You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameButalbital
Accession NumberDB00241  (APRD00266)
TypeSmall Molecule
GroupsApproved, Illicit
DescriptionButalbital, 5-allyl-5-isobutylbarbituric acid, is a barbiturate with an intermediate duration of action. It has the same chemical formula as talbutal but a different structure. Butalbital is often combined with other medications, such as acetaminophen or aspirin, and is commonly prescribed for the treatment of pain and headache. [Wikipedia]
Structure
Thumb
Synonyms
5-(2-methylpropyl)-5-prop-2-enyl-1,3-diazinane-2,4,6-trione
5-Allyl-5-(2-methylpropyl)barbituric acid
5-Allyl-5-(2'-methyl-N-propyl) barbituric acid
5-Allyl-5-isobutyl-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Allyl-5-isobutyl-pyrimidine-2,4,6-trione
5-Allyl-5-isobutylbarbituric acid
5-isobutyl-5-allylbarbituric acid
allylbarbital
allylbarbitone
Allylbarbituric acid
Butalbarbital
Butalbitalum
Iso-butylallylbarbituric acid
Itobarbital
Tetrallobarbital
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
SandoptalNot Available
Brand mixtures
NameLabellerIngredients
Acetaminophen, Butalbital and CaffeineSTAT Rx USA LLC
AllzitalLarken Laboratories, Inc.
Ascomp With CodeineNexgen Pharma, Inc.
BupapECR Pharmaceuticals
Butalbital Acetaminophen and CaffeineLake Erie Medical DBA Quality Care Products LLC
Butalbital and AcetaminophenQualitest Pharmaceuticals
Butalbital and Acetaminophen 50 Mg/325 mgSolubiomix
Butalbital CompoundMajor Pharmaceuticals
Butalbital, Acetaminophen and CaffeineWest Ward Pharmaceuticals Corp
Butalbital, Acetaminophen and Caffeine PlusSTAT Rx USA LLC
Butalbital, Acetaminophen and Caffeine With Codeine PhosphateWest Ward Pharmaceuticals Corp
Butalbital, Acetaminophen, and CaffeineWest ward Pharmaceutical Corp
Butalbital, Acetaminophen, CaffeineREMEDYREPACK INC.
Butalbital, Acetaminophen, Caffeine and Codeine PhosphateBreckenridge Pharmaceutical, Inc.
Butalbital, Acetaminophen, Caffeine, and Codeine PhosphateActavis Pharma, Inc.
Butalbital, Acetominophen and Caffeinebryant ranch prepack
Butalbital, Aspirin and CaffeineWest ward Pharmaceutical Corp
Butalbital, Aspirin and Caffeine TabletsQualitest
Butalbital, Aspirin, and CaffeineLannett Company, Inc.
Butalbital, Aspirin, Caffeine and Codeine PhosphateLannett Company, Inc.
Butalbital, Aspirin, Caffeine, and Codeine PhosphateMayne Pharma Inc.
ButapapMikart, Inc.
CapacetMagna Pharmaceuticals
EsgicForest Laboratories, Inc.
FioricetActavis Pharma, Inc.
Fioricet With CodeineWatson Pharma, Inc.
FiorinalActavis Pharma, Inc.
Fiorinal C1/2Tribute Pharmaceuticals Canada Inc
Fiorinal C1/4Tribute Pharmaceuticals Canada Inc
Fiorinal TabNovartis Pharmaceuticals Canada Inc
Fiorinal With CodeineActavis Pharma, Inc.
MargesicMarnel Pharmaceuticals, Llc
Marten-tabMarnel Pharmaceuticals, Inc.
OrbivanAtley Pharmaceuticals, Inc.
Phrenilin ForteValeant Pharmaceuticals North America LLC
PMS-pharnal CapsulesPharmascience Inc
PMS-pharnal TabletsPharmascience Inc
PMS-pharnal-C 1/4 CapsulesPharmascience Inc
PMS-pharnal-C1/2 CapsulesPharmascience Inc
Pronal - C1/2 CapsulesPro Doc Limitee
Pronal C1/4 CapsulesPro Doc Limitee
Pronal CapsulesPro Doc Limitee
Pronal TabletsPro Doc Limitee
Ratio-tecnalTeva Canada Limited
Ratio-tecnal C 1/2Teva Canada Limited
Ratio-tecnal C 1/4Teva Canada Limited
TenconInternational Ethical Labs, Inc.
Trianal C½Laboratoire Riva Inc
Trianal C¼Laboratoire Riva Inc
Trianal CapsulesLaboratoire Riva Inc
Trianal TabletLaboratoire Riva Inc
Vanatol LqGm Pharmaceuticals
ZebutalShionogi Inc.
