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Identification
NameEstazolam
Accession NumberDB01215  (APRD00955)
TypeSmall Molecule
GroupsApproved, Illicit
Description

A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
8-chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepineNot AvailableNot Available
EstazolamumNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Estazolamtablet1 mgoralTeva Pharmaceuticals USA Inc1997-07-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet2 mgoralTeva Pharmaceuticals USA Inc1997-07-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet1 mgoralWatson Laboratories, Inc.1997-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet2 mgoralWatson Laboratories, Inc.1997-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet2 mgoralRebel Distributors Corp1997-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet1 mgoralGolden State Medical Supply, Inc.1997-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estazolamtablet2 mgoralGolden State Medical Supply, Inc.1997-08-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
EsilganTakeda
EurodinTakeda
NuctalonTakeda
ProSomNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
CAS number29975-16-4
WeightAverage: 294.738
Monoisotopic: 294.067224079
Chemical FormulaC16H11ClN4
InChI KeyCDCHDCWJMGXXRH-UHFFFAOYSA-N
InChI
InChI=1S/C16H11ClN4/c17-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)18-9-15-20-19-10-21(14)15/h1-8,10H,9H2
IUPAC Name
12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene
SMILES
ClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as 1,4-benzodiazepines. These are organic compounds containing a benzene ring fused to a 1,4-azepine.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub Class1,4-benzodiazepines
Direct Parent1,4-benzodiazepines
Alternative Parents
Substituents
  • 1,4-benzodiazepine
  • Phenyl-1,3,4-triazole
  • Phenyl-1,2,4-triazole
  • Phenyltriazole
  • Chlorobenzene
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • Heteroaromatic compound
  • 1,2,4-triazole
  • Triazole
  • Azole
  • Ketimine
  • Azacycle
  • Organic 1,3-dipolar compound
  • Propargyl-type 1,3-dipolar organic compound
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.
PharmacodynamicsEstazolam, a triazolobenzodiazepine derivative, is an oral hypnotic agent with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than diazepam or nitrazepam.
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects 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.
AbsorptionTablets have been found to be equivalent in absorption to an orally administered solution of estazolam. In healthy subjects who received up to three times the recommended dose, peak estazolam plasma concentrations occurred within two hours after dosing (range 0.5 to 6.0 hours) and were proportional to the administered dose, suggesting linear pharmacokinetics over the dosage range tested.
Volume of distributionNot Available
Protein binding93% protein bound, independant of concentration.
Metabolism

Extensively metabolized in the liver. In vitro studies with human liver microsomes indicate that the biotransformation of estazolam to the major circulating metabolite 4-hydroxy-estazolam is mediated by cytochrome P450 3A (CYP3A).

SubstrateEnzymesProduct
Estazolam
Not Available
4-hydroxy-estazolamDetails
Route of eliminationEstazolam is extensively metabolized. The elimination of the parent drug takes place via hepatic metabolism of estazolam to hydroxylated and other metabolites that are eliminated largely in the urine both free and conjugated. Less than 5% of a 2 mg dose of estazolam was excreted unchanged in the urine, with only 4% of the dose appearing in the feces. Radiolabel mass balance studies indicate that the main route of excretion is via the kidneys. After 5 days, 87% of the administered radioactivity was excreted in human urine. Less than 4% of the dose was excreted unchanged.
Half lifeThe range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.
ClearanceNot Available
ToxicitySymptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.
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+1.0
Blood Brain Barrier+0.9796
Caco-2 permeable+0.8427
P-glycoprotein substrateNon-substrate0.5939
P-glycoprotein inhibitor INon-inhibitor0.7883
P-glycoprotein inhibitor IIInhibitor0.7786
Renal organic cation transporterInhibitor0.7784
CYP450 2C9 substrateNon-substrate0.8367
CYP450 2D6 substrateNon-substrate0.9081
CYP450 3A4 substrateSubstrate0.674
CYP450 1A2 substrateInhibitor0.8989
CYP450 2C9 substrateInhibitor0.822
CYP450 2D6 substrateNon-inhibitor0.8586
CYP450 2C19 substrateInhibitor0.6571
CYP450 3A4 substrateNon-inhibitor0.6818
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8676
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.7126
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.0584 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9752
hERG inhibition (predictor II)Non-inhibitor0.8944
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg
Tabletoral2 mg
Prices
Unit descriptionCostUnit
Prosom 2 mg tablet1.71USD tablet
Prosom 1 mg tablet1.53USD tablet
Estazolam 2 mg tablet0.96USD tablet
Estazolam 1 mg tablet0.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point228-229Hester, J.B. Jr.; U.S. Patent 3,701,782; October 31, 1972; assigned to The Upjohn Co.
water solubilityPractically insoluble (1.5 mg/L)Not Available
logP4.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0423 mg/mLALOGPS
logP1.72ALOGPS
logP2.09ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)18.4ChemAxon
pKa (Strongest Basic)4.97ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area43.07 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity94.44 m3·mol-1ChemAxon
Polarizability29.83 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraMS
References
Synthesis Reference

Hester, J.B. Jr.; U.S. Patent 3,701,782; October 31, 1972; assigned to The Upjohn Co.

