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Record Information
Version2.0
Creation Date2009-07-21 20:28:39 UTC
Update Date2014-12-24 20:25:56 UTC
Accession NumberT3D3023
Identification
Common NameEstazolam
ClassSmall Molecule
DescriptionEstazolam is only found in individuals that have used or taken this drug. It is 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] Benzodiazepines 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.
Compound Type
  • Anti-Anxiety Agent
  • Anticonvulsant
  • Drug
  • GABA Modulator
  • Metabolite
  • Organic Compound
  • Organochloride
  • Synthetic Compound
Chemical Structure
Thumb
Synonyms
Synonym
8-chloro-6-phenyl-4H-s-triazolo(4,3-a)(1,4)benzodiazepine
Esilgan
Estazolamum
Eurodin
Nuctalon
ProSom
Chemical FormulaC16H11ClN4
Average Molecular Mass294.738 g/mol
Monoisotopic Mass294.067 g/mol
CAS Registry Number29975-16-4
IUPAC Name12-chloro-9-phenyl-2,4,5,8-tetraazatricyclo[8.4.0.0²,⁶]tetradeca-1(10),3,5,8,11,13-hexaene
Traditional Nameestazolam
SMILESClC1=CC2=C(C=C1)N1C=NN=C1CN=C2C1=CC=CC=C1
InChI IdentifierInChI=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
InChI KeyInChIKey=CDCHDCWJMGXXRH-UHFFFAOYSA-N
Chemical Taxonomy
Description belongs to the class of organic compounds known as 1,2,4-triazolo[4,3-a][1,4]benzodiazepines. These are aromatic compounds containing a 1,4-benzodiazepine fused to and sharing a nitrogen atom with a 1,2,4-triazole ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzodiazepines
Sub Class1,4-benzodiazepines
Direct Parent1,2,4-triazolo[4,3-a][1,4]benzodiazepines
Alternative Parents
Substituents
  • 1,2,4-triazolo[4,3-a][1,4]benzodiazepine
  • Aryl chloride
  • Aryl halide
  • Monocyclic benzene moiety
  • Benzenoid
  • Azole
  • 1,2,4-triazole
  • Heteroaromatic compound
  • Ketimine
  • Propargyl-type 1,3-dipolar organic compound
  • Organic 1,3-dipolar compound
  • Azacycle
  • Organopnictogen compound
  • Organic nitrogen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Imine
  • Hydrocarbon derivative
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Biological Properties
StatusDetected and Not Quantified
OriginExogenous
Cellular Locations
  • Membrane
Biofluid LocationsNot Available
Tissue Locations
  • Kidney
  • Liver
PathwaysNot Available
Applications
Biological Roles
Chemical RolesNot Available
Physical Properties
StateSolid
AppearanceWhite powder.
Experimental Properties
PropertyValue
Melting Point228-229°C
Boiling PointNot Available
SolubilityPractically insoluble (1.5 mg/L)
LogP4.7
Predicted Properties
PropertyValueSource
Water Solubility0.042 g/LALOGPS
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 ŲChemAxon
Rotatable Bond Count1ChemAxon
Refractivity94.44 m³·mol⁻¹ChemAxon
Polarizability29.83 ųChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Spectra
Spectrum TypeDescriptionSplash KeyView
Predicted GC-MSPredicted GC-MS Spectrum - GC-MS (Non-derivatized) - 70eV, Positivesplash10-016r-2190000000-7bceaaf0dfe0270e210aJSpectraViewer
Predicted GC-MSPredicted GC-MS Spectrum - GC-MS (Non-derivatized) - 70eV, PositiveNot AvailableJSpectraViewer
Predicted GC-MSPredicted GC-MS Spectrum - GC-MS (Non-derivatized) - 70eV, PositiveNot AvailableJSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Positivesplash10-0002-0090000000-8b0f7d04b982deb5a038JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Positivesplash10-0002-0090000000-6608de192721b2ce8c75JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Positivesplash10-03xu-8690000000-2b0a33869a0469e8d7b5JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Negativesplash10-0006-0090000000-3bf04c7178bea5e8dea2JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Negativesplash10-0006-0090000000-4b4a11f4e7a928221cffJSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Negativesplash10-0a5c-1090000000-7609bb7b371102913ae0JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Positivesplash10-0002-0090000000-7f5d232a357b1b41cae8JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Positivesplash10-0002-0090000000-7f5d232a357b1b41cae8JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Positivesplash10-014j-0090000000-b88d0c4f35949ad6a7abJSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, Negativesplash10-0006-0090000000-1901824a83af80ea7083JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, Negativesplash10-0006-0090000000-1901824a83af80ea7083JSpectraViewer
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, Negativesplash10-0006-0090000000-f5fb876690ac80360a52JSpectraViewer
MSMass Spectrum (Electron Ionization)splash10-0a4u-4590000000-dbd088d66293b3b539c3JSpectraViewer | MoNA
Toxicity Profile
Route of ExposureTablets 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.
Mechanism of ToxicityBenzodiazepines 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.
MetabolismExtensively 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). Route of Elimination: Estazolam 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 Life: The range of estimates for the mean elimination half-life of estazolam varies from 10 to 24 hours.
Toxicity ValuesLD50: 740 mg/kg (oral, male mice) (4) LD50: 3200 mg/kg (oral, rat) (4) LD50 300 mg/kg (oral, rabbit) (4)
Lethal DoseNot Available
Carcinogenicity (IARC Classification)3, not classifiable as to its carcinogenicity to humans. (6)
Uses/SourcesFor the short-term management of insomnia characterized by difficulty in falling asleep, frequent nocturnal awakenings, and/or early morning awakenings.
Minimum Risk LevelNot Available
Health EffectsMay cause a potentially dangerous rash that may develop into Stevens Johnson syndrome, an extremely rare but potentially fatal skin disease.
SymptomsSymptoms of overdose include confusion, depressed breathing, drowsiness and eventually coma, lack of coordination, and slurred speech.
TreatmentGastric evacuation, either by the induction of emesis, lavage, or both, should be performed immediately. Maintenance of adequate ventilation is essential. General supportive care, including frequent monitoring of the vital signs and close observation of the patient, is indicated. Fluids should be administered intravenously to maintain blood pressure and encourage diuresis. The value of dialysis in treatment of benzodiazepine overdose has not been determined. The physician may wish to consider contacting a Poison Control Center for up-to-date information on the management of hypnotic drug product overdose. Flumazenil, a specific benzodiazepine receptor antagonist, is indicated for the complete or partial reversal of the sedative effects of benzodiazepines and may be used in situations when an overdose with a benzodiazepine is known or suspected. (5)
Normal Concentrations
Not Available
Abnormal Concentrations
Not Available
DrugBank IDDB01215
HMDB IDHMDB15346
PubChem Compound ID3261
ChEMBL IDCHEMBL1201169
ChemSpider ID3146
KEGG IDNot Available
UniProt IDNot Available
OMIM ID
ChEBI ID4858
BioCyc IDNot Available
CTD IDNot Available
Stitch IDEstazolam
PDB IDNot Available
ACToR IDNot Available
Wikipedia LinkEstazolam
References
Synthesis Reference