SaltsNot Available
Categories
UNIIKHS0AZ4JVK
CAS number77-26-9
WeightAverage: 224.2563
Monoisotopic: 224.116092388
Chemical FormulaC11H16N2O3
InChI KeyInChIKey=UZVHFVZFNXBMQJ-UHFFFAOYSA-N
InChI
InChI=1S/C11H16N2O3/c1-4-5-11(6-7(2)3)8(14)12-10(16)13-9(11)15/h4,7H,1,5-6H2,2-3H3,(H2,12,13,14,15,16)
IUPAC Name
5-(2-methylpropyl)-5-(prop-2-en-1-yl)-1,3-diazinane-2,4,6-trione
SMILES
CC(C)CC1(CC=C)C(=O)NC(=O)NC1=O
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as barbituric acid derivatives. These are compounds containing a perhydropyrimidine ring substituted at C-2, -4 and -6 by oxo groups.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazines
Sub ClassPyrimidines and pyrimidine derivatives
Direct ParentBarbituric acid derivatives
Alternative Parents
Substituents
  • Barbiturate
  • Ureide
  • 1,3-diazinane
  • Urea
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External Descriptors
Pharmacology
IndicationUsed in combination with acetaminophen or aspirin and caffeine for its sedative and relaxant effects in the treatment of tension headaches, migraines, and pain.
PharmacodynamicsButalbital is a short to intermediate-acting barbiturate. Barbiturates act as nonselective depressants of the central nervous system (CNS), capable of producing all levels of CNS mood alteration from excitation to mild sedation, hypnosis, and deep coma. In sufficiently high therapeutic doses, barbiturates induce anesthesia.
Mechanism of actionButalbital binds at a distinct binding site associated with a Cl- ionopore at the GABAA receptor, increasing the duration of time for which the Cl- ionopore is open. The post-synaptic inhibitory effect of GABA in the thalamus is, therefore, prolonged.
Related Articles
AbsorptionWell absorbed from the gastrointestinal tract and is expected to distribute to most tissues in the body.
Volume of distributionNot Available
Protein binding45%
Metabolism

Hepatic, although most of the dose is eliminated via the kidney (59 to 88%). Urinary excretion products included parent drug (about 3.6% of the dose), 5-isobutyl-5-(2,3-dihydroxypropyl) barbituric acid (about 24% of the dose), 5-allyl-5(3-hydroxy-2-methyl-1-propyl) barbituric acid (about 4.8%).

Route of eliminationNot Available
Half life35 hours
ClearanceNot Available
ToxicitySymptoms of acute barbiturate poisoning include drowsiness, confusion, coma, respiratory depression, hypotension, and shock.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9112
Blood Brain Barrier+0.9703
Caco-2 permeable-0.5936
P-glycoprotein substrateNon-substrate0.5365
P-glycoprotein inhibitor IInhibitor0.5179
P-glycoprotein inhibitor IINon-inhibitor0.9678
Renal organic cation transporterNon-inhibitor0.9331
CYP450 2C9 substrateNon-substrate0.7999
CYP450 2D6 substrateNon-substrate0.8708
CYP450 3A4 substrateNon-substrate0.6804
CYP450 1A2 substrateNon-inhibitor0.8535
CYP450 2C9 inhibitorNon-inhibitor0.8768
CYP450 2D6 inhibitorNon-inhibitor0.9324
CYP450 2C19 inhibitorNon-inhibitor0.8354
CYP450 3A4 inhibitorNon-inhibitor0.9074
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9626
Ames testNon AMES toxic0.5716
CarcinogenicityNon-carcinogens0.8861
BiodegradationNot ready biodegradable0.9833
Rat acute toxicity3.0783 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9898
hERG inhibition (predictor II)Non-inhibitor0.9711
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral
Syruporal
Capsuleoral
Prices
Unit descriptionCostUnit
Butalbital powder3.83USD g
Butalbital compound tablet1.04USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point138.5 °CPhysProp
water solubility1700 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.7Not Available
Predicted Properties
PropertyValueSource
Water Solubility2.23 mg/mLALOGPS
logP1.47ALOGPS
logP1.59ChemAxon
logS-2ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity58.05 m3·mol-1ChemAxon
Polarizability22.42 Å3ChemAxon
Number of Rings1ChemAxon
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
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesNot Available
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 7-Nitroindazole is combined with Butalbital.
AcepromazineThe risk or severity of adverse effects can be increased when Acepromazine is combined with Butalbital.
AceprometazineThe risk or severity of adverse effects can be increased when Aceprometazine is combined with Butalbital.
adipiplonThe risk or severity of adverse effects can be increased when adipiplon is combined with Butalbital.
AgomelatineThe risk or severity of adverse effects can be increased when Agomelatine is combined with Butalbital.
AlfaxaloneThe risk or severity of adverse effects can be increased when Alfaxalone is combined with Butalbital.
AlfentanilThe risk or severity of adverse effects can be increased when Alfentanil is combined with Butalbital.
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Alphacetylmethadol is combined with Butalbital.
AlprazolamThe risk or severity of adverse effects can be increased when Alprazolam is combined with Butalbital.
