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Identification
NameMethohexital
Accession NumberDB00474  (APRD00058)
TypeSmall Molecule
GroupsApproved
Description

An intravenous anesthetic with a short duration of action that may be used for induction of anesthesia. [PubChem]

Structure
Thumb
Synonyms
(+-)-5-Allyl-1-methyl-5-(1-methyl-2-pentynyl)barbituric acid
5-Allyl-1-methyl-5-(1-methyl-2-pentynyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Allyl-1-methyl-5-(1-methyl-pent-2-ynyl)-pyrimidine-2,4,6-trione
5-Allyl-5-(3-hexyn-2-yl)-1-methylbarbituric acid
alpha-DL-1-Methyl-5-allyl-5-(1'-methylpentyn-2-yl)barbituric acid
Methohexital
Methohexitalum
Methohexitone
Metohexital
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Brevital Sodiuminjection, powder, lyophilized, for solution500 mg/1intramuscular; intravenous; rectalPar Pharmaceutical, Inc.2007-11-01Not applicableUs
Brevital Sodiuminjection, powder, lyophilized, for solution500 mg/1intramuscular; intravenous; rectalA S Medication Solutions Llc2007-11-01Not applicableUs
Brevital Sodiuminjection, powder, lyophilized, for solution2.5 g/1intramuscular; intravenous; rectalPar Pharmaceutical, Inc.2007-11-01Not applicableUs
Brietal Sodium Ampoule 660powder for solution500 mgintravenousEli Lilly Canada Inc1960-12-312000-08-03Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BrevitalNot Available
BrietalNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Methohexital sodium
Thumb
  • InChI Key: KDXZREBVGAGZHS-UHFFFAOYNA-M
  • Monoisotopic Mass: 284.113687095
  • Average Mass: 284.2861
DBSALT000631
Categories
UNIIE5B8ND5IPE
CAS number151-83-7
WeightAverage: 262.3043
Monoisotopic: 262.131742452
Chemical FormulaC14H18N2O3
InChI KeyInChIKey=NZXKDOXHBHYTKP-UHFFFAOYSA-N
InChI
InChI=1S/C14H18N2O3/c1-5-7-8-10(3)14(9-6-2)11(17)15-13(19)16(4)12(14)18/h6,10H,2,5,9H2,1,3-4H3,(H,15,17,19)
IUPAC Name
5-(hex-3-yn-2-yl)-1-methyl-5-(prop-2-en-1-yl)-1,3-diazinane-2,4,6-trione
SMILES
CCC#CC(C)C1(CC=C)C(=O)NC(=O)N(C)C1=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
  • Tertiary amine
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aliphatic heteromonocyclic compound
Molecular FrameworkAliphatic heteromonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationMethohexital is indicated for use as an intravenous anaesthetic. It has also been commonly used to induce deep sedation.
PharmacodynamicsMethohexital, a barbiturate, is used for the induction of anesthesia prior to the use of other general anesthetic agents and for induction of anesthesia for short surgical, diagnostic, or therapeutic procedures associated with minimal painful stimuli. Little analgesia is conferred by barbiturates; their use in the presence of pain may result in excitation.
Mechanism of actionMethohexital 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
AbsorptionThe absolute bioavailability following rectal administration of methohexital is 17%.
Volume of distributionNot Available
Protein binding73%
Metabolism

Metabolism occurs in the liver through demethylation and oxidation. Side-chain oxidation is the most important biotransformation involved in termination of biologic activity.

Route of eliminationExcretion occurs via the kidneys through glomerular filtration.
Half life5.6 ± 2.7 minutes
ClearanceNot Available
ToxicityThe onset of toxicity following an overdose of intravenously administered methohexital will be within seconds of the infusion. If methohexital is administered rectally or is ingested, the onset of toxicity may be delayed. The manifestations of an ultrashort-acting barbiturate in overdose include central nervous system depression, respiratory depression, hypotension, loss of peripheral vascular resistance, and muscular hyperactivity ranging from twitching to convulsive-like movements. Other findings may include convulsions and allergic reactions. Following massive exposure to any barbiturate, pulmonary edema, circulatory collapse with loss of peripheral vascular tone, and cardiac arrest may occur.