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

MSDST3D3023.pdf
General References
  1. 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. [3089825 ]
  2. 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. [11995921 ]
  3. Watanabe S, Ohta H, Sakurai Y, Takao K, Ueki S: [Electroencephalographic effects of 450191-S and its metabolites in rabbits with chronic electrode implants]. Nihon Yakurigaku Zasshi. 1986 Jul;88(1):19-32. [3758874 ]
  4. Medicine Complete. Estazolam (3702) [Link]
  5. RxList: The Internet Drug Index (2009). [Link]
  6. International Agency for Research on Cancer (2014). IARC Monographs on the Evaluation of Carcinogenic Risks to Humans. [Link]
Gene Regulation
Up-Regulated GenesNot Available
Down-Regulated GenesNot Available

Targets

General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
  4. 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. [17016423 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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 similarity).
Gene Name:
GABRB1
Uniprot ID:
P18505
Molecular Weight:
54234.085 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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 modulatory agents such as pregnanolone.
Gene Name:
GABRP
Uniprot ID:
O00591
Molecular Weight:
50639.735 Da
References
  1. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
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. Braestrup C, Squires RF: Pharmacological characterization of benzodiazepine receptors in the brain. Eur J Pharmacol. 1978 Apr 1;48(3):263-70. [639854 ]
  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. [2889803 ]
  3. Iorio LC, Barnett A, Billard W: Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Life Sci. 1984 Jul 2;35(1):105-13. [6738302 ]
  4. Wamsley JK, Golden JS, Yamamura HI, Barnett A: Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Pharmacol Biochem Behav. 1985 Dec;23(6):973-8. [2867566 ]
General Function:
Cholesterol binding
Specific Function:
Can bind protoporphyrin IX and may play a role in the transport of porphyrins and heme (By similarity). Promotes the transport of cholesterol across mitochondrial membranes and may play a role in lipid metabolism (PubMed:24814875), but its precise physiological role is controversial. It is apparently not required for steroid hormone biosynthesis. Was initially identified as peripheral-type benzodiazepine receptor; can also bind isoquinoline carboxamides (PubMed:1847678).
Gene Name:
TSPO
Uniprot ID:
P30536
Molecular Weight:
18827.81 Da
References
  1. Taketani S, Kohno H, Okuda M, Furukawa T, Tokunaga R: Induction of peripheral-type benzodiazepine receptors during differentiation of mouse erythroleukemia cells. A possible involvement of these receptors in heme biosynthesis. J Biol Chem. 1994 Mar 11;269(10):7527-31. [8125973 ]
  2. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
  3. 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. [17016423 ]
18. GABA-A receptor (anion channel) (Protein Group)
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
Included Proteins:
P14867 , P47869 , P34903 , P48169 , P31644 , Q16445 , P18505 , P47870 , P28472 , O14764 , P78334 , Q8N1C3 , P18507 , Q99928 , O00591 , Q9UN88