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