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+0.9143
Blood Brain Barrier+0.982
Caco-2 permeable+0.5
P-glycoprotein substrateNon-substrate0.6307
P-glycoprotein inhibitor IInhibitor0.5661
P-glycoprotein inhibitor IINon-inhibitor0.9294
Renal organic cation transporterNon-inhibitor0.9297
CYP450 2C9 substrateNon-substrate0.823
CYP450 2D6 substrateNon-substrate0.8823
CYP450 3A4 substrateNon-substrate0.6454
CYP450 1A2 substrateNon-inhibitor0.8001
CYP450 2C9 inhibitorNon-inhibitor0.8179
CYP450 2D6 inhibitorNon-inhibitor0.9099
CYP450 2C19 inhibitorNon-inhibitor0.7836
CYP450 3A4 inhibitorNon-inhibitor0.8501
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.954
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.8264
BiodegradationNot ready biodegradable0.9737
Rat acute toxicity2.9098 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.978
hERG inhibition (predictor II)Non-inhibitor0.9697
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Jhp pharmaceuticals llc
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintramuscular; intravenous; rectal2.5 g/1
Injection, powder, lyophilized, for solutionintramuscular; intravenous; rectal500 mg/1
Powder for solutionintravenous500 mg
Prices
Unit descriptionCostUnit
Brevital sodium 2.5 gm vial221.2USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP1.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0524 mg/mLALOGPS
logP2.43ALOGPS
logP2.29ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)8.73ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area66.48 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity71.51 m3·mol-1ChemAxon
Polarizability27.4 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (12.5 KB)
Spectra
Spectrum TypeDescriptionSplash Key
MSMass Spectrum (Electron Ionization)splash10-0fbc-9520000000-5141cdceea7f6d5013b0View in MoNA
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN01AF01N05CA15
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (184 KB)
MSDSDownload (46.5 KB)
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Methohexital.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Methohexital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Methohexital.
AcetazolamideMethohexital may increase the hypotensive activities of Acetazolamide.
AldesleukinMethohexital may increase the hypotensive activities of Aldesleukin.
AliskirenMethohexital may increase the hypotensive activities of Aliskiren.
AmilorideMethohexital may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Methohexital.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Methohexital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Methohexital.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Methohexital.
AmrinoneThe metabolism of Amrinone can be increased when combined with Methohexital.
Amyl NitriteMethohexital may increase the hypotensive activities of Amyl Nitrite.
ApraclonidineMethohexital may increase the hypotensive activities of Apraclonidine.
AtenololMethohexital may increase the hypotensive activities of Atenolol.
AzelastineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Azilsartan medoxomilMethohexital may increase the hypotensive activities of Azilsartan medoxomil.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Methohexital.
BenazeprilMethohexital may increase the hypotensive activities of Benazepril.
BendroflumethiazideMethohexital may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BepridilThe metabolism of Bepridil can be increased when combined with Methohexital.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Methohexital.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Methohexital.
BretyliumMethohexital may increase the hypotensive activities of Bretylium.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
BumetanideMethohexital may increase the hypotensive activities of Bumetanide.
BuprenorphineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ButalbitalThe metabolism of Butalbital can be increased when combined with Methohexital.
CaffeineThe metabolism of Caffeine can be increased when combined with Methohexital.
CanagliflozinMethohexital may increase the hypotensive activities of Canagliflozin.
CandesartanMethohexital may increase the hypotensive activities of Candesartan.
CaptoprilMethohexital may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Methohexital.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Methohexital.
ChloramphenicolThe metabolism of Methohexital can be decreased when combined with Chloramphenicol.
