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Identification
NameHalazepam
Accession NumberDB00801  (APRD01009)
TypeSmall Molecule
GroupsApproved, Illicit, Withdrawn
DescriptionHalazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a trifluoromethyl derivative of nordazepam. While its structure may be similar to chlordiazepoxide and diazepam, it has both less toxicity and less tendency to cause paradoxical hostility and aggression than either of them. Halazepam is no longer marketed in the United States, and was withdrawn by Schering-Plough due to poor sales. [Wikipedia]
Structure
Thumb
Synonyms
Halazepam
Halazépam
Halazepam
Halazepamum
Paxipam
External Identifiers
  • Sch 12041
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AlaprylMenarini
PacinoneSchering-Plough
PaxipamSchering-Plough
Brand mixturesNot Available
SaltsNot Available
Categories
UNII320YC168LF
CAS number23092-17-3
WeightAverage: 352.738
Monoisotopic: 352.059025338
Chemical FormulaC17H12ClF3N2O
InChI KeyInChIKey=WYCLKVQLVUQKNZ-UHFFFAOYSA-N
InChI
InChI=1S/C17H12ClF3N2O/c18-12-6-7-14-13(8-12)16(11-4-2-1-3-5-11)22-9-15(24)23(14)10-17(19,20)21/h1-8H,9-10H2
IUPAC Name
7-chloro-5-phenyl-1-(2,2,2-trifluoroethyl)-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
FC(F)(F)CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=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
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl chloride
  • 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
  • Organofluoride
  • Organochloride
  • Organohalogen compound
  • Imine
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationUsed to relieve anxiety, nervousness, and tension associated with anxiety disorders.
PharmacodynamicsNot Available
Mechanism of actionBenzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, 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 of GABA by increasing GABA affinity for the GABA receptor. Binding of GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half lifeNot Available
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+0.9952
Blood Brain Barrier+0.9966
Caco-2 permeable+0.6558
P-glycoprotein substrateSubstrate0.6489
P-glycoprotein inhibitor IInhibitor0.739
P-glycoprotein inhibitor IIInhibitor0.6548
Renal organic cation transporterInhibitor0.5819
CYP450 2C9 substrateNon-substrate0.7819
CYP450 2D6 substrateNon-substrate0.8422
CYP450 3A4 substrateSubstrate0.7404
CYP450 1A2 substrateInhibitor0.776
CYP450 2C9 inhibitorInhibitor0.5458
CYP450 2D6 inhibitorNon-inhibitor0.809
CYP450 2C19 inhibitorInhibitor0.7949
CYP450 3A4 inhibitorInhibitor0.5085
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7781
Ames testNon AMES toxic0.8369
CarcinogenicityNon-carcinogens0.7657
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.7143 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9836
hERG inhibition (predictor II)Inhibitor0.5729
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Schering corp sub schering plough corp
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point165 °CPhysProp
logP3.97SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0017 mg/mLALOGPS
logP3.52ALOGPS
logP4.03ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)18.88ChemAxon
pKa (Strongest Basic)2.33ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.67 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity85.26 m3·mol-1ChemAxon
Polarizability31.82 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)splash10-0fmi-3539000000-76854e3f82279b906a7fView in MoNA
References
Synthesis Reference

U.S. Patents 3,429,874 and 3,641,147.

General References
  1. Fann WE, Pitts WM, Wheless JC: Pharmacology, efficacy, and adverse effects of halazepam, a new benzodiazepine. Pharmacotherapy. 1982 Mar-Apr;2(2):72-9. [PubMed:6152591 ]
External Links
ATC CodesN05BA13
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
7-NitroindazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with 7-Nitroindazole.
AcepromazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Aceprometazine.
adipiplonThe risk or severity of adverse effects can be increased when Halazepam is combined with adipiplon.
AgomelatineThe risk or severity of adverse effects can be increased when Halazepam is combined with Agomelatine.
AlfaxaloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Alfaxalone.
AlfentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Alfentanil.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Halazepam is combined with Alphacetylmethadol.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Halazepam.
AmisulprideThe risk or severity of adverse effects can be increased when Halazepam is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Amitriptyline.
AmobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Amobarbital.
AmoxapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Halazepam is combined with Amperozide.
AripiprazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Aripiprazole.
ArticaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Articaine.
AsenapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Asenapine.
AzaperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Azaperone.
AzelastineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
AzelastineThe risk or severity of adverse effects can be increased when Azelastine is combined with Halazepam.
BaclofenThe risk or severity of adverse effects can be increased when Halazepam is combined with Baclofen.
BarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Barbital.
BenzocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Benzocaine.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Halazepam is combined with Benzyl alcohol.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
BrimonidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Bromazepam.
BrompheniramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Brompheniramine.
BrotizolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Brotizolam.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Halazepam.
BuprenorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Buprenorphine.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Halazepam.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Halazepam.
ButacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Butacaine.
ButalbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Butalbital.
ButambenThe risk or severity of adverse effects can be increased when Halazepam is combined with Butamben.
ButethalThe risk or severity of adverse effects can be increased when Halazepam is combined with Butethal.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Halazepam.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Halazepam.
CarbinoxamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Carbinoxamine.
CarfentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Carfentanil.
CarisoprodolThe risk or severity of adverse effects can be increased when Halazepam is combined with Carisoprodol.
CetirizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cetirizine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Halazepam is combined with Chloral hydrate.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Halazepam.
ChlormezanoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlormezanone.
ChloroprocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Chloroprocaine.
ChlorphenamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorphenamine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Halazepam.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorprothixene.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorzoxazone.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Halazepam.
CitalopramThe risk or severity of adverse effects can be increased when Halazepam is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Halazepam is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Halazepam is combined with Clobazam.
clomethiazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with clomethiazole.
ClomipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Halazepam.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Halazepam.
CocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cocaine.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Halazepam.
CyclizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyclobenzaprine.
CyproheptadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyproheptadine.
DantroleneThe risk or severity of adverse effects can be increased when Halazepam is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Halazepam.
DapoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dapoxetine.
deramciclaneThe risk or severity of adverse effects can be increased when Halazepam is combined with deramciclane.
DesfluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Desflurane.
DesipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Desloratadine.
DetomidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Detomidine.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dexbrompheniramine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Halazepam.
DextromoramideThe risk or severity of adverse effects can be increased when Halazepam is combined with Dextromoramide.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Halazepam.
DezocineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dezocine.
DiazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Diazepam.
DifenoxinThe risk or severity of adverse effects can be increased when Halazepam is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydrocodeine.
DihydroetorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydroetorphine.
DihydromorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydromorphine.
DimenhydrinateThe risk or severity of adverse effects can be increased when Halazepam is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Diphenhydramine.
DiphenoxylateThe risk or severity of adverse effects can be increased when Halazepam is combined with Diphenoxylate.
DoramectinThe risk or severity of adverse effects can be increased when Halazepam is combined with Doramectin.
DoxepinThe risk or severity of adverse effects can be increased when Halazepam is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
DoxylamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when Halazepam is combined with DPDPE.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Halazepam.
DrotebanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Drotebanol.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Halazepam.
EcgonineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ecgonine.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Halazepam is combined with ECGONINE METHYL ESTER.
EfavirenzThe risk or severity of adverse effects can be increased when Halazepam is combined with Efavirenz.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Halazepam.
EntacaponeThe risk or severity of adverse effects can be increased when Halazepam is combined with Entacapone.
EscitalopramThe risk or severity of adverse effects can be increased when Halazepam is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Estazolam.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Halazepam.
EthanolHalazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Halazepam.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Halazepam.
EthosuximideThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethotoin.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethyl carbamate.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethyl loflazepate.
EthylmorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethylmorphine.
EtidocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etidocaine.
EtifoxineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etifoxine.
EtizolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Etizolam.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Halazepam.
EtoperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etorphine.
EzogabineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Halazepam is combined with Felbamate.
FencamfamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fencamfamine.
FenfluramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Halazepam is combined with Fentanyl.
FexofenadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fexofenadine.
FlibanserinThe risk or severity of adverse effects can be increased when Halazepam is combined with Flibanserin.
FludiazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Fludiazepam.
FlunarizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Flunitrazepam.
FluoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Halazepam is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Halazepam.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Halazepam.
FluspirileneThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluspirilene.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Halazepam is combined with Fospropofol.
GabapentinThe risk or severity of adverse effects can be increased when Halazepam is combined with Gabapentin.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Halazepam is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Halazepam is combined with Gamma Hydroxybutyric Acid.
GlutethimideThe risk or severity of adverse effects can be increased when Halazepam is combined with Glutethimide.
