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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GroupsApproved, Illicit, Withdrawn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 Halazepam is no longer marketed in the United States, and was withdrawn by Schering-Plough due to poor sales.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 KeyWYCLKVQLVUQKNZ-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
Pharmacology
IndicationUsed to relieve anxiety, nervousness, and tension associated with anxiety disorders.
Structured Indications Not Available
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Gamma-aminobutyric acid receptor subunit alpha-1Proteinyes
potentiator
HumanP14867 details
Gamma-aminobutyric acid receptor subunit alpha-2Proteinyes
potentiator
HumanP47869 details
Gamma-aminobutyric acid receptor subunit alpha-3Proteinyes
potentiator
HumanP34903 details
Gamma-aminobutyric acid receptor subunit alpha-5Proteinyes
potentiator
HumanP31644 details
Gamma-aminobutyric acid receptor subunit gamma-1Proteinyes
potentiator
HumanQ8N1C3 details
Gamma-aminobutyric acid receptor subunit gamma-2Proteinyes
potentiator
HumanP18507 details
Gamma-aminobutyric acid receptor subunit gamma-3Proteinyes
potentiator
HumanQ99928 details
Gamma-aminobutyric acid receptor subunit beta-1Proteinyes
potentiator
HumanP18505 details
Gamma-aminobutyric acid receptor subunit beta-2Proteinyes
potentiator
HumanP47870 details
Gamma-aminobutyric acid receptor subunit beta-3Proteinyes
potentiator
HumanP28472 details
Gamma-aminobutyric acid receptor subunit deltaProteinyes
potentiator
HumanO14764 details
Gamma-aminobutyric acid receptor subunit epsilonProteinyes
potentiator
HumanP78334 details
Gamma-aminobutyric acid receptor subunit piProteinyes
potentiator
HumanO00591 details
Gamma-aminobutyric acid receptor subunit rho-1Proteinyes
potentiator
HumanP24046 details
Gamma-aminobutyric acid receptor subunit rho-2Proteinyes
potentiator
HumanP28476 details
Gamma-aminobutyric acid receptor subunit rho-3Proteinyes
potentiator
HumanA8MPY1 details
GABA-A receptor (anion channel)Protein groupyes
positive allosteric modulator
Humannot applicabledetails
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
Interactions
Drug Interactions
DrugInteractionDrug group
1,1,1,2 TetrafluoroethaneThe risk or severity of adverse effects can be increased when Halazepam is combined with 1,1,1,2 Tetrafluoroethane.Investigational
7-NitroindazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with 7-Nitroindazole.Experimental
AcepromazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Acepromazine.Approved, Vet Approved
AceprometazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Aceprometazine.Approved
adipiplonThe risk or severity of adverse effects can be increased when Halazepam is combined with adipiplon.Investigational
AgomelatineThe risk or severity of adverse effects can be increased when Halazepam is combined with Agomelatine.Approved, Investigational
AlfaxaloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Alfaxalone.Vet Approved
AlfentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Halazepam is combined with Alphacetylmethadol.Experimental, Illicit
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Halazepam.Approved, Illicit, Investigational
AmisulprideThe risk or severity of adverse effects can be increased when Halazepam is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Amitriptyline.Approved
AmobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Amobarbital.Approved, Illicit
AmoxapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Amoxapine.Approved
AmperozideThe risk or severity of adverse effects can be increased when Halazepam is combined with Amperozide.Experimental
AripiprazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Aripiprazole.Approved, Investigational
ArticaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Articaine.Approved
AsenapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Asenapine.Approved
AzaperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Azaperone.Vet Approved
AzelastineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Halazepam is combined with Azelastine.Approved
BaclofenThe risk or severity of adverse effects can be increased when Halazepam is combined with Baclofen.Approved
BarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Barbital.Illicit
BenperidolThe risk or severity of adverse effects can be increased when Halazepam is combined with Benperidol.Investigational
BenzocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Benzocaine.Approved
Benzyl alcoholThe risk or severity of adverse effects can be increased when Halazepam is combined with Benzyl alcohol.Approved
BrexpiprazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Brexpiprazole.Approved
BrimonidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Brimonidine.Approved
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved
BromazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Bromazepam.Approved, Illicit
BrompheniramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Brompheniramine.Approved
BrotizolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Brotizolam.Approved, Withdrawn
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Halazepam.Approved, Investigational
BuprenorphineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Halazepam.Approved, Investigational
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Halazepam.Approved, Illicit
ButacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Butacaine.Vet Approved
ButalbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Butalbital.Approved, Illicit
ButambenThe risk or severity of adverse effects can be increased when Halazepam is combined with Butamben.Approved
ButethalThe risk or severity of adverse effects can be increased when Halazepam is combined with Butethal.Approved, Illicit
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Halazepam.Approved, Illicit, Vet Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Halazepam.Approved, Investigational
CarbinoxamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Carbinoxamine.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Carfentanil.Illicit, Vet Approved
CarisoprodolThe risk or severity of adverse effects can be increased when Halazepam is combined with Carisoprodol.Approved
CetirizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cetirizine.Approved
Chloral hydrateThe risk or severity of adverse effects can be increased when Halazepam is combined with Chloral hydrate.Approved, Illicit, Vet Approved