ChlorothiazideMethohexital may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Methohexital.
ChlorthalidoneMethohexital may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilMethohexital may increase the hypotensive activities of Cilazapril.
ClevidipineMethohexital may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Methohexital.
ClonidineMethohexital may increase the hypotensive activities of Clonidine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Methohexital.
DapagliflozinMethohexital may increase the hypotensive activities of Dapagliflozin.
DesipramineThe metabolism of Desipramine can be increased when combined with Methohexital.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Methohexital.
DexmedetomidineMethohexital may increase the hypotensive activities of Dexmedetomidine.
DiclofenamideMethohexital may increase the hypotensive activities of Diclofenamide.
DicoumarolThe metabolism of Dicoumarol can be increased when combined with Methohexital.
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Methohexital.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Methohexital.
DinutuximabMethohexital may increase the hypotensive activities of Dinutuximab.
DipyridamoleMethohexital may increase the hypotensive activities of Dipyridamole.
DoxazosinMethohexital may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Methohexital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Methohexital.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Methohexital.
EmpagliflozinMethohexital may increase the hypotensive activities of Empagliflozin.
EnalaprilMethohexital may increase the hypotensive activities of Enalapril.
EnalaprilatMethohexital may increase the hypotensive activities of Enalaprilat.
EplerenoneMethohexital may increase the hypotensive activities of Eplerenone.
EprosartanMethohexital may increase the hypotensive activities of Eprosartan.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Methohexital.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Methohexital.
Etacrynic acidMethohexital may increase the hypotensive activities of Ethacrynic acid.
EthanolMethohexital may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Ethinyl EstradiolThe therapeutic efficacy of Ethinyl Estradiol can be decreased when used in combination with Methohexital.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Methohexital.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Methohexital.
FelbamateThe serum concentration of Methohexital can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Methohexital.
FlunarizineThe metabolism of Flunarizine can be increased when combined with Methohexital.
FosinoprilMethohexital may increase the hypotensive activities of Fosinopril.
FurosemideMethohexital may increase the hypotensive activities of Furosemide.
GabapentinThe metabolism of Gabapentin can be increased when combined with Methohexital.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Methohexital.
GuanfacineMethohexital may increase the hypotensive activities of Guanfacine.
HydralazineMethohexital may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideMethohexital may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydrocodoneMethohexital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
ImipramineThe metabolism of Imipramine can be increased when combined with Methohexital.
IndapamideMethohexital may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanMethohexital may increase the hypotensive activities of Irbesartan.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Methohexital.
IsosorbideMethohexital may increase the hypotensive activities of Isosorbide.
Isosorbide DinitrateMethohexital may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitrateMethohexital may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprineMethohexital may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Methohexital.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Methohexital.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Methohexital.
LercanidipineThe metabolism of Lercanidipine can be increased when combined with Methohexital.
LevobunololMethohexital may increase the hypotensive activities of Levobunolol.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Methohexital.
LisinoprilMethohexital may increase the hypotensive activities of Lisinopril.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Methohexital.
LosartanMethohexital may increase the hypotensive activities of Losartan.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MannitolMethohexital may increase the hypotensive activities of Mannitol.
MecamylamineMethohexital may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Methohexital.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Methohexital.
MetforminMethohexital may increase the hypotensive activities of Metformin.
MethazolamideMethohexital may increase the hypotensive activities of Methazolamide.
MethotrimeprazineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethyclothiazideMethohexital may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaMethohexital may increase the hypotensive activities of Methyldopa.
MetipranololMethohexital may increase the hypotensive activities of Metipranolol.
MetolazoneMethohexital may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Methohexital.
MetyrosineMethohexital may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MinoxidilMethohexital may increase the hypotensive activities of Minoxidil.
MirtazapineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MoexiprilMethohexital may increase the hypotensive activities of Moexipril.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
NadololMethohexital may increase the hypotensive activities of Nadolol.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Methohexital.