AmisulprideThe risk or severity of adverse effects can be increased when Amisulpride is combined with Butalbital.
AmitriptylineThe risk or severity of adverse effects can be increased when Butalbital is combined with Amitriptyline.
AmobarbitalThe risk or severity of adverse effects can be increased when Amobarbital is combined with Butalbital.
AmoxapineThe risk or severity of adverse effects can be increased when Butalbital is combined with Amoxapine.
AmperozideThe risk or severity of adverse effects can be increased when Amperozide is combined with Butalbital.
AripiprazoleThe risk or severity of adverse effects can be increased when Aripiprazole is combined with Butalbital.
ArticaineThe risk or severity of adverse effects can be increased when Articaine is combined with Butalbital.
AsenapineThe risk or severity of adverse effects can be increased when Asenapine is combined with Butalbital.
AzaperoneThe risk or severity of adverse effects can be increased when Azaperone is combined with Butalbital.
AzelastineButalbital 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 Butalbital.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Butalbital.
BarbitalThe risk or severity of adverse effects can be increased when Barbital is combined with Butalbital.
BenzocaineThe risk or severity of adverse effects can be increased when Benzocaine is combined with Butalbital.
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Butalbital.
BrexpiprazoleThe risk or severity of adverse effects can be increased when Butalbital is combined with Brexpiprazole.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
BrimonidineThe risk or severity of adverse effects can be increased when Butalbital is combined with Brimonidine.
BromazepamThe risk or severity of adverse effects can be increased when Bromazepam is combined with Butalbital.
BrompheniramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Brompheniramine.
BrotizolamThe risk or severity of adverse effects can be increased when Brotizolam is combined with Butalbital.
BupivacaineThe risk or severity of adverse effects can be increased when Bupivacaine is combined with Butalbital.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Butalbital.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Butalbital.
ButabarbitalThe risk or severity of adverse effects can be increased when Butabarbital is combined with Butalbital.
ButacaineThe risk or severity of adverse effects can be increased when Butacaine is combined with Butalbital.
ButambenThe risk or severity of adverse effects can be increased when Butamben is combined with Butalbital.
ButethalThe risk or severity of adverse effects can be increased when Butethal is combined with Butalbital.
ButorphanolThe risk or severity of adverse effects can be increased when Butorphanol is combined with Butalbital.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Butalbital.
CarbinoxamineThe risk or severity of adverse effects can be increased when Butalbital is combined with Carbinoxamine.
CarfentanilThe risk or severity of adverse effects can be increased when Carfentanil is combined with Butalbital.
CarisoprodolThe risk or severity of adverse effects can be increased when Butalbital is combined with Carisoprodol.
CetirizineThe risk or severity of adverse effects can be increased when Butalbital is combined with Cetirizine.
Chloral hydrateThe risk or severity of adverse effects can be increased when Chloral hydrate is combined with Butalbital.
ChlordiazepoxideThe risk or severity of adverse effects can be increased when Chlordiazepoxide is combined with Butalbital.
ChlormezanoneThe risk or severity of adverse effects can be increased when Chlormezanone is combined with Butalbital.
ChloroprocaineThe risk or severity of adverse effects can be increased when Chloroprocaine is combined with Butalbital.
ChlorphenamineThe risk or severity of adverse effects can be increased when Butalbital is combined with Chlorphenamine.
ChlorpromazineThe risk or severity of adverse effects can be increased when Chlorpromazine is combined with Butalbital.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Chlorprothixene is combined with Butalbital.
ChlorzoxazoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Chlorzoxazone.
CinchocaineThe risk or severity of adverse effects can be increased when Cinchocaine is combined with Butalbital.
CitalopramThe risk or severity of adverse effects can be increased when Butalbital is combined with Citalopram.
ClemastineThe risk or severity of adverse effects can be increased when Butalbital is combined with Clemastine.
ClidiniumThe risk or severity of adverse effects can be increased when Butalbital is combined with Clidinium.
ClobazamThe risk or severity of adverse effects can be increased when Butalbital is combined with Clobazam.
clomethiazoleThe risk or severity of adverse effects can be increased when clomethiazole is combined with Butalbital.
ClomipramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Clomipramine.
ClonazepamThe risk or severity of adverse effects can be increased when Butalbital is combined with Clonazepam.
ClonidineThe risk or severity of adverse effects can be increased when Butalbital is combined with Clonidine.
ClorazepateThe risk or severity of adverse effects can be increased when Clorazepate is combined with Butalbital.
ClozapineThe risk or severity of adverse effects can be increased when Clozapine is combined with Butalbital.
CocaineThe risk or severity of adverse effects can be increased when Cocaine is combined with Butalbital.
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Butalbital.
CyclizineThe risk or severity of adverse effects can be increased when Butalbital is combined with Cyclizine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Butalbital.
CyproheptadineThe risk or severity of adverse effects can be increased when Butalbital is combined with Cyproheptadine.