General Reference
  1. Watanabe S, Ohta H, Sakurai Y, Takao K, Ueki S: [Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants] Nippon Yakurigaku Zasshi. 1986 Jul;88(1):19-32. Pubmed
  2. Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. Pubmed
  3. Usami N, Yamamoto T, Shintani S, Ishikura S, Higaki Y, Katagiri Y, Hara A: Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biol Pharm Bull. 2002 Apr;25(4):441-5. Pubmed
External Links
ATC CodesN05CD04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
BuprenorphineCNS Depressants may enhance the CNS depressant effect of Buprenorphine.
ClarithromycinMacrolide Antibiotics may increase the serum concentration of Estazolam.
ClozapineBenzodiazepines may enhance the adverse/toxic effect of CloZAPine.
DoxylamineMay enhance the CNS depressant effect of CNS Depressants.
DronabinolMay enhance the CNS depressant effect of CNS Depressants.
DroperidolMay enhance the CNS depressant effect of CNS Depressants.
FosphenytoinBenzodiazepines may increase the serum concentration of Fosphenytoin. Short-term exposure to benzodiazepines may not present as much risk as chronic therapy.
HydrocodoneCNS Depressants may enhance the CNS depressant effect of Hydrocodone.
HydroxyzineMay enhance the CNS depressant effect of CNS Depressants.
ItraconazoleItraconazole may increase the serum concentration of Estazolam.
LopinavirRitonavir may increase the serum concentration of Estazolam.
Magnesium SulfateMay enhance the CNS depressant effect of CNS Depressants.
MethadoneBenzodiazepines may enhance the CNS depressant effect of Methadone.
MethotrimeprazineCNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants.
MetyrosineCNS Depressants may enhance the sedative effect of Metyrosine.
MirtazapineCNS Depressants may enhance the CNS depressant effect of Mirtazapine.
NabiloneMay enhance the CNS depressant effect of CNS Depressants.
OlanzapineMay enhance the adverse/toxic effect of Benzodiazepines.
OrphenadrineCNS Depressants may enhance the CNS depressant effect of Orphenadrine.
PerampanelMay enhance the CNS depressant effect of CNS Depressants.
PhenytoinBenzodiazepines may increase the serum concentration of Phenytoin. Short-term exposure to benzodiazepines may not present as much risk as chronic therapy.
PramipexoleCNS Depressants may enhance the sedative effect of Pramipexole.
RitonavirRitonavir may increase the serum concentration of Estazolam.
RopiniroleCNS Depressants may enhance the sedative effect of ROPINIRole.
RotigotineCNS Depressants may enhance the sedative effect of Rotigotine.
RufinamideMay enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
SulfisoxazoleMacrolide Antibiotics may increase the serum concentration of Estazolam.
SuvorexantCNS Depressants may enhance the CNS depressant effect of Suvorexant.
TapentadolMay enhance the CNS depressant effect of CNS Depressants.
TeduglutideMay increase the serum concentration of Benzodiazepines.
TelithromycinMacrolide Antibiotics may increase the serum concentration of Estazolam.
ThalidomideCNS Depressants may enhance the CNS depressant effect of Thalidomide.
YohimbineMay diminish the therapeutic effect of Antianxiety Agents.
ZolpidemCNS Depressants may enhance the CNS depressant effect of Zolpidem.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

Targets

1. Gamma-aminobutyric acid receptor subunit alpha-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-1 P14867 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

2. Gamma-aminobutyric acid receptor subunit alpha-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-2 P47869 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

3. Gamma-aminobutyric acid receptor subunit alpha-3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-3 P34903 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

4. Gamma-aminobutyric acid receptor subunit alpha-5

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-5 P31644 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

5. Gamma-aminobutyric acid receptor subunit gamma-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit gamma-1 Q8N1C3 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

6. Gamma-aminobutyric acid receptor subunit gamma-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit gamma-2 P18507 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

7. Gamma-aminobutyric acid receptor subunit gamma-3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit gamma-3 Q99928 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

8. Gamma-aminobutyric acid receptor subunit beta-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit beta-1 P18505 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

9. Gamma-aminobutyric acid receptor subunit beta-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit beta-2 P47870 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

10. Gamma-aminobutyric acid receptor subunit beta-3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit beta-3 P28472 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

11. Gamma-aminobutyric acid receptor subunit delta

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit delta O14764 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

12. Gamma-aminobutyric acid receptor subunit epsilon

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit epsilon P78334 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

13. Gamma-aminobutyric acid receptor subunit pi

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit pi O00591 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

14. Gamma-aminobutyric acid receptor subunit rho-1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit rho-1 P24046 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

15. Gamma-aminobutyric acid receptor subunit rho-2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit rho-2 P28476 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

16. Gamma-aminobutyric acid receptor subunit rho-3

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: potentiator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit rho-3 A8MPY1 Details

References:

  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. Pubmed
  2. Miller LG, Greenblatt DJ, Barnhill JG, Deutsch SI, Shader RI, Paul SM: Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam. J Neurochem. 1987 Nov;49(5):1595-601. Pubmed

17. GABA-A receptor (anion channel)

Kind: protein group

Organism: Human

Pharmacological action: yes

Actions: positive allosteric modulator

Components

Name UniProt ID Details
Gamma-aminobutyric acid receptor subunit alpha-1 P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2 P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3 P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4 P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5 P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6 Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1 P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2 P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3 P28472 Details
Gamma-aminobutyric acid receptor subunit delta O14764 Details
Gamma-aminobutyric acid receptor subunit epsilon P78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1 Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2 P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3 Q99928 Details
Gamma-aminobutyric acid receptor subunit pi O00591 Details
Gamma-aminobutyric acid receptor subunit theta Q9UN88 Details

References:

  1. ChEMBL Compound Report Card (Accessed December 2013)

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

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. Epub 2009 Nov 24. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on April 17, 2014 11:42