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Identification
NameHeptabarbital
Accession NumberDB01354
TypeSmall Molecule
GroupsApproved
Description

Heptabarbital is an intermediate or short term barbiturate used mainly for sedation and hypnosis.

Structure
Thumb
Synonyms
Heptabarb
Heptabarbital
Heptabarbitone
Heptabarbum
Heptadorm
Heptamal
Heptamalum
Heptbarbital
Medapan
Medomine
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
MedominGeigy
MedomineCiba
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIV10R70ML23
CAS number509-86-4
WeightAverage: 250.2936
Monoisotopic: 250.131742452
Chemical FormulaC13H18N2O3
InChI KeyInChIKey=PAZQYDJGLKSCSI-UHFFFAOYSA-N
InChI
InChI=1S/C13H18N2O3/c1-2-13(9-7-5-3-4-6-8-9)10(16)14-12(18)15-11(13)17/h7H,2-6,8H2,1H3,(H2,14,15,16,17,18)
IUPAC Name
5-(cyclohept-1-en-1-yl)-5-ethyl-1,3-diazinane-2,4,6-trione
SMILES
CCC1(C(=O)NC(=O)NC1=O)C1=CCCCCC1
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 DescriptorsNot Available
Pharmacology
IndicationUsed mainly for sedation and hypnosis.
PharmacodynamicsNot Available
Mechanism of actionHeptabarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Heptabarbital also appears to bind neuronal nicotinic acetylcholine receptors.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySymptoms of an overdose typically include sluggishness, incoordination, difficulty in thinking, slowness of speech, faulty judgment, drowsiness or coma, shallow breathing, staggering, and in severe cases 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+0.9655
Blood Brain Barrier+0.9387
Caco-2 permeable-0.5831
P-glycoprotein substrateSubstrate0.6344
P-glycoprotein inhibitor INon-inhibitor0.5941
P-glycoprotein inhibitor IINon-inhibitor0.9689
Renal organic cation transporterNon-inhibitor0.8902
CYP450 2C9 substrateNon-substrate0.7692
CYP450 2D6 substrateNon-substrate0.8793
CYP450 3A4 substrateNon-substrate0.6914
CYP450 1A2 substrateNon-inhibitor0.7892
CYP450 2C9 inhibitorNon-inhibitor0.7694
CYP450 2D6 inhibitorNon-inhibitor0.9057
CYP450 2C19 inhibitorNon-inhibitor0.7389
CYP450 3A4 inhibitorNon-inhibitor0.9666
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8083
Ames testAMES toxic0.5298
CarcinogenicityNon-carcinogens0.8893
BiodegradationNot ready biodegradable0.9686
Rat acute toxicity1.7309 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9588
hERG inhibition (predictor II)Non-inhibitor0.8583
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 point174U.S. Patent 2,501,551.
water solubility250 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.03HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility0.324 mg/mLALOGPS
logP2.41ALOGPS
logP1.91ChemAxon
logS-2.9ALOGPS
pKa (Strongest Acidic)8.14ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity66.25 m3·mol-1ChemAxon
Polarizability25.86 Å3ChemAxon
Number of Rings2ChemAxon
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 Reference

U.S. Patent 2,501,551.

General ReferencesNot Available
External Links
ATC CodesN05CA11
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololThe serum concentration of Acebutolol can be decreased when it is combined with Heptabarbital.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Heptabarbital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Heptabarbital.
AcetazolamideHeptabarbital may increase the hypotensive activities of Acetazolamide.
AldesleukinHeptabarbital may increase the hypotensive activities of Aldesleukin.
AliskirenHeptabarbital may increase the hypotensive activities of Aliskiren.
AmilorideHeptabarbital may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Heptabarbital.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Heptabarbital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Heptabarbital.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Heptabarbital.
Amyl NitriteHeptabarbital may increase the hypotensive activities of Amyl Nitrite.
ApraclonidineHeptabarbital may increase the hypotensive activities of Apraclonidine.