DantroleneThe risk or severity of adverse effects can be increased when Butalbital is combined with Dantrolene.
DapiprazoleThe risk or severity of adverse effects can be increased when Dapiprazole is combined with Butalbital.
DapoxetineThe risk or severity of adverse effects can be increased when Butalbital is combined with Dapoxetine.
DapsoneThe risk or severity of adverse effects can be increased when Dapsone is combined with Butalbital.
deramciclaneThe risk or severity of adverse effects can be increased when deramciclane is combined with Butalbital.
DesfluraneThe risk or severity of adverse effects can be increased when Desflurane is combined with Butalbital.
DesipramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Desipramine.
DesloratadineThe risk or severity of adverse effects can be increased when Butalbital is combined with Desloratadine.
DetomidineThe risk or severity of adverse effects can be increased when Detomidine is combined with Butalbital.
DexbrompheniramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Dexbrompheniramine.
DexmedetomidineThe risk or severity of adverse effects can be increased when Dexmedetomidine is combined with Butalbital.
DextromoramideThe risk or severity of adverse effects can be increased when Dextromoramide is combined with Butalbital.
DextropropoxypheneThe risk or severity of adverse effects can be increased when Dextropropoxyphene is combined with Butalbital.
DezocineThe risk or severity of adverse effects can be increased when Dezocine is combined with Butalbital.
DiazepamThe risk or severity of adverse effects can be increased when Diazepam is combined with Butalbital.
DifenoxinThe risk or severity of adverse effects can be increased when Butalbital is combined with Difenoxin.
DihydrocodeineThe risk or severity of adverse effects can be increased when Dihydrocodeine is combined with Butalbital.
DihydroetorphineThe risk or severity of adverse effects can be increased when Dihydroetorphine is combined with Butalbital.
DihydromorphineThe risk or severity of adverse effects can be increased when Dihydromorphine is combined with Butalbital.
DimenhydrinateThe risk or severity of adverse effects can be increased when Butalbital is combined with Dimenhydrinate.
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Butalbital.
DiphenoxylateThe risk or severity of adverse effects can be increased when Diphenoxylate is combined with Butalbital.
DoramectinThe risk or severity of adverse effects can be increased when Doramectin is combined with Butalbital.
DoxepinThe risk or severity of adverse effects can be increased when Butalbital is combined with Doxepin.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
DoxylamineThe risk or severity of adverse effects can be increased when Butalbital is combined with Doxylamine.
DPDPEThe risk or severity of adverse effects can be increased when DPDPE is combined with Butalbital.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
DroperidolThe risk or severity of adverse effects can be increased when Droperidol is combined with Butalbital.
DrotebanolThe risk or severity of adverse effects can be increased when Drotebanol is combined with Butalbital.
DyclonineThe risk or severity of adverse effects can be increased when Dyclonine is combined with Butalbital.
EcgonineThe risk or severity of adverse effects can be increased when Ecgonine is combined with Butalbital.
ECGONINE METHYL ESTERThe risk or severity of adverse effects can be increased when ECGONINE METHYL ESTER is combined with Butalbital.
EfavirenzThe risk or severity of adverse effects can be increased when Butalbital is combined with Efavirenz.
EnfluraneThe risk or severity of adverse effects can be increased when Enflurane is combined with Butalbital.
EntacaponeThe risk or severity of adverse effects can be increased when Butalbital is combined with Entacapone.
EscitalopramThe risk or severity of adverse effects can be increased when Butalbital is combined with Escitalopram.
EstazolamThe risk or severity of adverse effects can be increased when Estazolam is combined with Butalbital.
EszopicloneThe risk or severity of adverse effects can be increased when Eszopiclone is combined with Butalbital.
EthanolButalbital 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 Butalbital.
EthchlorvynolThe risk or severity of adverse effects can be increased when Ethchlorvynol is combined with Butalbital.
EthosuximideThe risk or severity of adverse effects can be increased when Butalbital is combined with Ethosuximide.
EthotoinThe risk or severity of adverse effects can be increased when Butalbital is combined with Ethotoin.
Ethyl carbamateThe risk or severity of adverse effects can be increased when Ethyl carbamate is combined with Butalbital.
Ethyl loflazepateThe risk or severity of adverse effects can be increased when Ethyl loflazepate is combined with Butalbital.
EthylmorphineThe risk or severity of adverse effects can be increased when Ethylmorphine is combined with Butalbital.
EtidocaineThe risk or severity of adverse effects can be increased when Etidocaine is combined with Butalbital.
EtifoxineThe risk or severity of adverse effects can be increased when Etifoxine is combined with Butalbital.
EtizolamThe risk or severity of adverse effects can be increased when Etizolam is combined with Butalbital.
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Butalbital.
EtoperidoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Etoperidone.
EtorphineThe risk or severity of adverse effects can be increased when Etorphine is combined with Butalbital.
