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Identification
NameButethal
Accession NumberDB01353
TypeSmall Molecule
GroupsApproved, Illicit
Description

Butethal is a sedative and a hypnotic drug.

Structure
Thumb
Synonyms
Butethal
Butobarbital
Butobarbitone
Neonal
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
NeonalNot Available
SonerylNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIOHZ8QAW6YC
CAS number77-28-1
WeightAverage: 212.2456
Monoisotopic: 212.116092388
Chemical FormulaC10H16N2O3
InChI KeyInChIKey=STDBAQMTJLUMFW-UHFFFAOYSA-N
InChI
InChI=1S/C10H16N2O3/c1-3-5-6-10(4-2)7(13)11-9(15)12-8(10)14/h3-6H2,1-2H3,(H2,11,12,13,14,15)
IUPAC Name
5-butyl-5-ethyl-1,3-diazinane-2,4,6-trione
SMILES
CCCCC1(CC)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 DescriptorsNot Available
Pharmacology
IndicationFor the treatment of insomnia.
PharmacodynamicsButethal (also known as butobarbitone and butobarbital) belongs to a group of medicines called the barbiturates. It is thought to act on receptors in the brain (GABA receptors) causing the release of the chemical GABA. This chemical inhibits certain areas of the brain resulting in sleepiness.
Mechanism of actionButethal 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. All of these effects are associated with marked decreases in GABA-sensitive neuronal calcium conductance (gCa). The net result of barbiturate action is acute potentiation of inhibitory GABAergic tone. Barbiturates also act through potent (if less well characterized) and direct inhibition of excitatory AMPA-type glutamate receptors, resulting in a profound suppression of glutamatergic neurotransmission.
Related Articles
AbsorptionRapidly absorbed following oral administration.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic.

Route of eliminationNot Available
Half life37 hours
ClearanceNot Available
ToxicitySigns of overdose include confusion (severe), decrease in or loss of reflexes, drowsiness (severe), fever, irritability (continuing), low body temperature, poor judgment, shortness of breath or slow or troubled breathing, slow heartbeat, slurred speech, staggering, trouble in sleeping, unusual movements of the eyes, weakness (severe).
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+0.9222
Blood Brain Barrier+0.9712
Caco-2 permeable-0.5923
P-glycoprotein substrateSubstrate0.601
P-glycoprotein inhibitor INon-inhibitor0.684
P-glycoprotein inhibitor IINon-inhibitor0.968
Renal organic cation transporterNon-inhibitor0.9116
CYP450 2C9 substrateNon-substrate0.7899
CYP450 2D6 substrateNon-substrate0.9146
CYP450 3A4 substrateNon-substrate0.739
CYP450 1A2 substrateNon-inhibitor0.9149
CYP450 2C9 inhibitorNon-inhibitor0.8109
CYP450 2D6 inhibitorNon-inhibitor0.9343
CYP450 2C19 inhibitorNon-inhibitor0.7678
CYP450 3A4 inhibitorNon-inhibitor0.9762
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9528
Ames testNon AMES toxic0.6449
CarcinogenicityNon-carcinogens0.8975
BiodegradationNot ready biodegradable0.947
Rat acute toxicity3.0258 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9709
hERG inhibition (predictor II)Non-inhibitor0.8922
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 point128.5 °CPhysProp
water solubility4880 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.73HANSCH,C ET AL. (1995)
logS-1.64ADME Research, USCD
pKa7.86SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility1.27 mg/mLALOGPS
logP1.65ALOGPS
logP1.61ChemAxon
logS-2.2ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity53.45 m3·mol-1ChemAxon
Polarizability21.62 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 CodesN05CA03
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 Butethal.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Butethal.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Butethal.
AcetazolamideButethal may increase the hypotensive activities of Acetazolamide.
AldesleukinButethal may increase the hypotensive activities of Aldesleukin.
AliskirenButethal may increase the hypotensive activities of Aliskiren.
AmilorideButethal may increase the hypotensive activities of Amiloride.
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Butethal.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Butethal.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Butethal.
AmoxapineThe metabolism of Amoxapine can be increased when combined with Butethal.
Amyl NitriteButethal may increase the hypotensive activities of Amyl Nitrite.
ApraclonidineButethal may increase the hypotensive activities of Apraclonidine.
AtenololButethal may increase the hypotensive activities of Atenolol.
Azilsartan medoxomilButethal may increase the hypotensive activities of Azilsartan medoxomil.
BenazeprilButethal may increase the hypotensive activities of Benazepril.