NesiritideMethohexital may increase the hypotensive activities of Nesiritide.
NicardipineThe metabolism of Nicardipine can be increased when combined with Methohexital.
NifedipineThe metabolism of Nifedipine can be increased when combined with Methohexital.
NimodipineThe metabolism of Nimodipine can be increased when combined with Methohexital.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Methohexital.
NitrendipineThe metabolism of Nitrendipine can be increased when combined with Methohexital.
NitroglycerinMethohexital may increase the hypotensive activities of Nitroglycerin.
NitroprussideMethohexital may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Methohexital.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Methohexital.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Methohexital.
OlmesartanMethohexital may increase the hypotensive activities of Olmesartan.
OrphenadrineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PapaverineMethohexital may increase the hypotensive activities of Papaverine.
ParaldehydeMethohexital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Methohexital is combined with Paroxetine.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Methohexital.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
PerhexilineThe metabolism of Perhexiline can be increased when combined with Methohexital.
PerindoprilMethohexital may increase the hypotensive activities of Perindopril.
PethidineMethohexital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PindololThe serum concentration of Pindolol can be decreased when it is combined with Methohexital.
PramipexoleMethohexital may increase the sedative activities of Pramipexole.
PrazosinMethohexital may increase the hypotensive activities of Prazosin.
PrenylamineThe metabolism of Prenylamine can be increased when combined with Methohexital.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Methohexital.
PropacetamolThe metabolism of Propacetamol can be increased when combined with Methohexital.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Methohexital.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Methohexital.
PyridoxineThe metabolism of Methohexital can be increased when combined with Pyridoxine.
QuetiapineMethohexital may increase the hypotensive activities of Quetiapine.
QuinaprilMethohexital may increase the hypotensive activities of Quinapril.
RamiprilMethohexital may increase the hypotensive activities of Ramipril.
ReserpineMethohexital may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Methohexital can be increased when combined with Rifabutin.
RifampicinThe metabolism of Methohexital can be increased when combined with Rifampicin.
RifapentineThe metabolism of Methohexital can be increased when combined with Rifapentine.
RiociguatMethohexital may increase the hypotensive activities of Riociguat.
RisedronateThe metabolism of Risedronate can be increased when combined with Methohexital.
RopiniroleMethohexital may increase the sedative activities of Ropinirole.
RotigotineMethohexital may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Methohexital.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
SomatostatinThe risk or severity of adverse effects can be increased when Somatostatin is combined with Methohexital.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Methohexital.
SpironolactoneMethohexital may increase the hypotensive activities of Spironolactone.
SuvorexantMethohexital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
TelmisartanMethohexital may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Methohexital.
TerazosinMethohexital may increase the hypotensive activities of Terazosin.
ThalidomideMethohexital may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Methohexital.
TimololThe serum concentration of Timolol can be decreased when it is combined with Methohexital.
TizanidineMethohexital may increase the hypotensive activities of Tizanidine.
TorasemideMethohexital may increase the hypotensive activities of Torasemide.
TrandolaprilMethohexital may increase the hypotensive activities of Trandolapril.
TriamtereneMethohexital may increase the hypotensive activities of Triamterene.
TrichlormethiazideMethohexital may increase the orthostatic hypotensive activities of Trichlormethiazide.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Methohexital.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Methohexital.
Valproic AcidThe serum concentration of Methohexital can be increased when it is combined with Valproic Acid.
ValsartanMethohexital may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Methohexital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Methohexital.
WarfarinThe metabolism of Warfarin can be increased when combined with Methohexital.
ZolpidemMethohexital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By si...
Gene Name:
GABRA1
Uniprot ID:
P14867
Molecular Weight:
51801.395 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Koltchine VV, Ye Q, Finn SE, Harrison NL: Chimeric GABAA/glycine receptors: expression and barbiturate pharmacology. Neuropharmacology. 1996;35(9-10):1445-56. [PubMed:9014160 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:10