EzogabineThe risk or severity of adverse effects can be increased when Butalbital is combined with Ezogabine.
FelbamateThe risk or severity of adverse effects can be increased when Butalbital is combined with Felbamate.
FencamfamineThe risk or severity of adverse effects can be increased when Fencamfamine is combined with Butalbital.
FenfluramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Fenfluramine.
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Butalbital.
FexofenadineThe risk or severity of adverse effects can be increased when Butalbital is combined with Fexofenadine.
FlibanserinThe risk or severity of adverse effects can be increased when Butalbital is combined with Flibanserin.
FludiazepamThe risk or severity of adverse effects can be increased when Fludiazepam is combined with Butalbital.
FlunarizineThe risk or severity of adverse effects can be increased when Butalbital is combined with Flunarizine.
FlunitrazepamThe risk or severity of adverse effects can be increased when Flunitrazepam is combined with Butalbital.
FluoxetineThe risk or severity of adverse effects can be increased when Butalbital is combined with Fluoxetine.
FlupentixolThe risk or severity of adverse effects can be increased when Flupentixol is combined with Butalbital.
FluphenazineThe risk or severity of adverse effects can be increased when Fluphenazine is combined with Butalbital.
FlurazepamThe risk or severity of adverse effects can be increased when Flurazepam is combined with Butalbital.
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Butalbital.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Butalbital is combined with Fluticasone Propionate.
FluvoxamineThe risk or severity of adverse effects can be increased when Butalbital is combined with Fluvoxamine.
FosphenytoinThe risk or severity of adverse effects can be increased when Butalbital is combined with Fosphenytoin.
FospropofolThe risk or severity of adverse effects can be increased when Fospropofol is combined with Butalbital.
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Butalbital.
gabapentin enacarbilThe risk or severity of adverse effects can be increased when Butalbital is combined with gabapentin enacarbil.
Gamma Hydroxybutyric AcidThe risk or severity of adverse effects can be increased when Gamma Hydroxybutyric Acid is combined with Butalbital.
GlutethimideThe risk or severity of adverse effects can be increased when Glutethimide is combined with Butalbital.
GuanfacineThe risk or severity of adverse effects can be increased when Butalbital is combined with Guanfacine.
HalazepamThe risk or severity of adverse effects can be increased when Halazepam is combined with Butalbital.
HaloperidolThe risk or severity of adverse effects can be increased when Haloperidol is combined with Butalbital.
HalothaneThe risk or severity of adverse effects can be increased when Halothane is combined with Butalbital.
HeroinThe risk or severity of adverse effects can be increased when Heroin is combined with Butalbital.
HexobarbitalThe risk or severity of adverse effects can be increased when Hexobarbital is combined with Butalbital.
HydrocodoneThe risk or severity of adverse effects can be increased when Hydrocodone is combined with Butalbital.
HydromorphoneThe risk or severity of adverse effects can be increased when Hydromorphone is combined with Butalbital.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
HydroxyzineThe risk or severity of adverse effects can be increased when Butalbital is combined with Hydroxyzine.
IloperidoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Iloperidone.
ImipramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Imipramine.
IndalpineThe risk or severity of adverse effects can be increased when Butalbital is combined with Indalpine.
IsofluraneThe risk or severity of adverse effects can be increased when Isoflurane is combined with Butalbital.
KetamineThe risk or severity of adverse effects can be increased when Ketamine is combined with Butalbital.
KetazolamThe risk or severity of adverse effects can be increased when Ketazolam is combined with Butalbital.
KetobemidoneThe risk or severity of adverse effects can be increased when Ketobemidone is combined with Butalbital.
LamotrigineThe risk or severity of adverse effects can be increased when Butalbital is combined with Lamotrigine.
LevetiracetamThe risk or severity of adverse effects can be increased when Butalbital is combined with Levetiracetam.
LevobupivacaineThe risk or severity of adverse effects can be increased when Levobupivacaine is combined with Butalbital.
LevocabastineThe risk or severity of adverse effects can be increased when Butalbital is combined with Levocabastine.
LevocetirizineThe risk or severity of adverse effects can be increased when Butalbital is combined with Levocetirizine.
LevodopaThe risk or severity of adverse effects can be increased when Butalbital is combined with Levodopa.
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Levomethadyl Acetate is combined with Butalbital.
LevomilnacipranThe risk or severity of adverse effects can be increased when Butalbital is combined with Levomilnacipran.
LevorphanolThe risk or severity of adverse effects can be increased when Levorphanol is combined with Butalbital.
LidocaineThe risk or severity of adverse effects can be increased when Lidocaine is combined with Butalbital.
LithiumThe risk or severity of adverse effects can be increased when Lithium is combined with Butalbital.
LofentanilThe risk or severity of adverse effects can be increased when Lofentanil is combined with Butalbital.
LoratadineThe risk or severity of adverse effects can be increased when Butalbital is combined with Loratadine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Butalbital.