BendroflumethiazideButethal may increase the orthostatic hypotensive activities of Bendroflumethiazide.
BetaxololThe serum concentration of Betaxolol can be decreased when it is combined with Butethal.
BisoprololThe serum concentration of Bisoprolol can be decreased when it is combined with Butethal.
BretyliumButethal may increase the hypotensive activities of Bretylium.
BrimonidineButethal may increase the hypotensive activities of Brimonidine.
BumetanideButethal may increase the hypotensive activities of Bumetanide.
ButalbitalThe metabolism of Butalbital can be increased when combined with Butethal.
CaffeineThe metabolism of Caffeine can be increased when combined with Butethal.
CanagliflozinButethal may increase the hypotensive activities of Canagliflozin.
CandesartanButethal may increase the hypotensive activities of Candesartan.
CaptoprilButethal may increase the hypotensive activities of Captopril.
CarteololThe serum concentration of Carteolol can be decreased when it is combined with Butethal.
CarvedilolThe serum concentration of Carvedilol can be decreased when it is combined with Butethal.
ChloramphenicolThe metabolism of Butethal can be decreased when combined with Chloramphenicol.
ChlorothiazideButethal may increase the orthostatic hypotensive activities of Chlorothiazide.
ChlorthalidoneButethal may increase the orthostatic hypotensive activities of Chlorthalidone.
CilazaprilButethal may increase the hypotensive activities of Cilazapril.
ClevidipineButethal may increase the hypotensive activities of Clevidipine.
ClomipramineThe metabolism of Clomipramine can be increased when combined with Butethal.
ClonidineButethal may increase the hypotensive activities of Clonidine.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Butethal.
DapagliflozinButethal may increase the hypotensive activities of Dapagliflozin.
DesipramineThe metabolism of Desipramine can be increased when combined with Butethal.
DesogestrelThe therapeutic efficacy of Desogestrel can be decreased when used in combination with Butethal.
DexmedetomidineButethal may increase the hypotensive activities of Dexmedetomidine.
DiclofenamideButethal may increase the hypotensive activities of Diclofenamide.
DienogestThe therapeutic efficacy of Dienogest can be decreased when used in combination with Butethal.
DiltiazemThe metabolism of Diltiazem can be increased when combined with Butethal.
DinutuximabButethal may increase the hypotensive activities of Dinutuximab.
DipyridamoleButethal may increase the hypotensive activities of Dipyridamole.
DoxazosinButethal may increase the hypotensive activities of Doxazosin.
DoxepinThe metabolism of Doxepin can be increased when combined with Butethal.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Butethal.
DrospirenoneThe therapeutic efficacy of Drospirenone can be decreased when used in combination with Butethal.
EmpagliflozinButethal may increase the hypotensive activities of Empagliflozin.
EnalaprilButethal may increase the hypotensive activities of Enalapril.
EnalaprilatButethal may increase the hypotensive activities of Enalaprilat.
EplerenoneButethal may increase the hypotensive activities of Eplerenone.
EprosartanButethal may increase the hypotensive activities of Eprosartan.
EsmololThe serum concentration of Esmolol can be decreased when it is combined with Butethal.
EstradiolThe therapeutic efficacy of Estradiol can be decreased when used in combination with Butethal.
Etacrynic acidButethal may increase the hypotensive activities of Ethacrynic acid.
Ethinyl EstradiolThe therapeutic efficacy of Ethinyl Estradiol can be decreased when used in combination with Butethal.
Ethynodiol diacetateThe therapeutic efficacy of Ethynodiol can be decreased when used in combination with Butethal.
EtonogestrelThe therapeutic efficacy of Etonogestrel can be decreased when used in combination with Butethal.
FelbamateThe serum concentration of Butethal can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Butethal.
FosinoprilButethal may increase the hypotensive activities of Fosinopril.
FurosemideButethal may increase the hypotensive activities of Furosemide.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Butethal.
GuanfacineButethal may increase the hypotensive activities of Guanfacine.
HydralazineButethal may increase the hypotensive activities of Hydralazine.
HydrochlorothiazideButethal may increase the orthostatic hypotensive activities of Hydrochlorothiazide.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Butethal.
ImipramineThe metabolism of Imipramine can be increased when combined with Butethal.
IndapamideButethal may increase the orthostatic hypotensive activities of Indapamide.
IrbesartanButethal may increase the hypotensive activities of Irbesartan.
IsomethepteneThe metabolism of Isometheptene can be increased when combined with Butethal.
IsosorbideButethal may increase the hypotensive activities of Isosorbide.
