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Identification
NameFludiazepam
Accession NumberDB01567
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionFludiazepam is a drug which is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is a scheduled drug in the U.S., but is approved for use in Japan.
Structure
Thumb
Synonyms
7-chloro-5-(O-Fluorophenyl)-1,3-dihydro-1-methyl-2H-1,4-benzodiazepin-2-one
Erispan
Fludiazepamum
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ErispanSumitomo
Brand mixturesNot Available
SaltsNot Available
Categories
UNII7F64A2K16Z
CAS number3900-31-0
WeightAverage: 302.731
Monoisotopic: 302.062218928
Chemical FormulaC16H12ClFN2O
InChI KeyInChIKey=ROYOYTLGDLIGBX-UHFFFAOYSA-N
InChI
InChI=1S/C16H12ClFN2O/c1-20-14-7-6-10(17)8-12(14)16(19-9-15(20)21)11-4-2-3-5-13(11)18/h2-8H,9H2,1H3
IUPAC Name
7-chloro-5-(2-fluorophenyl)-1-methyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
SMILES
CN1C2=C(C=C(Cl)C=C2)C(=NCC1=O)C1=CC=CC=C1F
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
  • Halobenzene
  • Fluorobenzene
  • Chlorobenzene
  • Benzenoid
  • Monocyclic benzene moiety
  • Aryl halide
  • Aryl fluoride
  • 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
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationUsed for the short-term treatment of anxiety disorders.
PharmacodynamicsFludiazepam is a benzodiazepine derivative. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Fludiazepam accumulates primarily in the cortex and thalamus.
Mechanism of actionFludiazepam has similar action to diazepam, but binds with four times more affinity to benzodiazepine receptors than diazepam.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySymptoms of overdose include drowsiness, weakness, nausea, dizziness, abdominal pain, cerebral oedema and renal tubular necrosis, hyperglycaemia and hypoglycaemia, liver damage, encephalopathy, coma and death.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9946
Caco-2 permeable+0.8567
P-glycoprotein substrateSubstrate0.6618
P-glycoprotein inhibitor IInhibitor0.5293
P-glycoprotein inhibitor IINon-inhibitor0.8532
Renal organic cation transporterInhibitor0.592
CYP450 2C9 substrateNon-substrate0.6724
CYP450 2D6 substrateNon-substrate0.9087
CYP450 3A4 substrateSubstrate0.8081
CYP450 1A2 substrateInhibitor0.7925
CYP450 2C9 inhibitorNon-inhibitor0.5446
CYP450 2D6 inhibitorNon-inhibitor0.8884
CYP450 2C19 inhibitorInhibitor0.5598
CYP450 3A4 inhibitorInhibitor0.5153
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5827
Ames testNon AMES toxic0.8792
CarcinogenicityNon-carcinogens0.817
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.2719 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9953
hERG inhibition (predictor II)Non-inhibitor0.8236
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point218.5-219Yamamato, H., Inaba, S.,Okamoto, T., Hirohashi, T., Ishizumi, K., Yamamoto, M., Maruyama, l., Mori, K. and Kobayashi, T.; U.S. Patents 3,723,461; March 27, 1973; 3,828,027; August 6, 1974 and 3,925,364; December 9, 1975; all assigned to Sumitomo Chemical Co., Ltd.
logP2.75HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.0144 mg/mLALOGPS
logP2.83ALOGPS
logP3.22ChemAxon
logS-4.3ALOGPS
pKa (Strongest Basic)1.89ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area32.67 Å2ChemAxon
Rotatable Bond Count1ChemAxon
Refractivity80.03 m3·mol-1ChemAxon
Polarizability29.45 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)splash10-0uk9-2794000000-6f1a3e2e0783b2069f2fView in MoNA
References
Synthesis Reference

Yamamato, H., Inaba, S.,Okamoto, T., Hirohashi, T., Ishizumi, K., Yamamoto, M., Maruyama, l., Mori, K. and Kobayashi, T.; U.S. Patents 3,723,461; March 27, 1973; 3,828,027; August 6, 1974 and 3,925,364; December 9, 1975; all assigned to Sumitomo Chemical Co., Ltd.

General References
  1. Ishiwata K, Yanai K, Ido T, Miura-Kanno Y, Kawashima K: Synthesis and biodistribution of [11C]fludiazepam for imaging benzodiazepine receptors. Int J Rad Appl Instrum B. 1988;15(4):365-71. [PubMed:2855634 ]
  2. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
External Links
ATC CodesN05BA17
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 Fludiazepam is combined with 7-Nitroindazole.
AcepromazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Acepromazine.
AceprometazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Aceprometazine.
adipiplonThe risk or severity of adverse effects can be increased when Fludiazepam is combined with adipiplon.
AgomelatineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Agomelatine.
AlfaxaloneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Alfaxalone.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Fludiazepam.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Fludiazepam.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Fludiazepam.
AmisulprideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Amisulpride.
AmitriptylineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Amitriptyline.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Fludiazepam.
AmoxapineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Amperozide.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Fludiazepam.
ArticaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Articaine.
AsenapineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Asenapine.
AzaperoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Azaperone.
AzelastineFludiazepam 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 Fludiazepam.
BaclofenThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Baclofen.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Fludiazepam.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Fludiazepam.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Benzyl alcohol.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
BrimonidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Fludiazepam.
BrompheniramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Brompheniramine.
BrotizolamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Brotizolam.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Fludiazepam.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Fludiazepam.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Fludiazepam.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Fludiazepam.
ButacaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Butacaine.
ButalbitalThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Butalbital.
ButambenThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Butamben.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Fludiazepam.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Fludiazepam.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Fludiazepam.
CarbinoxamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Carbinoxamine.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Fludiazepam.
CarisoprodolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Carisoprodol.
CetirizineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Cetirizine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Fludiazepam.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Fludiazepam.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Fludiazepam.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Fludiazepam.
ChlorphenamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Chlorphenamine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Fludiazepam.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Fludiazepam.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Chlorzoxazone.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Fludiazepam.
CitalopramThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clobazam.
clomethiazoleThe risk or severity of adverse effects can be increased when Fludiazepam is combined with clomethiazole.
ClomipramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Fludiazepam.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Fludiazepam.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Fludiazepam.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Fludiazepam.
CyclizineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Fludiazepam.
CyproheptadineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Cyproheptadine.
DantroleneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Fludiazepam.
DapoxetineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Dapoxetine.
deramciclaneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with deramciclane.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Fludiazepam.
DesipramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Desloratadine.
DetomidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Detomidine.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Dexbrompheniramine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Fludiazepam.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Fludiazepam.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Fludiazepam.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Fludiazepam.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Fludiazepam.
DifenoxinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Fludiazepam.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Fludiazepam.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Fludiazepam.
DimenhydrinateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Fludiazepam.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Fludiazepam.
DoramectinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Doramectin.
DoxepinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
DoxylamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when Fludiazepam is combined with DPDPE.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Fludiazepam.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Fludiazepam.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Fludiazepam.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Fludiazepam.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when Fludiazepam is combined with ECGONINE METHYL ESTER.
EfavirenzThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Efavirenz.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Fludiazepam.
EntacaponeThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Entacapone.
EscitalopramThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Fludiazepam.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Fludiazepam.
EthanolFludiazepam 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 Fludiazepam.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Fludiazepam.
EthosuximideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ethotoin.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ethyl carbamate.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Fludiazepam.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Fludiazepam.
EtidocaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Etidocaine.
EtifoxineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Etifoxine.
EtizolamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Etizolam.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Fludiazepam.
EtoperidoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Fludiazepam.
EzogabineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Felbamate.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Fludiazepam.
FenfluramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Fludiazepam.
FexofenadineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fexofenadine.
FlibanserinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Flibanserin.
FlunarizineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Fludiazepam.
FluoxetineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Fludiazepam.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Fludiazepam.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Fludiazepam.
FluspirileneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fluspirilene.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Fospropofol.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Fludiazepam.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Fludiazepam is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Fludiazepam.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Fludiazepam.
GuanfacineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Guanfacine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Fludiazepam.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Fludiazepam.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Fludiazepam.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Fludiazepam.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Fludiazepam.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Fludiazepam.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Fludiazepam.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
HydroxyzineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Imipramine.
IndalpineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Fludiazepam.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Fludiazepam.
KetazolamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ketazolam.
KetobemidoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ketobemidone.
LamotrigineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Lamotrigine.
LevetiracetamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Fludiazepam.
LevocabastineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Fludiazepam.
LevomilnacipranThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Fludiazepam.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Fludiazepam.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Fludiazepam.
LofentanilThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Lofentanil.
LoratadineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Fludiazepam.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Fludiazepam.
Lu AA21004The risk or severity of adverse effects can be increased when Fludiazepam is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Lurasidone.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Maprotiline.
MeclizineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Meclizine.
MedetomidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Medetomidine.
MefloquineThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Mefloquine.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Fludiazepam.
MelperoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Melperone.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Fludiazepam.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Fludiazepam.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Fludiazepam.
MetaxaloneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Metaxalone.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Fludiazepam.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Fludiazepam.
MethapyrileneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Methapyrilene.
MethaqualoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Methaqualone.
MethocarbamolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Fludiazepam.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Fludiazepam.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Fludiazepam.
MethsuximideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Methsuximide.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Fludiazepam.
MetyrosineFludiazepam may increase the sedative activities of Metyrosine.
MianserinThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Mianserin.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Fludiazepam.
MilnacipranThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
MirtazapineFludiazepam 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 Fludiazepam.
MolindoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Fludiazepam.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Fludiazepam.
NabiloneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Fludiazepam.
NitrazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Nitrazepam.
Nitrous oxideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Nitrous oxide.
NormethadoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Normethadone.
NortriptylineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Nortriptyline.
OlanzapineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Olopatadine.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Fludiazepam.
OpiumThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Opium.
OrlistatThe serum concentration of Fludiazepam can be decreased when it is combined with Orlistat.
OrphenadrineFludiazepam 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 Fludiazepam.
OsanetantThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Osanetant.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Fludiazepam.
OxprenololThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Oxprenolol.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Fludiazepam.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Fludiazepam.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Fludiazepam.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Fludiazepam.
ParaldehydeFludiazepam 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 Fludiazepam.
ParoxetineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Fludiazepam.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Fludiazepam.
PerampanelThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Perospirone.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Fludiazepam.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Fludiazepam.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Fludiazepam.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Phenoxyethanol.
PhenytoinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Fludiazepam.
PipamperoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Pipamperone.
PipotiazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Pomalidomide.
PramipexoleFludiazepam may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Pramocaine.
PrazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Prazepam.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Fludiazepam.
PrilocaineThe risk or severity of adverse effects can be increased when Prilocaine is combined with Fludiazepam.
PrimidoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Primidone.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Fludiazepam.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Fludiazepam.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Fludiazepam.
PromethazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Promethazine.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Fludiazepam.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Fludiazepam.
PropoxycaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Propoxycaine.
ProtriptylineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Protriptyline.
PSD502The risk or severity of adverse effects can be increased when Fludiazepam is combined with PSD502.
QuazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Quazepam.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Fludiazepam.
RamelteonThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ramelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Fludiazepam.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Fludiazepam.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Fludiazepam.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Fludiazepam.
RomifidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Romifidine.
RopiniroleFludiazepam may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Fludiazepam.
RotigotineFludiazepam may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Fludiazepam.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when Fludiazepam is combined with S-Ethylisothiourea.
ScopolamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Scopolamine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Fludiazepam.
SertindoleThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Sertindole.
SertralineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Fludiazepam.
Sodium oxybateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Sodium oxybate.
StiripentolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Fludiazepam.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Fludiazepam.
SuvorexantThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tapentadol.
TasimelteonThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Fludiazepam.
TetrabenazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tetrabenazine.
TetracaineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tetracaine.
TetrodotoxinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tetrodotoxin.
ThalidomideFludiazepam 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 Fludiazepam.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Fludiazepam.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Fludiazepam.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Fludiazepam.
ThiothixeneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Thiothixene.
TiagabineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tiagabine.
TiletamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tiletamine.
TizanidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tizanidine.
TolcaponeThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Tolcapone.
TopiramateThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Fludiazepam.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Trans-2-Phenylcyclopropylamine.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Fludiazepam.
TrazodoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Fludiazepam.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Fludiazepam.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Fludiazepam.
TrimipramineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Trimipramine.
TriprolidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Triprolidine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Fludiazepam.
VigabatrinThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Vigabatrin.
VilazodoneThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Xylazine.
YohimbineThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Yohimbine.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Fludiazepam.
ZiconotideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Fludiazepam.
ZolazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Zolazepam.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Fludiazepam.
ZonisamideThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Fludiazepam.
ZotepineThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Zotepine.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol.
  • Avoid excessive quantities of coffee or tea (Caffeine).
  • Avoid taking with grapefruit juice.

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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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. Nakatsuka I, Shimizu H, Asami Y, Katoh T, Hirose A, Yoshitake A: Benzodiazepines and their metabolites: relationship between binding affinity to the benzodiazepine receptor and pharmacological activity. Life Sci. 1985 Jan 14;36(2):113-9. [PubMed:2857046 ]
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Drug created on July 31, 2007 07:10 / Updated on August 17, 2016 12:23