LoxapineThe risk or severity of adverse effects can be increased when Loxapine is combined with Butalbital.
Lu AA21004The risk or severity of adverse effects can be increased when Butalbital is combined with Lu AA21004.
LurasidoneThe risk or severity of adverse effects can be increased when Lurasidone is combined with Butalbital.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
Magnesium SulfateThe risk or severity of adverse effects can be increased when Butalbital is combined with Magnesium Sulfate.
MaprotilineThe risk or severity of adverse effects can be increased when Butalbital is combined with Maprotiline.
MeclizineThe risk or severity of adverse effects can be increased when Butalbital is combined with Meclizine.
MedetomidineThe risk or severity of adverse effects can be increased when Medetomidine is combined with Butalbital.
MelatoninThe risk or severity of adverse effects can be increased when Melatonin is combined with Butalbital.
MelperoneThe risk or severity of adverse effects can be increased when Melperone is combined with Butalbital.
MepivacaineThe risk or severity of adverse effects can be increased when Mepivacaine is combined with Butalbital.
MeprobamateThe risk or severity of adverse effects can be increased when Meprobamate is combined with Butalbital.
MesoridazineThe risk or severity of adverse effects can be increased when Mesoridazine is combined with Butalbital.
MetaxaloneThe risk or severity of adverse effects can be increased when Butalbital is combined with Metaxalone.
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Butalbital.
Methadyl AcetateThe risk or severity of adverse effects can be increased when Methadyl Acetate is combined with Butalbital.
MethapyrileneThe risk or severity of adverse effects can be increased when Methapyrilene is combined with Butalbital.
MethaqualoneThe risk or severity of adverse effects can be increased when Methaqualone is combined with Butalbital.
MethocarbamolThe risk or severity of adverse effects can be increased when Butalbital is combined with Methocarbamol.
MethohexitalThe risk or severity of adverse effects can be increased when Methohexital is combined with Butalbital.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Methotrimeprazine is combined with Butalbital.
MethoxyfluraneThe risk or severity of adverse effects can be increased when Methoxyflurane is combined with Butalbital.
MethsuximideThe risk or severity of adverse effects can be increased when Butalbital is combined with Methsuximide.
MethylphenobarbitalThe risk or severity of adverse effects can be increased when Methylphenobarbital is combined with Butalbital.
MetyrosineButalbital may increase the sedative activities of Metyrosine.
MidazolamThe risk or severity of adverse effects can be increased when Midazolam is combined with Butalbital.
MilnacipranThe risk or severity of adverse effects can be increased when Butalbital is combined with Milnacipran.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
MirtazapineButalbital 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 Butalbital.
MolindoneThe risk or severity of adverse effects can be increased when Molindone is combined with Butalbital.
MorphineThe risk or severity of adverse effects can be increased when Morphine is combined with Butalbital.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Butalbital.
NabiloneThe risk or severity of adverse effects can be increased when Butalbital is combined with Nabilone.
NalbuphineThe risk or severity of adverse effects can be increased when Nalbuphine is combined with Butalbital.
NitrazepamThe risk or severity of adverse effects can be increased when Nitrazepam is combined with Butalbital.
Nitric OxideThe risk or severity of adverse effects can be increased when Nitric Oxide is combined with Butalbital.
Nitrous oxideThe risk or severity of adverse effects can be increased when Nitrous oxide is combined with Butalbital.
NormethadoneThe risk or severity of adverse effects can be increased when Normethadone is combined with Butalbital.
NortriptylineThe risk or severity of adverse effects can be increased when Butalbital is combined with Nortriptyline.
OlanzapineThe risk or severity of adverse effects can be increased when Butalbital is combined with Olanzapine.
OlopatadineThe risk or severity of adverse effects can be increased when Butalbital is combined with Olopatadine.
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Butalbital.
OpiumThe risk or severity of adverse effects can be increased when Opium is combined with Butalbital.
OrphenadrineButalbital 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 Butalbital.
OsanetantThe risk or severity of adverse effects can be increased when Osanetant is combined with Butalbital.
OxazepamThe risk or severity of adverse effects can be increased when Oxazepam is combined with Butalbital.
OxprenololThe risk or severity of adverse effects can be increased when Oxprenolol is combined with Butalbital.
OxybuprocaineThe risk or severity of adverse effects can be increased when Oxybuprocaine is combined with Butalbital.
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Butalbital.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Butalbital.
PaliperidoneThe risk or severity of adverse effects can be increased when Paliperidone is combined with Butalbital.
ParaldehydeButalbital 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 Butalbital.
ParoxetineThe risk or severity of adverse effects can be increased when Butalbital is combined with Paroxetine.
PentazocineThe risk or severity of adverse effects can be increased when Pentazocine is combined with Butalbital.
PentobarbitalThe risk or severity of adverse effects can be increased when Pentobarbital is combined with Butalbital.