AtenololHeptabarbital may increase the hypotensive activities of Atenolol.
Azilsartan medoxomilHeptabarbital may increase the hypotensive activities of Azilsartan medoxomil.
BenazeprilHeptabarbital may increase the hypotensive activities of Benazepril.
BendroflumethiazideHeptabarbital may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Heptabarbital.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Heptabarbital.
BretyliumHeptabarbital may increase the hypotensive activities of Bretylium.
BrimonidineHeptabarbital may increase the hypotensive activities of Brimonidine.
BumetanideHeptabarbital may increase the hypotensive activities of Bumetanide.
ButalbitalThe metabolism of Butalbital can be increased when combined with Heptabarbital.
CaffeineThe metabolism of Caffeine can be increased when combined with Heptabarbital.
CanagliflozinHeptabarbital may increase the hypotensive activities of Canagliflozin.
CandesartanHeptabarbital may increase the hypotensive activities of Candesartan.
CaptoprilHeptabarbital may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Heptabarbital.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Heptabarbital.
ChloramphenicolThe metabolism of Heptabarbital can be decreased when combined with Chloramphenicol.
ChlorothiazideHeptabarbital may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorthalidoneHeptabarbital may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilHeptabarbital may increase the hypotensive activities of Cilazapril.
ClevidipineHeptabarbital may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Heptabarbital.
ClonidineHeptabarbital may increase the hypotensive activities of Clonidine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Heptabarbital.
DapagliflozinHeptabarbital may increase the hypotensive activities of Dapagliflozin.
DesipramineThe metabolism of Desipramine can be increased when combined with Heptabarbital.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Heptabarbital.
DexmedetomidineHeptabarbital may increase the hypotensive activities of Dexmedetomidine.
DiclofenamideHeptabarbital may increase the hypotensive activities of Diclofenamide.
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Heptabarbital.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Heptabarbital.
DinutuximabHeptabarbital may increase the hypotensive activities of Dinutuximab.
DipyridamoleHeptabarbital may increase the hypotensive activities of Dipyridamole.
DoxazosinHeptabarbital may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Heptabarbital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Heptabarbital.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Heptabarbital.
EmpagliflozinHeptabarbital may increase the hypotensive activities of Empagliflozin.
EnalaprilHeptabarbital may increase the hypotensive activities of Enalapril.
EnalaprilatHeptabarbital may increase the hypotensive activities of Enalaprilat.
EplerenoneHeptabarbital may increase the hypotensive activities of Eplerenone.
EprosartanHeptabarbital may increase the hypotensive activities of Eprosartan.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Heptabarbital.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Heptabarbital.
Etacrynic acidHeptabarbital may increase the hypotensive activities of Ethacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Ethinyl Estradiol can be decreased when used in combination with Heptabarbital.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Heptabarbital.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Heptabarbital.
FelbamateThe serum concentration of Heptabarbital can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Heptabarbital.
FosinoprilHeptabarbital may increase the hypotensive activities of Fosinopril.
FurosemideHeptabarbital may increase the hypotensive activities of Furosemide.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Heptabarbital.
GuanfacineHeptabarbital may increase the hypotensive activities of Guanfacine.
HydralazineHeptabarbital may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideHeptabarbital may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Heptabarbital.
ImipramineThe metabolism of Imipramine can be increased when combined with Heptabarbital.
IndapamideHeptabarbital may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanHeptabarbital may increase the hypotensive activities of Irbesartan.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Heptabarbital.
IsosorbideHeptabarbital may increase the hypotensive activities of Isosorbide.
Isosorbide DinitrateHeptabarbital may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitrateHeptabarbital may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprineHeptabarbital may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Heptabarbital.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Heptabarbital.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Heptabarbital.
LevobunololHeptabarbital may increase the hypotensive activities of Levobunolol.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Heptabarbital.
LisinoprilHeptabarbital may increase the hypotensive activities of Lisinopril.
LosartanHeptabarbital may increase the hypotensive activities of Losartan.
