jan;38(1):41-57. [PubMed:10668858 ]
  2. Sachs B, Erdmann S, Al-Masaoudi T, Merk HF: In vitro drug allergy detection system incorporating human liver microsomes in chlorazepate-induced skin rash: drug-specific proliferation associated with interleukin-5 secretion. Br J Dermatol. 2001 Feb;144(2):316-20. [PubMed:11251565 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on April 08, 2014 11:29