PerampanelThe risk or severity of adverse effects can be increased when Butalbital is combined with Perampanel.
PerospironeThe risk or severity of adverse effects can be increased when Perospirone is combined with Butalbital.
PerphenazineThe risk or severity of adverse effects can be increased when Perphenazine is combined with Butalbital.
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Butalbital.
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Butalbital.
PhenoxyethanolThe risk or severity of adverse effects can be increased when Phenoxyethanol is combined with Butalbital.
PhenytoinThe risk or severity of adverse effects can be increased when Butalbital is combined with Phenytoin.
PimozideThe risk or severity of adverse effects can be increased when Pimozide is combined with Butalbital.
PipamperoneThe risk or severity of adverse effects can be increased when Pipamperone is combined with Butalbital.
PipotiazineThe risk or severity of adverse effects can be increased when Butalbital is combined with Pipotiazine.
PizotifenThe risk or severity of adverse effects can be increased when Butalbital is combined with Pizotifen.
PomalidomideThe risk or severity of adverse effects can be increased when Butalbital is combined with Pomalidomide.
PramipexoleButalbital may increase the sedative activities of Pramipexole.
PramocaineThe risk or severity of adverse effects can be increased when Pramocaine is combined with Butalbital.
PrazepamThe risk or severity of adverse effects can be increased when Prazepam is combined with Butalbital.
PregabalinThe risk or severity of adverse effects can be increased when Pregabalin is combined with Butalbital.
PrilocaineThe risk or severity of adverse effects can be increased when Butalbital is combined with Prilocaine.
PrimidoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Primidone.
ProcaineThe risk or severity of adverse effects can be increased when Procaine is combined with Butalbital.
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Butalbital.
PromazineThe risk or severity of adverse effects can be increased when Promazine is combined with Butalbital.
PromethazineThe risk or severity of adverse effects can be increased when Butalbital is combined with Promethazine.
ProparacaineThe risk or severity of adverse effects can be increased when Proparacaine is combined with Butalbital.
PropofolThe risk or severity of adverse effects can be increased when Propofol is combined with Butalbital.
PropoxycaineThe risk or severity of adverse effects can be increased when Propoxycaine is combined with Butalbital.
ProtriptylineThe risk or severity of adverse effects can be increased when Butalbital is combined with Protriptyline.
PSD502The risk or severity of adverse effects can be increased when PSD502 is combined with Butalbital.
QuazepamThe risk or severity of adverse effects can be increased when Quazepam is combined with Butalbital.
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Butalbital.
RamelteonThe risk or severity of adverse effects can be increased when Butalbital is combined with Ramelteon.
RemifentanilThe risk or severity of adverse effects can be increased when Remifentanil is combined with Butalbital.
RemoxiprideThe risk or severity of adverse effects can be increased when Remoxipride is combined with Butalbital.
ReserpineThe risk or severity of adverse effects can be increased when Reserpine is combined with Butalbital.
RisperidoneThe risk or severity of adverse effects can be increased when Risperidone is combined with Butalbital.
RomifidineThe risk or severity of adverse effects can be increased when Romifidine is combined with Butalbital.
RopiniroleButalbital may increase the sedative activities of Ropinirole.
RopivacaineThe risk or severity of adverse effects can be increased when Ropivacaine is combined with Butalbital.
RotigotineButalbital may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Butalbital.
S-EthylisothioureaThe risk or severity of adverse effects can be increased when S-Ethylisothiourea is combined with Butalbital.
ScopolamineThe risk or severity of adverse effects can be increased when Butalbital is combined with Scopolamine.
SecobarbitalThe risk or severity of adverse effects can be increased when Secobarbital is combined with Butalbital.
SertindoleThe risk or severity of adverse effects can be increased when Sertindole is combined with Butalbital.
SertralineThe risk or severity of adverse effects can be increased when Butalbital is combined with Sertraline.
SevofluraneThe risk or severity of adverse effects can be increased when Sevoflurane is combined with Butalbital.
Sodium NitriteThe risk or severity of adverse effects can be increased when Butalbital is combined with Sodium Nitrite.
Sodium oxybateThe risk or severity of adverse effects can be increased when Sodium oxybate is combined with Butalbital.
StiripentolThe risk or severity of adverse effects can be increased when Butalbital is combined with Stiripentol.
SufentanilThe risk or severity of adverse effects can be increased when Sufentanil is combined with Butalbital.
SulpirideThe risk or severity of adverse effects can be increased when Sulpiride is combined with Butalbital.
SuvorexantThe risk or severity of adverse effects can be increased when Butalbital is combined with Suvorexant.
TapentadolThe risk or severity of adverse effects can be increased when Butalbital is combined with Tapentadol.
TasimelteonThe risk or severity of adverse effects can be increased when Butalbital is combined with Tasimelteon.
TemazepamThe risk or severity of adverse effects can be increased when Temazepam is combined with Butalbital.
