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Identification
NameClotiazepam
Accession NumberDB01559
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionClotiazepam is a benzodiazepine derivative, not approved for sale in the U.S. or Canada, but has been approved in the U.K. It is a schedule IV drug in Canada.
Structure
Thumb
Synonyms
Clotiazepamum
Rize
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ClozanPfizer
DistensanEsteve
RizeDae Woong
RizenFormenti
TienorFarmaka
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIZCN055599V
CAS number33671-46-4
WeightAverage: 318.821
Monoisotopic: 318.059361509
Chemical FormulaC16H15ClN2OS
InChI KeyCHBRHODLKOZEPZ-UHFFFAOYSA-N
InChI
InChI=1S/C16H15ClN2OS/c1-3-10-8-12-15(11-6-4-5-7-13(11)17)18-9-14(20)19(2)16(12)21-10/h4-8H,3,9H2,1-2H3
IUPAC Name
5-(2-chlorophenyl)-7-ethyl-1-methyl-1H,2H,3H-thieno[2,3-e][1,4]diazepin-2-one
SMILES
CCC1=CC2=C(S1)N(C)C(=O)CN=C2C1=CC=CC=C1Cl
Pharmacology
IndicationFor the treatment of anxiety disorders.
Structured Indications Not Available
PharmacodynamicsClotiazepam is a benzodiazepine derivative possessing anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Stage 2 NREM sleep is significantly increased by clotiazepam.
Mechanism of actionClotiazepam acts at the benzodiazepine receptors (BZD). This agonizes the action of GABA, increasing the frequency of opening of the channel chlorinates and penetration of the ions chlorinates through the ionophore. Increase in membrane polarization decreases the probability of discharge of neurons.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gamma-aminobutyric acid receptor subunit alpha-1Proteinyes
potentiator
HumanP14867 details
Gamma-aminobutyric acid receptor subunit alpha-2Proteinyes
potentiator
HumanP47869 details
Gamma-aminobutyric acid receptor subunit alpha-3Proteinyes
potentiator
HumanP34903 details
Gamma-aminobutyric acid receptor subunit alpha-5Proteinyes
potentiator
HumanP31644 details
Gamma-aminobutyric acid receptor subunit gamma-1Proteinyes
potentiator
HumanQ8N1C3 details
Gamma-aminobutyric acid receptor subunit gamma-2Proteinyes
potentiator
HumanP18507 details
Gamma-aminobutyric acid receptor subunit gamma-3Proteinyes
potentiator
HumanQ99928 details
Gamma-aminobutyric acid receptor subunit beta-1Proteinyes
potentiator
HumanP18505 details
Gamma-aminobutyric acid receptor subunit beta-2Proteinyes
potentiator
HumanP47870 details
Gamma-aminobutyric acid receptor subunit beta-3Proteinyes
potentiator
HumanP28472 details
Gamma-aminobutyric acid receptor subunit deltaProteinyes
potentiator
HumanO14764 details
Gamma-aminobutyric acid receptor subunit epsilonProteinyes
potentiator
HumanP78334 details
Gamma-aminobutyric acid receptor subunit piProteinyes
potentiator
HumanO00591 details
Gamma-aminobutyric acid receptor subunit rho-1Proteinyes
potentiator
HumanP24046 details
Gamma-aminobutyric acid receptor subunit rho-2Proteinyes
potentiator
HumanP28476 details
Gamma-aminobutyric acid receptor subunit rho-3Proteinyes
potentiator
HumanA8MPY1 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding99% bound to plasma proteins.
Metabolism

Hepatic.