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Halazepam.Approved, Illicit
ChlormezanoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlormezanone.Approved, Withdrawn
ChloroprocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Chloroprocaine.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorphenamine.Approved
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Halazepam.Approved, Vet Approved
ChlorprothixeneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorprothixene.Approved, Withdrawn
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Chlorzoxazone.Approved
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Halazepam.Approved, Vet Approved
CitalopramThe risk or severity of adverse effects can be increased when Halazepam is combined with Citalopram.Approved
ClemastineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clemastine.Approved
ClidiniumThe risk or severity of adverse effects can be increased when Halazepam is combined with Clidinium.Approved
ClobazamThe risk or severity of adverse effects can be increased when Halazepam is combined with Clobazam.Approved, Illicit
clomethiazoleThe risk or severity of adverse effects can be increased when Halazepam is combined with clomethiazole.Investigational
ClomipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clomipramine.Approved, Vet Approved
ClonazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Clonazepam.Approved, Illicit
ClonidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Clonidine.Approved
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Halazepam.Approved, Illicit
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Halazepam.Approved
CocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cocaine.Approved, Illicit
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Halazepam.Approved, Illicit
CyclizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyclizine.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyclobenzaprine.Approved
CyproheptadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Cyproheptadine.Approved
DantroleneThe risk or severity of adverse effects can be increased when Halazepam is combined with Dantrolene.Approved
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Halazepam.Approved
DapoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dapoxetine.Investigational
deramciclaneThe risk or severity of adverse effects can be increased when Halazepam is combined with deramciclane.Investigational
DesfluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Desflurane.Approved
DesipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Desipramine.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Desloratadine.Approved, Investigational
DesvenlafaxineThe risk or severity of adverse effects can be increased when Halazepam is combined with Desvenlafaxine.Approved
DetomidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Detomidine.Vet Approved
DexbrompheniramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dexbrompheniramine.Approved
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Halazepam.Approved, Vet Approved
DextromoramideThe risk or severity of adverse effects can be increased when Halazepam is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Halazepam.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dezocine.Approved
DiazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Diazepam.Approved, Illicit, Vet Approved
DifenoxinThe risk or severity of adverse effects can be increased when Halazepam is combined with Difenoxin.Approved, Illicit
DihydrocodeineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Dihydromorphine.Experimental, Illicit
DimenhydrinateThe risk or severity of adverse effects can be increased when Halazepam is combined with Dimenhydrinate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Diphenhydramine.Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Halazepam is combined with Diphenoxylate.Approved, Illicit
DoramectinThe risk or severity of adverse effects can be increased when Halazepam is combined with Doramectin.Vet Approved
DoxepinThe risk or severity of adverse effects can be increased when Halazepam is combined with Doxepin.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Halazepam is combined with DPDPE.Investigational
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Illicit
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Vet Approved
DrotebanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Drotebanol.Experimental, Illicit
DuloxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Duloxetine.Approved
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Halazepam.Approved
EcgonineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ecgonine.Experimental, Illicit
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Halazepam is combined with ECGONINE METHYL ESTER.Experimental
EcopipamThe risk or severity of adverse effects can be increased when Halazepam is combined with Ecopipam.Investigational
EfavirenzThe risk or severity of adverse effects can be increased when Halazepam is combined with Efavirenz.Approved, Investigational
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Halazepam.Approved, Vet Approved
EntacaponeThe risk or severity of adverse effects can be increased when Halazepam is combined with Entacapone.Approved, Investigational
EscitalopramThe risk or severity of adverse effects can be increased when Halazepam is combined with Escitalopram.Approved, Investigational
EstazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Estazolam.Approved, Illicit
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Halazepam.Approved
EthanolHalazepam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Halazepam.Approved, Illicit, Withdrawn
EthosuximideThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethosuximide.Approved
EthotoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethotoin.Approved
Ethyl carbamateThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethyl carbamate.Withdrawn
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethyl loflazepate.Approved, Illicit
EthylmorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ethylmorphine.Approved, Illicit
EtidocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etidocaine.Approved
EtifoxineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etifoxine.Withdrawn
EtizolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Etizolam.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Halazepam.Approved
EtoperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Etoperidone.Approved
EtorphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Etorphine.Illicit, Vet Approved
EzogabineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ezogabine.Approved
FelbamateThe risk or severity of adverse effects can be increased when Halazepam is combined with Felbamate.Approved
FencamfamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fencamfamine.Approved, Illicit, Withdrawn
FentanylThe risk or severity of adverse effects can be increased when Halazepam is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fexofenadine.Approved
FlibanserinThe risk or severity of adverse effects can be increased when Halazepam is combined with Flibanserin.Approved
FludiazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Fludiazepam.Approved, Illicit
FlunarizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Flunarizine.Approved
FlunitrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Flunitrazepam.Approved, Illicit
FluoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of adverse effects can be increased when Halazepam is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Halazepam.Approved
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Halazepam.Approved, Illicit
FluspirileneThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluspirilene.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Halazepam is combined with Fluticasone Propionate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Halazepam.Approved, Investigational
FosphenytoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Fosphenytoin.Approved
FospropofolThe risk or severity of adverse effects can be increased when Halazepam is combined with Fospropofol.Approved, Illicit
GabapentinThe risk or severity of adverse effects can be increased when Halazepam is combined with Gabapentin.Approved, Investigational
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Halazepam is combined with gabapentin enacarbil.Approved
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Halazepam is combined with Gamma Hydroxybutyric Acid.Approved, Illicit
GepironeThe risk or severity of adverse effects can be increased when Halazepam is combined with Gepirone.Investigational
GlutethimideThe risk or severity of adverse effects can be increased when Halazepam is combined with Glutethimide.Approved, Illicit
GuanfacineThe risk or severity of adverse effects can be increased when Halazepam is combined with Guanfacine.Approved, Investigational
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Halazepam.Approved
HalothaneThe risk or severity of adverse effects can be increased when Halazepam is combined with Halothane.Approved, Vet Approved
HeroinThe risk or severity of adverse effects can be increased when Halazepam is combined with Heroin.Approved, Illicit
HexobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Hexobarbital.Approved
HydrocodoneHalazepam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Halazepam.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved
IloperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Iloperidone.Approved
ImipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Imipramine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Halazepam is combined with Indalpine.Investigational, Withdrawn
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Halazepam.Approved, Vet Approved
KetamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketamine.Approved, Vet Approved
KetazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketazolam.Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Ketobemidone.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Halazepam is combined with Lamotrigine.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Halazepam is combined with Levetiracetam.Approved, Investigational
LevobupivacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levobupivacaine.Approved
LevocabastineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocabastine.Approved
LevocetirizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Levocetirizine.Approved
LevodopaThe risk or severity of adverse effects can be increased when Halazepam is combined with Levodopa.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Halazepam is combined with Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Halazepam is combined with Levomilnacipran.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Levorphanol.Approved
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Halazepam.Approved, Vet Approved
LithiumThe risk or severity of adverse effects can be increased when Halazepam is combined with Lithium.Approved
LofentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Lofentanil.Illicit
LoratadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Loratadine.Approved
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Halazepam.Approved
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Halazepam.Approved
Lu AA21004The risk or severity of adverse effects can be increased when Halazepam is combined with Lu AA21004.Investigational
LurasidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Lurasidone.Approved
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Vet Approved
MaprotilineThe risk or severity of adverse effects can be increased when Halazepam is combined with Maprotiline.Approved
MeclizineThe risk or severity of adverse effects can be increased when Halazepam is combined with Meclizine.Approved
MedetomidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Medetomidine.Vet Approved
MelatoninThe risk or severity of adverse effects can be increased when Halazepam is combined with Melatonin.Approved, Nutraceutical, Vet Approved
MelperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Melperone.Approved
MepivacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Mepivacaine.Approved, Vet Approved
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Halazepam.Approved, Illicit
MesoridazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Mesoridazine.Approved
MetaxaloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Metaxalone.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Halazepam.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Halazepam is combined with Methadyl Acetate.Approved, Illicit
MethapyrileneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methapyrilene.Withdrawn
MethaqualoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methaqualone.Illicit, Withdrawn
MethocarbamolThe risk or severity of adverse effects can be increased when Halazepam is combined with Methocarbamol.Approved, Vet Approved
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Halazepam.Approved
MethotrimeprazineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.Approved
MethoxyfluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Methoxyflurane.Approved, Vet Approved
MethsuximideThe risk or severity of adverse effects can be increased when Halazepam is combined with Methsuximide.Approved
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Methylphenobarbital.Approved
MetyrosineHalazepam may increase the sedative activities of Metyrosine.Approved
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Halazepam.Approved, Illicit
MilnacipranThe risk or severity of adverse effects can be increased when Halazepam is combined with Milnacipran.Approved
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Investigational
MirtazapineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.Approved
MolindoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Molindone.Approved
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Halazepam.Approved, Investigational
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved, Investigational
NalbuphineThe risk or severity of adverse effects can be increased when Halazepam is combined with Nalbuphine.Approved
NefazodoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Nefazodone.Approved, Withdrawn
NitrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Nitrazepam.Approved
Nitrous oxideThe risk or severity of adverse effects can be increased when Halazepam is combined with Nitrous oxide.Approved, Vet Approved
NormethadoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Normethadone.Approved, Illicit
NortriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Nortriptyline.Approved
OlanzapineThe risk or severity of adverse effects can be increased when Olanzapine is combined with Halazepam.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Halazepam is combined with Olopatadine.Approved
OndansetronThe risk or severity of adverse effects can be increased when Halazepam is combined with Ondansetron.Approved
OpiumThe risk or severity of adverse effects can be increased when Halazepam is combined with Opium.Approved, Illicit
OrphenadrineHalazepam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.Approved
OsanetantThe risk or severity of adverse effects can be increased when Halazepam is combined with Osanetant.Investigational
OxazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxazepam.Approved
OxetacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxetacaine.Investigational
OxprenololThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxprenolol.Approved
OxybuprocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxybuprocaine.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Halazepam.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Oxymorphone.Approved, Investigational, Vet Approved
PaliperidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Paliperidone.Approved
ParaldehydeHalazepam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Paroxetine.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Halazepam.Approved, Vet Approved
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Halazepam.Approved, Vet Approved
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved
PerazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Perazine.Investigational
PerospironeThe risk or severity of adverse effects can be increased when Halazepam is combined with Perospirone.Approved
PerphenazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Perphenazine.Approved
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Halazepam.Approved
PhenobarbitalThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenobarbital.Approved
PhenoxyethanolThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenoxyethanol.Approved
PhenytoinThe risk or severity of adverse effects can be increased when Halazepam is combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of adverse effects can be increased when Halazepam is combined with Pimozide.Approved
PipamperoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Pipamperone.Approved
PipotiazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Pipotiazine.Approved
PiritramideThe risk or severity of adverse effects can be increased when Halazepam is combined with Piritramide.Investigational
PizotifenThe risk or severity of adverse effects can be increased when Halazepam is combined with Pizotifen.Approved
PomalidomideThe risk or severity of adverse effects can be increased when Halazepam is combined with Pomalidomide.Approved
PramipexoleHalazepam may increase the sedative activities of Pramipexole.Approved, Investigational
PramocaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Pramocaine.Approved
PrazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Prazepam.Approved, Illicit
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Halazepam.Approved, Illicit, Investigational
PregnanoloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Pregnanolone.Investigational
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Halazepam.Approved
PrimidoneThe risk or severity of adverse effects can be increased when Halazepam is combined with Primidone.Approved, Vet Approved
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Halazepam.Approved, Investigational, Vet Approved
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Halazepam.Approved, Vet Approved
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Halazepam.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Promethazine.Approved
ProparacaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Proparacaine.Approved, Vet Approved
PropofolThe risk or severity of adverse effects can be increased when Halazepam is combined with Propofol.Approved, Investigational, Vet Approved
PropoxycaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Propoxycaine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Halazepam is combined with Protriptyline.Approved
PSD502The risk or severity of adverse effects can be increased when Halazepam is combined with PSD502.Investigational
QuazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Quazepam.Approved, Illicit
QuetiapineThe risk or severity of adverse effects can be increased when Halazepam is combined with Quetiapine.Approved
RacloprideThe risk or severity of adverse effects can be increased when Halazepam is combined with Raclopride.Investigational
RamelteonThe risk or severity of adverse effects can be increased when Halazepam is combined with Ramelteon.Approved, Investigational
RemifentanilThe risk or severity of adverse effects can be increased when Halazepam is combined with Remifentanil.Approved