GuanfacineThe risk or severity of adverse effects can be increased when Halazepam is combined with Guanfacine.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Halazepam.
HalothaneThe risk or severity of adverse effects can be increased when Halazepam is combined with Halothane.
HeroinThe risk or severity of adverse effects can be increased when Halazepam is combined with Heroin.
HexobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Hexobarbital.
HydrocodoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Hydrocodone.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Halazepam.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
HydroxyzineThe risk or severity of adverse effects can be increased when Halazepam is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Imipramine.
IndalpineThe risk or severity of adverse effects can be increased when Halazepam is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Halazepam.
KetamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketamine.
KetazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketazolam.
KetobemidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketobemidone.
LamotrigineThe risk or severity of adverse effects can be increased when Halazepam is combined with Lamotrigine.
LevetiracetamThe risk or severity of adverse effects can be increased when Halazepam is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levobupivacaine.
LevocabastineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Halazepam is combined with Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Halazepam is combined with Levomethadyl Acetate.
LevomilnacipranThe risk or severity of adverse effects can be increased when Halazepam is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Levorphanol.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Halazepam.
LithiumThe risk or severity of adverse effects can be increased when Halazepam is combined with Lithium.
LofentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Lofentanil.
LoratadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Halazepam.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Halazepam.
Lu AA21004The risk or severity of adverse effects can be increased when Halazepam is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Halazepam is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Halazepam is combined with Maprotiline.
MeclizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Meclizine.
MedetomidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Medetomidine.
MelatoninThe risk or severity of adverse effects can be increased when Halazepam is combined with Melatonin.
MelperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Melperone.
MepivacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Mepivacaine.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Halazepam.
MesoridazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Mesoridazine.
MetaxaloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Metaxalone.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Halazepam.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Halazepam is combined with Methadyl Acetate.
MethapyrileneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methapyrilene.
MethaqualoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methaqualone.
MethocarbamolThe risk or severity of adverse effects can be increased when Halazepam is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Halazepam.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Methotrimeprazine.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methoxyflurane.
MethsuximideThe risk or severity of adverse effects can be increased when Halazepam is combined with Methsuximide.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Methylphenobarbital.
MetyrosineHalazepam may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Halazepam.
MilnacipranThe risk or severity of adverse effects can be increased when Halazepam is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
MirtazapineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Halazepam.
MolindoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Halazepam.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Halazepam.
NabiloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Nalbuphine.
NitrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Nitrazepam.
Nitrous oxideThe risk or severity of adverse effects can be increased when Halazepam is combined with Nitrous oxide.
NormethadoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Normethadone.
NortriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Nortriptyline.
OlanzapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Olopatadine.
OndansetronThe risk or severity of adverse effects can be increased when Halazepam is combined with Ondansetron.
OpiumThe risk or severity of adverse effects can be increased when Halazepam is combined with Opium.
OrphenadrineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
OrphenadrineThe risk or severity of adverse effects can be increased when Orphenadrine is combined with Halazepam.
OsanetantThe risk or severity of adverse effects can be increased when Halazepam is combined with Osanetant.
OxazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxazepam.
OxprenololThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxprenolol.
OxybuprocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxybuprocaine.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Halazepam.
OxymorphoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxymorphone.
PaliperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Paliperidone.
ParaldehydeHalazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParaldehydeThe risk or severity of adverse effects can be increased when Paraldehyde is combined with Halazepam.
ParoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Halazepam.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Halazepam.
PerampanelThe risk or severity of adverse effects can be increased when Halazepam is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Halazepam is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Perphenazine.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Halazepam.
PhenobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenobarbital.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenoxyethanol.
PhenytoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Halazepam is combined with Pimozide.
PipamperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Pipamperone.
PipotiazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Halazepam is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Halazepam is combined with Pomalidomide.
PramipexoleHalazepam may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Pramocaine.
PrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Prazepam.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Halazepam.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Halazepam.
PrimidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Primidone.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Halazepam.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Halazepam.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Halazepam.
PromethazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Promethazine.
ProparacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Proparacaine.
PropofolThe risk or severity of adverse effects can be increased when Halazepam is combined with Propofol.
PropoxycaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Propoxycaine.
ProtriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Protriptyline.
PSD502The risk or severity of adverse effects can be increased when Halazepam is combined with PSD502.
QuazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Quazepam.
QuetiapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Quetiapine.
RamelteonThe risk or severity of adverse effects can be increased when Halazepam is combined with Ramelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Remifentanil.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Halazepam.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Halazepam.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Halazepam.
RomifidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Romifidine.
RopiniroleHalazepam may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Halazepam.
RotigotineHalazepam may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Halazepam.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Halazepam is combined with S-Ethylisothiourea.
ScopolamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Scopolamine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Halazepam.
SertindoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Halazepam is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Sevoflurane.
Sodium oxybateThe risk or severity of adverse effects can be increased when Halazepam is combined with Sodium oxybate.
StiripentolThe risk or severity of adverse effects can be increased when Halazepam is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Halazepam.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Halazepam.
SuvorexantThe risk or severity of adverse effects can be increased when Halazepam is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Halazepam is combined with Tapentadol.
TasimelteonThe risk or severity of adverse effects can be increased when Halazepam is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Halazepam.
TetrabenazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetrabenazine.
TetracaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetracaine.
TetrodotoxinThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetrodotoxin.
ThalidomideHalazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
ThalidomideThe risk or severity of adverse effects can be increased when Thalidomide is combined with Halazepam.
ThiamylalThe risk or severity of adverse effects can be increased when Halazepam is combined with Thiamylal.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Halazepam.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Halazepam.
ThiothixeneThe risk or severity of adverse effects can be increased when Halazepam is combined with Thiothixene.
TiagabineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tiagabine.
TiletamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tiletamine.
TizanidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tizanidine.
TolcaponeThe risk or severity of adverse effects can be increased when Halazepam is combined with Tolcapone.
TopiramateThe risk or severity of adverse effects can be increased when Halazepam is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Halazepam.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Halazepam.
TrazodoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Triazolam.
TrifluoperazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Halazepam.
TrimipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trimipramine.
TriprolidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Triprolidine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Halazepam.
VigabatrinThe risk or severity of adverse effects can be increased when Halazepam is combined with Vigabatrin.
VilazodoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Xylazine.
YohimbineThe therapeutic efficacy of Halazepam can be decreased when used in combination with Yohimbine.
ZaleplonThe risk or severity of adverse effects can be increased when Halazepam is combined with Zaleplon.
ZiconotideThe risk or severity of adverse effects can be increased when Halazepam is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Halazepam.
ZolazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Zolazepam.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Halazepam.
ZonisamideThe risk or severity of adverse effects can be increased when Halazepam is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Zopiclone.
ZotepineThe risk or severity of adverse effects can be increased when Halazepam is combined with Zotepine.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Halazepam is combined with Zuclopenthixol.
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. 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. 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. [PubMed: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. [PubMed:2867566 ]
  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
Molecular Weight:
51325.85 Da
References
  1. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
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. 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. [PubMed:6738302 ]
  2. 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. [PubMed:2867566 ]
Kind
Protein group
Organism
Human
Pharmacological action
yes
Actions
positive allosteric modulator
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).
Components:
NameUniProt IDDetails
Gamma-aminobutyric acid receptor subunit alpha-1P14867 Details
Gamma-aminobutyric acid receptor subunit alpha-2P47869 Details
Gamma-aminobutyric acid receptor subunit alpha-3P34903 Details
Gamma-aminobutyric acid receptor subunit alpha-4P48169 Details
Gamma-aminobutyric acid receptor subunit alpha-5P31644 Details
Gamma-aminobutyric acid receptor subunit alpha-6Q16445 Details
Gamma-aminobutyric acid receptor subunit beta-1P18505 Details
Gamma-aminobutyric acid receptor subunit beta-2P47870 Details
Gamma-aminobutyric acid receptor subunit beta-3P28472 Details
Gamma-aminobutyric acid receptor subunit deltaO14764 Details
Gamma-aminobutyric acid receptor subunit epsilonP78334 Details
Gamma-aminobutyric acid receptor subunit gamma-1Q8N1C3 Details
Gamma-aminobutyric acid receptor subunit gamma-2P18507 Details
Gamma-aminobutyric acid receptor subunit gamma-3Q99928 Details
Gamma-aminobutyric acid receptor subunit piO00591 Details
Gamma-aminobutyric acid receptor subunit thetaQ9UN88 Details
References
  1. ChEMBL Compound Report Card [Link]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23