Route of eliminationNot Available
Half life4 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe metabolism of Clotiazepam can be decreased when combined with Abiraterone.Approved
AmiodaroneThe metabolism of Clotiazepam can be decreased when combined with Amiodarone.Approved, Investigational
AprepitantThe serum concentration of Clotiazepam can be increased when it is combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Clotiazepam can be decreased when combined with Armodafinil.Approved, Investigational
AtazanavirThe metabolism of Clotiazepam can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Clotiazepam can be decreased when combined with Atomoxetine.Approved
BexaroteneThe serum concentration of Clotiazepam can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Clotiazepam can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Clotiazepam can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Clotiazepam can be decreased when it is combined with Bosentan.Approved, Investigational
CarbamazepineThe metabolism of Clotiazepam can be increased when combined with Carbamazepine.Approved, Investigational
CeritinibThe serum concentration of Clotiazepam can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Clotiazepam can be decreased when combined with Chloramphenicol.Approved, Vet Approved
CholecalciferolThe metabolism of Clotiazepam can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Clotiazepam can be decreased when combined with Cimetidine.Approved
CitalopramThe metabolism of Clotiazepam can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Clotiazepam can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Clotiazepam can be decreased when combined with Clemastine.Approved
ClopidogrelThe metabolism of Clotiazepam can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Clotiazepam can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Clotiazepam can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Clotiazepam can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Clotiazepam can be decreased when combined with Crizotinib.Approved
CyclosporineThe metabolism of Clotiazepam can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Clotiazepam can be decreased when it is combined with Dabrafenib.Approved
DarunavirThe metabolism of Clotiazepam can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Clotiazepam can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Clotiazepam can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Clotiazepam can be decreased when combined with Delavirdine.Approved
DesipramineThe metabolism of Clotiazepam can be decreased when combined with Desipramine.Approved
DexamethasoneThe serum concentration of Clotiazepam can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DihydroergotamineThe metabolism of Clotiazepam can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Clotiazepam can be decreased when combined with Diltiazem.Approved
DoxorubicinThe metabolism of Clotiazepam can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Clotiazepam can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Clotiazepam can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Clotiazepam can be decreased when it is combined with Efavirenz.Approved, Investigational
EnzalutamideThe serum concentration of Clotiazepam can be decreased when it is combined with Enzalutamide.Approved
ErythromycinThe metabolism of Clotiazepam can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Clotiazepam can be decreased when it is combined with Eslicarbazepine acetate.Approved
EsomeprazoleThe metabolism of Clotiazepam can be decreased when combined with Esomeprazole.Approved, Investigational
EtravirineThe serum concentration of Clotiazepam can be decreased when it is combined with Etravirine.Approved
FluconazoleThe metabolism of Clotiazepam can be decreased when combined with Fluconazole.Approved
FluoxetineThe metabolism of Clotiazepam can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe metabolism of Clotiazepam can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Clotiazepam can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Clotiazepam can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Clotiazepam can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Clotiazepam can be increased when it is combined with Fusidic Acid.Approved
GemfibrozilThe metabolism of Clotiazepam can be decreased when combined with Gemfibrozil.Approved
IdelalisibThe serum concentration of Clotiazepam can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Clotiazepam can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Clotiazepam can be decreased when combined with Indinavir.Approved
IsavuconazoniumThe metabolism of Clotiazepam can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Clotiazepam can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Clotiazepam can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Clotiazepam can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Clotiazepam can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Clotiazepam can be decreased when combined with Ketoconazole.Approved, Investigational
LopinavirThe metabolism of Clotiazepam can be decreased when combined with Lopinavir.Approved
LovastatinThe metabolism of Clotiazepam can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Clotiazepam can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Clotiazepam can be decreased when it is combined with Lumacaftor.Approved
MifepristoneThe serum concentration of Clotiazepam can be increased when it is combined with Mifepristone.Approved, Investigational
MitotaneThe serum concentration of Clotiazepam can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Clotiazepam can be decreased when combined with Moclobemide.Approved
ModafinilThe serum concentration of Clotiazepam can be decreased when it is combined with Modafinil.Approved, Investigational
NafcillinThe serum concentration of Clotiazepam can be decreased when it is combined with Nafcillin.Approved
NefazodoneThe metabolism of Clotiazepam can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Clotiazepam can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Clotiazepam can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Clotiazepam can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Clotiazepam can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Clotiazepam can be decreased when combined with Nilotinib.Approved, Investigational
OlaparibThe metabolism of Clotiazepam can be decreased when combined with Olaparib.Approved
OmeprazoleThe metabolism of Clotiazepam can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Clotiazepam can be increased when it is combined with Osimertinib.Approved
PalbociclibThe serum concentration of Clotiazepam can be increased when it is combined with Palbociclib.Approved
PantoprazoleThe metabolism of Clotiazepam can be decreased when combined with Pantoprazole.Approved
ParoxetineThe metabolism of Clotiazepam can be decreased when combined with Paroxetine.Approved, Investigational
PentobarbitalThe metabolism of Clotiazepam can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Clotiazepam can be increased when combined with Phenobarbital.Approved
PhenytoinThe metabolism of Clotiazepam can be increased when combined with Phenytoin.Approved, Vet Approved
PosaconazoleThe metabolism of Clotiazepam can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrimidoneThe metabolism of Clotiazepam can be increased when combined with Primidone.Approved, Vet Approved
QuazepamThe serum concentration of Clotiazepam can be increased when it is combined with Quazepam.Approved, Illicit
RanolazineThe metabolism of Clotiazepam can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Clotiazepam can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Clotiazepam can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Clotiazepam can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Clotiazepam can be decreased when combined with Ritonavir.Approved, Investigational
SaquinavirThe metabolism of Clotiazepam can be decreased when combined with Saquinavir.Approved, Investigational
SertralineThe metabolism of Clotiazepam can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Clotiazepam can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Clotiazepam can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Clotiazepam can be increased when it is combined with Simeprevir.Approved
SorafenibThe metabolism of Clotiazepam can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Clotiazepam can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Clotiazepam can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Clotiazepam can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TelaprevirThe metabolism of Clotiazepam can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Clotiazepam can be decreased when combined with Telithromycin.Approved
ThiotepaThe metabolism of Clotiazepam can be decreased when combined with Thiotepa.Approved
TiclopidineThe metabolism of Clotiazepam can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Clotiazepam can be decreased when it is combined with Tocilizumab.Approved
TopiramateThe metabolism of Clotiazepam can be decreased when combined with Topiramate.Approved
TranylcypromineThe metabolism of Clotiazepam can be decreased when combined with Tranylcypromine.Approved
VenlafaxineThe metabolism of Clotiazepam can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Clotiazepam can be decreased when combined with Verapamil.Approved
VoriconazoleThe metabolism of Clotiazepam can be decreased when combined with Voriconazole.Approved, Investigational
YohimbineThe therapeutic efficacy of Clotiazepam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZiprasidoneThe metabolism of Clotiazepam can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis Reference