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Halazepam.Approved, Withdrawn
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Halazepam.Approved
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Halazepam.Approved, Investigational
RitanserinThe risk or severity of adverse effects can be increased when Halazepam is combined with Ritanserin.Investigational
RomifidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Romifidine.Vet Approved
RopiniroleHalazepam may increase the sedative activities of Ropinirole.Approved, Investigational
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Halazepam.Approved
RotigotineHalazepam may increase the sedative activities of Rotigotine.Approved
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Halazepam.Approved
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Halazepam is combined with S-Ethylisothiourea.Experimental
Sage 547The risk or severity of adverse effects can be increased when Halazepam is combined with Sage 547.Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Scopolamine.Approved
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Halazepam.Approved, Vet Approved
SertindoleThe risk or severity of adverse effects can be increased when Halazepam is combined with Sertindole.Approved, Withdrawn
SertralineThe risk or severity of adverse effects can be increased when Halazepam is combined with Sertraline.Approved
SevofluraneThe risk or severity of adverse effects can be increased when Halazepam is combined with Sevoflurane.Approved, Vet Approved
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved
StiripentolThe risk or severity of adverse effects can be increased when Halazepam is combined with Stiripentol.Approved
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Halazepam.Approved, Investigational
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Halazepam.Approved
SuvorexantHalazepam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.Approved
TandospironeThe risk or severity of adverse effects can be increased when Halazepam is combined with Tandospirone.Investigational
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Halazepam.Approved
TasimelteonThe risk or severity of adverse effects can be increased when Halazepam is combined with Tasimelteon.Approved
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Halazepam.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetrabenazine.Approved
TetracaineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetracaine.Approved, Vet Approved
TetrodotoxinThe risk or severity of adverse effects can be increased when Halazepam is combined with Tetrodotoxin.Investigational
ThalidomideHalazepam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.Approved, Investigational, Withdrawn
ThiamylalThe risk or severity of adverse effects can be increased when Halazepam is combined with Thiamylal.Approved, Vet Approved
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Halazepam.Approved, Vet Approved
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Halazepam.Approved
ThiothixeneThe risk or severity of adverse effects can be increased when Halazepam is combined with Thiothixene.Approved
TiagabineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tiagabine.Approved
TiaprideThe risk or severity of adverse effects can be increased when Halazepam is combined with Tiapride.Investigational
TiletamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tiletamine.Vet Approved
TizanidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Tizanidine.Approved
TolcaponeThe risk or severity of adverse effects can be increased when Halazepam is combined with Tolcapone.Approved, Withdrawn
TopiramateThe risk or severity of adverse effects can be increased when Halazepam is combined with Topiramate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Halazepam.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trans-2-Phenylcyclopropylamine.Experimental
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Halazepam.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Halazepam.Approved, Investigational
TriazolamThe risk or severity of adverse effects can be increased when Halazepam is combined with Triazolam.Approved
TrifluoperazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trifluoperazine.Approved
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Halazepam.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Halazepam is combined with Trimipramine.Approved
TriprolidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Triprolidine.Approved
Uc1010The risk or severity of adverse effects can be increased when Halazepam is combined with Uc1010.Investigational
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Halazepam.Approved, Investigational
VenlafaxineThe risk or severity of adverse effects can be increased when Halazepam is combined with Venlafaxine.Approved
VigabatrinThe risk or severity of adverse effects can be increased when Halazepam is combined with Vigabatrin.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Halazepam is combined with Vortioxetine.Approved
XylazineThe risk or severity of adverse effects can be increased when Halazepam is combined with Xylazine.Vet Approved
YohimbineThe therapeutic efficacy of Halazepam can be decreased when used in combination with Yohimbine.Approved, Vet Approved
ZaleplonThe risk or severity of adverse effects can be increased when Halazepam is combined with Zaleplon.Approved, Illicit, Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Halazepam is combined with Ziconotide.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Halazepam is combined with Zimelidine.Withdrawn
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Halazepam.Approved
ZolazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Zolazepam.Vet Approved
ZolpidemHalazepam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Halazepam is combined with Zonisamide.Approved, Investigational
ZopicloneThe risk or severity of adverse effects can be increased when Halazepam is combined with Zopiclone.Approved
ZotepineThe risk or severity of adverse effects can be increased when Halazepam is combined with Zotepine.Approved
ZuclopenthixolThe risk or severity of adverse effects can be increased when Halazepam is combined with Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
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
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
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

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