Identification

Name
Quazepam
Accession Number
DB01589
Type
Small Molecule
Groups
Approved, Illicit
Description

Quazepam is a drug which is a benzodiazepine derivative. It induces impairment of motor function and has hypnotic properties. Quazepam is used to treat insomnia.

Structure
Thumb
Synonyms
  • Quazepamum
External IDs
SCH 16134 / SCH-16134
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DoralTablet15 mg/1OralPhysicians Total Care, Inc.1994-03-022002-06-30Us
DoralTablet15 mg/1OralGalt Pharmaceuticals Llc2017-07-19Not applicableUs
DoralTablet15 mg/1OralNuro Pharma, Inc.1985-12-272014-12-18Us
DoralTablet15 mg/1OralQuestcor Pharmaceuticals, Inc.1985-12-272013-06-20Us
QuazepamTablet15 mg/1OralA S Medication Solutions2013-08-08Not applicableUs
QuazepamTablet15 mg/1OralLake Erie Medical Dba Quality Care Produts Llc2013-08-082015-08-24Us
QuazepamTablet15 mg/1OralKLE 2, Inc.2013-08-082015-10-30Us
QuazepamTablet15 mg/1OralUnit Dose Services2013-08-082015-10-30Us
QuazepamTablet15 mg/1OralThompson Medical Solutions Llc2016-04-122018-05-29Us
QuazepamTablet15 mg/1OralA S Medication Solutions2013-08-08Not applicableUs
International/Other Brands
Doral / Dormalin
Categories
UNII
JF8V0828ZI
CAS number
36735-22-5
Weight
Average: 386.794
Monoisotopic: 386.026759579
Chemical Formula
C17H11ClF4N2S
InChI Key
IKMPWMZBZSAONZ-UHFFFAOYSA-N
InChI
InChI=1S/C17H11ClF4N2S/c18-10-5-6-14-12(7-10)16(11-3-1-2-4-13(11)19)23-8-15(25)24(14)9-17(20,21)22/h1-7H,8-9H2
IUPAC Name
7-chloro-5-(2-fluorophenyl)-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-1,4-benzodiazepine-2-thione
SMILES
FC1=CC=CC=C1C1=NCC(=S)N(CC(F)(F)F)C2=C1C=C(Cl)C=C2

Pharmacology

Indication

Used to treat insomnia.

Associated Conditions
Pharmacodynamics

Quazepam is a benzodiazepine derivative. The main pharmacological action of quazepam is the enhancement of the neurotransmitter, GABA at the GABAA receptor.

Mechanism of action

Benzodiazepines bind nonspecifically to benzodiazepine receptors, which 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.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit alpha-5
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit gamma-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit beta-3
potentiator
Human
AGamma-aminobutyric acid receptor subunit delta
potentiator
Human
AGamma-aminobutyric acid receptor subunit epsilon
potentiator
Human
AGamma-aminobutyric acid receptor subunit pi
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-1
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-2
potentiator
Human
AGamma-aminobutyric acid receptor subunit rho-3
potentiator
Human
AGABA-A receptor (anion channel)
positive allosteric modulator
Human
Absorption

Bioavailability is 29-35% following oral administration.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism

Hepatic.

Route of elimination
Not Available
Half life

39 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Quazepam.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Quazepam.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Quazepam is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthineThe therapeutic efficacy of Quazepam can be decreased when used in combination with 3-isobutyl-1-methyl-7H-xanthine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when 3,4-Methylenedioxyamphetamine is combined with Quazepam.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Quazepam.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Quazepam.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Quazepam.
4-MethoxyamphetamineThe risk or severity of adverse effects can be increased when 4-Methoxyamphetamine is combined with Quazepam.
5-androstenedioneThe metabolism of Quazepam can be decreased when combined with 5-androstenedione.
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB0015528
KEGG Drug
D00457
KEGG Compound
C07336
PubChem Compound
4999
PubChem Substance
46505952
ChemSpider
4825
ChEBI
8694
ChEMBL
CHEMBL1200472
Therapeutic Targets Database
DAP000690
PharmGKB
PA164744373
Drugs.com
Drugs.com Drug Page
Wikipedia
Quazepam
ATC Codes
N05CD10 — Quazepam