Nakanishi, M., Araki, K.,Tahara, T. and Shiroki, M.; US. Patent 3,849,405; November 19, 1974; assigned to Yoshitomi Pharmaceutical Industries, Ltd.

General References
  1. Nakazawa Y, Kotorii M, Oshima M, Horikawa S, Tachibana H: Effects of thienodiazepine derivatives on human sleep as compared to those of benzodiazepine derivatives. Psychopharmacologia. 1975 Oct 31;44(2):165-71. [PubMed:709 ]
External Links
ATC CodesN05BA21
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9849
Blood Brain Barrier+0.97
Caco-2 permeable+0.662
P-glycoprotein substrateSubstrate0.6147
P-glycoprotein inhibitor INon-inhibitor0.7404
P-glycoprotein inhibitor IINon-inhibitor0.7762
Renal organic cation transporterNon-inhibitor0.5527
CYP450 2C9 substrateNon-substrate0.7485
CYP450 2D6 substrateNon-substrate0.8558
CYP450 3A4 substrateSubstrate0.7356
CYP450 1A2 substrateInhibitor0.8341
CYP450 2C9 inhibitorNon-inhibitor0.5206
CYP450 2D6 inhibitorNon-inhibitor0.8462
CYP450 2C19 inhibitorInhibitor0.6555
CYP450 3A4 inhibitorNon-inhibitor0.5194
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7292
Ames testNon AMES toxic0.7848
CarcinogenicityNon-carcinogens0.7554
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3701 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9974
hERG inhibition (predictor II)Non-inhibitor0.8359
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point105-106Nakanishi, M., Araki, K.,Tahara, T. and Shiroki, M.; US. Patent 3,849,405; November 19, 1974; assigned to Yoshitomi Pharmaceutical Industries, Ltd.
logP3.18MARUYAMA,T ET AL. (1992)
Predicted Properties
PropertyValueSource
Water Solubility0.00537 mg/mLALOGPS
logP3.58ALOGPS
logP4.11ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)2.39ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.67 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity85.66 m3·mol-1ChemAxon
Polarizability33.01 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-014u-3494000000-432038f1e527960b02fcView in MoNA
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as thienodiazepines. These are heteropolycyclic containing a thiophene ring fused to a diazepine ring. Thiophene is 5-membered ring consisting of four carbon and one sulfur atoms. Diazepine is a 7-membered ring consisting of five carbon and two nitrogen atoms.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassThienodiazepines
Sub ClassNot Available
Direct ParentThienodiazepines
Alternative Parents
Substituents
  • Thieno-para-diazepine
  • 2,3,5-trisubstituted thiophene
  • Halobenzene
  • Chlorobenzene
  • Para-diazepine
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • Thiophene
  • 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 DescriptorsNot Available

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. Baburin I, Khom S, Timin E, Hohaus A, Sieghart W, Hering S: Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits. Br J Pharmacol. 2008 Oct;155(3):424-33. doi: 10.1038/bjp.2008.271. Epub 2008 Jul 7. [PubMed:18604239 ]
  2. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Baburin I, Khom S, Timin E, Hohaus A, Sieghart W, Hering S: Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits. Br J Pharmacol. 2008 Oct;155(3):424-33. doi: 10.1038/bjp.2008.271. Epub 2008 Jul 7. [PubMed:18604239 ]
  2. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Baburin I, Khom S, Timin E, Hohaus A, Sieghart W, Hering S: Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits. Br J Pharmacol. 2008 Oct;155(3):424-33. doi: 10.1038/bjp.2008.271. Epub 2008 Jul 7. [PubMed:18604239 ]
  2. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
  3. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Baburin I, Khom S, Timin E, Hohaus A, Sieghart W, Hering S: Estimating the efficiency of benzodiazepines on GABA(A) receptors comprising gamma1 or gamma2 subunits. Br J Pharmacol. 2008 Oct;155(3):424-33. doi: 10.1038/bjp.2008.271. Epub 2008 Jul 7. [PubMed:18604239 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]
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. Mandrioli R, Mercolini L, Raggi MA: Benzodiazepine metabolism: an analytical perspective. Curr Drug Metab. 2008 Oct;9(8):827-44. [PubMed:18855614 ]

Enzymes

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. 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.
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:
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
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. 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 ]
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Drug created on July 31, 2007 07:10 / Updated on August 17, 2016 12:23