TetrabenazineThe risk or severity of adverse effects can be increased when Butalbital is combined with Tetrabenazine.
TetracaineThe risk or severity of adverse effects can be increased when Tetracaine is combined with Butalbital.
TetrodotoxinThe risk or severity of adverse effects can be increased when Tetrodotoxin is combined with Butalbital.
ThalidomideButalbital 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 Butalbital.
ThiamylalThe risk or severity of adverse effects can be increased when Thiamylal is combined with Butalbital.
ThiopentalThe risk or severity of adverse effects can be increased when Thiopental is combined with Butalbital.
ThioridazineThe risk or severity of adverse effects can be increased when Thioridazine is combined with Butalbital.
ThiothixeneThe risk or severity of adverse effects can be increased when Thiothixene is combined with Butalbital.
TiagabineThe risk or severity of adverse effects can be increased when Butalbital is combined with Tiagabine.
TiletamineThe risk or severity of adverse effects can be increased when Tiletamine is combined with Butalbital.
TizanidineThe risk or severity of adverse effects can be increased when Butalbital is combined with Tizanidine.
TolcaponeThe risk or severity of adverse effects can be increased when Butalbital is combined with Tolcapone.
TopiramateThe risk or severity of adverse effects can be increased when Butalbital is combined with Topiramate.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Butalbital.
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Butalbital.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Butalbital.
TrazodoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Trazodone.
TriazolamThe risk or severity of adverse effects can be increased when Triazolam is combined with Butalbital.
TrifluoperazineThe risk or severity of adverse effects can be increased when Trifluoperazine is combined with Butalbital.
TriflupromazineThe risk or severity of adverse effects can be increased when Triflupromazine is combined with Butalbital.
TrimipramineThe risk or severity of adverse effects can be increased when Butalbital is combined with Trimipramine.
TriprolidineThe risk or severity of adverse effects can be increased when Butalbital is combined with Triprolidine.
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Butalbital.
VigabatrinThe risk or severity of adverse effects can be increased when Butalbital is combined with Vigabatrin.
VilazodoneThe risk or severity of adverse effects can be increased when Butalbital is combined with Vilazodone.
VortioxetineThe risk or severity of adverse effects can be increased when Butalbital is combined with Vortioxetine.
XylazineThe risk or severity of adverse effects can be increased when Xylazine is combined with Butalbital.
ZaleplonThe risk or severity of adverse effects can be increased when Zaleplon is combined with Butalbital.
ZiconotideThe risk or severity of adverse effects can be increased when Butalbital is combined with Ziconotide.
ZimelidineThe risk or severity of adverse effects can be increased when Butalbital is combined with Zimelidine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Ziprasidone is combined with Butalbital.
ZolazepamThe risk or severity of adverse effects can be increased when Zolazepam is combined with Butalbital.
ZolpidemThe risk or severity of adverse effects can be increased when Zolpidem is combined with Butalbital.
ZonisamideThe risk or severity of adverse effects can be increased when Butalbital is combined with Zonisamide.
ZopicloneThe risk or severity of adverse effects can be increased when Zopiclone is combined with Butalbital.
ZotepineThe risk or severity of adverse effects can be increased when Zotepine is combined with Butalbital.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Zuclopenthixol is combined with Butalbital.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Whiting PJ: The GABAA receptor gene family: new opportunities for drug development. Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57. [PubMed:14579514 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
  4. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  5. Cutrer FM, Mitsikostas DD, Ayata G, Sanchez del Rio M: Attenuation by butalbital of capsaicin-induced c-fos-like immunoreactivity in trigeminal nucleus caudalis. Headache. 1999 Nov-Dec;39(10):697-704. [PubMed:11279945 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. 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 ]
  8. 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 ]
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. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
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. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
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:
GABRA4
Uniprot ID:
P48169
Molecular Weight:
61622.645 Da
References
  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
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. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
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:
GABRA6
Uniprot ID:
Q16445
Molecular Weight:
51023.69 Da
References
  1. Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232 ]
  2. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ligand-gated ion channel activity
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions.
Gene Name:
CHRNA4
Uniprot ID:
P43681
Molecular Weight:
69956.47 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Toxic substance binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
Gene Name:
CHRNA7
Uniprot ID:
P36544
Molecular Weight:
56448.925 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Arias HR, Bhumireddy P: Anesthetics as chemical tools to study the structure and function of nicotinic acetylcholine receptors. Curr Protein Pept Sci. 2005 Oct;6(5):451-72. [PubMed:16248797 ]
  3. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Ionotropic glutamate receptor activity
Specific Function:
Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and t...
Gene Name:
GRIA2
Uniprot ID:
P42262
Molecular Weight:
98820.32 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Kainate selective glutamate receptor activity
Specific Function:
Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inacti...
Gene Name:
GRIK2
Uniprot ID:
Q13002
Molecular Weight:
102582.475 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449 ]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207 ]
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]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23