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Physicians Total Care Inc.
  • Questcor
Dosage forms
FormRouteStrength
TabletOral15 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7608616No2008-06-032028-06-03Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)137.5-139 °CPhysProp
logP4.03SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.00231 mg/mLALOGPS
logP4.76ALOGPS
logP5.06ChemAxon
logS-5.2ALOGPS
pKa (Strongest Acidic)18.93ChemAxon
pKa (Strongest Basic)2.59ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area15.6 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity93.47 m3·mol-1ChemAxon
Polarizability33.99 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9385
Blood Brain Barrier+0.9789
Caco-2 permeable+0.5748
P-glycoprotein substrateSubstrate0.5341
P-glycoprotein inhibitor IInhibitor0.9324
P-glycoprotein inhibitor IIInhibitor0.8253
Renal organic cation transporterInhibitor0.6883
CYP450 2C9 substrateNon-substrate0.8255
CYP450 2D6 substrateNon-substrate0.8135
CYP450 3A4 substrateSubstrate0.5133
CYP450 1A2 substrateInhibitor0.7023
CYP450 2C9 inhibitorInhibitor0.5757
CYP450 2D6 inhibitorNon-inhibitor0.6337
CYP450 2C19 inhibitorInhibitor0.688
CYP450 3A4 inhibitorInhibitor0.7937
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9484
Ames testNon AMES toxic0.6683
CarcinogenicityNon-carcinogens0.7273
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9195 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.978
hERG inhibition (predictor II)Inhibitor0.6396
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-05aa-3988000000-ca1cf29da979ef46dd6c
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzodiazepines
Sub Class
1,4-benzodiazepines
Direct Parent
1,4-benzodiazepines
Alternative Parents
Fluorobenzenes / Aryl fluorides / Aryl chlorides / Thiolactams / Ketimines / Propargyl-type 1,3-dipolar organic compounds / Azacyclic compounds / Thiocarbonyl compounds / Organopnictogen compounds / Organofluorides
show 3 more
Substituents
1,4-benzodiazepine / Fluorobenzene / Halobenzene / Aryl chloride / Aryl fluoride / Aryl halide / Monocyclic benzene moiety / Benzenoid / Thiolactam / Ketimine
show 16 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
benzodiazepine (CHEBI:8694)

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...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  4. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-2
Molecular Weight
51325.85 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-3
Molecular Weight
55164.055 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-5
Molecular Weight
52145.645 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-1
Molecular Weight
53594.49 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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...
Gene Name
GABRG2
Uniprot ID
P18507
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-2
Molecular Weight
54161.78 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit gamma-3
Molecular Weight
54288.16 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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...
Gene Name
GABRB1
Uniprot ID
P18505
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-1
Molecular Weight
54234.085 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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...
Gene Name
GABRB3
Uniprot ID
P28472
Uniprot Name
Gamma-aminobutyric acid receptor subunit beta-3
Molecular Weight
54115.04 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit delta
Molecular Weight
50707.835 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit epsilon
Molecular Weight
57971.175 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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 ute...
Gene Name
GABRP
Uniprot ID
O00591
Uniprot Name
Gamma-aminobutyric acid receptor subunit pi
Molecular Weight
50639.735 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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...
Gene Name
GABRR1
Uniprot ID
P24046
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-1
Molecular Weight
55882.91 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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...
Gene Name
GABRR2
Uniprot ID
P28476
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-2
Molecular Weight
54150.41 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]
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
Uniprot Name
Gamma-aminobutyric acid receptor subunit rho-3
Molecular Weight
54271.1 Da
References
  1. Meldrum BS, Chapman AG: Benzodiazepine receptors and their relationship to the treatment of epilepsy. Epilepsia. 1986;27 Suppl 1:S3-13. [PubMed:3017690]
  2. Billard W, Crosby G, Iorio L, Chipkin R, Barnett A: Selective affinity of the benzodiazepines quazepam and 2-oxo-quazepam for BZ1 binding site and demonstration of 3H-2-oxo-quazepam as a BZ1 selective radioligand. Life Sci. 1988;42(2):179-87. [PubMed:2892106]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Sugimoto K, Araki N, Ohmori M, Harada K, Cui Y, Tsuruoka S, Kawaguchi A, Fujimura A: Interaction between grapefruit juice and hypnotic drugs: comparison of triazolam and quazepam. Eur J Clin Pharmacol. 2006 Mar;62(3):209-15. doi: 10.1007/s00228-005-0071-1. Epub 2006 Jan 17. [PubMed:16416305]
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
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 un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Quazepam FDA Label [File]

Drug created on August 29, 2007 09:30 / Updated on November 02, 2018 05:03