MannitolHeptabarbital may increase the hypotensive activities of Mannitol.
MecamylamineHeptabarbital may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Heptabarbital.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Heptabarbital.
MetforminHeptabarbital may increase the hypotensive activities of Metformin.
MethazolamideHeptabarbital may increase the hypotensive activities of Methazolamide.
MethyclothiazideHeptabarbital may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaHeptabarbital may increase the hypotensive activities of Methyldopa.
MetipranololHeptabarbital may increase the hypotensive activities of Metipranolol.
MetolazoneHeptabarbital may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Heptabarbital.
MinoxidilHeptabarbital may increase the hypotensive activities of Minoxidil.
MoexiprilHeptabarbital may increase the hypotensive activities of Moexipril.
NadololHeptabarbital may increase the hypotensive activities of Nadolol.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Heptabarbital.
NesiritideHeptabarbital may increase the hypotensive activities of Nesiritide.
NicardipineThe metabolism of Nicardipine can be increased when combined with Heptabarbital.
NifedipineThe metabolism of Nifedipine can be increased when combined with Heptabarbital.
NimodipineThe metabolism of Nimodipine can be increased when combined with Heptabarbital.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Heptabarbital.
NitroglycerinHeptabarbital may increase the hypotensive activities of Nitroglycerin.
NitroprussideHeptabarbital may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Heptabarbital.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Heptabarbital.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Heptabarbital.
OlmesartanHeptabarbital may increase the hypotensive activities of Olmesartan.
PapaverineHeptabarbital may increase the hypotensive activities of Papaverine.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Heptabarbital.
PerindoprilHeptabarbital may increase the hypotensive activities of Perindopril.
PethidineHeptabarbital 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 Heptabarbital.
PrazosinHeptabarbital may increase the hypotensive activities of Prazosin.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Heptabarbital.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Heptabarbital.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Heptabarbital.
PyridoxineThe metabolism of Heptabarbital can be increased when combined with Pyridoxine.
QuetiapineHeptabarbital may increase the hypotensive activities of Quetiapine.
QuinaprilHeptabarbital may increase the hypotensive activities of Quinapril.
RamiprilHeptabarbital may increase the hypotensive activities of Ramipril.
ReserpineHeptabarbital may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Heptabarbital can be increased when combined with Rifabutin.
RifampicinThe metabolism of Heptabarbital can be increased when combined with Rifampicin.
RifapentineThe metabolism of Heptabarbital can be increased when combined with Rifapentine.
RiociguatHeptabarbital may increase the hypotensive activities of Riociguat.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Heptabarbital.
SpironolactoneHeptabarbital may increase the hypotensive activities of Spironolactone.
TelmisartanHeptabarbital may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Heptabarbital.
TerazosinHeptabarbital may increase the hypotensive activities of Terazosin.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Heptabarbital.
TimololThe serum concentration of Timolol can be decreased when it is combined with Heptabarbital.
TizanidineHeptabarbital may increase the hypotensive activities of Tizanidine.
TorasemideHeptabarbital may increase the hypotensive activities of Torasemide.
TrandolaprilHeptabarbital may increase the hypotensive activities of Trandolapril.
TriamtereneHeptabarbital may increase the hypotensive activities of Triamterene.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Heptabarbital.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Heptabarbital.
Valproic AcidThe serum concentration of Heptabarbital can be increased when it is combined with Valproic Acid.
ValsartanHeptabarbital may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Heptabarbital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Heptabarbital.
WarfarinThe metabolism of Warfarin can be increased when combined with Heptabarbital.
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. 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 ]
  4. 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 ]
  5. Goodman, Louis Sanford;Brunton, Laurence L.;Chabner, Bruce;Knollman, Bjorn (2011). The Pharmacological Basis of Therapeutics (12th ed.). McGraw-Hill Professional Publishing. [ISBN:978-0-07-162442-8 ]
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 ]
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Drug created on July 06, 2007 13:49 / Updated on August 17, 2016 12:23