Isosorbide DinitrateButethal may increase the hypotensive activities of Isosorbide Dinitrate.
Isosorbide MononitrateButethal may increase the hypotensive activities of Isosorbide Mononitrate.
IsoxsuprineButethal may increase the hypotensive activities of Isoxsuprine.
IsradipineThe metabolism of Isradipine can be increased when combined with Butethal.
LabetalolThe serum concentration of Labetalol can be decreased when it is combined with Butethal.
LamotrigineThe serum concentration of Lamotrigine can be decreased when it is combined with Butethal.
LevobunololButethal may increase the hypotensive activities of Levobunolol.
LevonorgestrelThe therapeutic efficacy of Levonorgestrel can be decreased when used in combination with Butethal.
LisinoprilButethal may increase the hypotensive activities of Lisinopril.
LosartanButethal may increase the hypotensive activities of Losartan.
MannitolButethal may increase the hypotensive activities of Mannitol.
MecamylamineButethal may increase the hypotensive activities of Mecamylamine.
Medroxyprogesterone acetateThe therapeutic efficacy of Medroxyprogesterone Acetate can be decreased when used in combination with Butethal.
MestranolThe therapeutic efficacy of Mestranol can be decreased when used in combination with Butethal.
MetforminButethal may increase the hypotensive activities of Metformin.
MethazolamideButethal may increase the hypotensive activities of Methazolamide.
MethyclothiazideButethal may increase the orthostatic hypotensive activities of Methyclothiazide.
MethyldopaButethal may increase the hypotensive activities of Methyldopa.
MetipranololButethal may increase the hypotensive activities of Metipranolol.
MetolazoneButethal may increase the orthostatic hypotensive activities of Metolazone.
MetoprololThe serum concentration of Metoprolol can be decreased when it is combined with Butethal.
MinoxidilButethal may increase the hypotensive activities of Minoxidil.
MoexiprilButethal may increase the hypotensive activities of Moexipril.
NadololButethal may increase the hypotensive activities of Nadolol.
NebivololThe serum concentration of Nebivolol can be decreased when it is combined with Butethal.
NesiritideButethal may increase the hypotensive activities of Nesiritide.
NicardipineThe metabolism of Nicardipine can be increased when combined with Butethal.
NifedipineThe metabolism of Nifedipine can be increased when combined with Butethal.
NimodipineThe metabolism of Nimodipine can be increased when combined with Butethal.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Butethal.
NitroglycerinButethal may increase the hypotensive activities of Nitroglycerin.
NitroprussideButethal may increase the hypotensive activities of Nitroprusside.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Butethal.
NorgestimateThe therapeutic efficacy of Norgestimate can be decreased when used in combination with Butethal.
NortriptylineThe metabolism of Nortriptyline can be increased when combined with Butethal.
OlmesartanButethal may increase the hypotensive activities of Olmesartan.
PapaverineButethal may increase the hypotensive activities of Papaverine.
PenbutololThe serum concentration of Penbutolol can be decreased when it is combined with Butethal.
PerindoprilButethal may increase the hypotensive activities of Perindopril.
PethidineButethal 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 Butethal.
PrazosinButethal may increase the hypotensive activities of Prazosin.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Butethal.
PropranololThe serum concentration of Propranolol can be decreased when it is combined with Butethal.
ProtriptylineThe metabolism of Protriptyline can be increased when combined with Butethal.
PyridoxineThe metabolism of Butethal can be increased when combined with Pyridoxine.
QuetiapineButethal may increase the hypotensive activities of Quetiapine.
QuinaprilButethal may increase the hypotensive activities of Quinapril.
RamiprilButethal may increase the hypotensive activities of Ramipril.
ReserpineButethal may increase the hypotensive activities of Reserpine.
RifabutinThe metabolism of Butethal can be increased when combined with Rifabutin.
RifampicinThe metabolism of Butethal can be increased when combined with Rifampicin.
RifapentineThe metabolism of Butethal can be increased when combined with Rifapentine.
RiociguatButethal may increase the hypotensive activities of Riociguat.
SotalolThe serum concentration of Sotalol can be decreased when it is combined with Butethal.
SpironolactoneButethal may increase the hypotensive activities of Spironolactone.
TelmisartanButethal may increase the hypotensive activities of Telmisartan.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Butethal.
TerazosinButethal may increase the hypotensive activities of Terazosin.
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Butethal.
TimololThe serum concentration of Timolol can be decreased when it is combined with Butethal.
TizanidineButethal may increase the hypotensive activities of Tizanidine.
TorasemideButethal may increase the hypotensive activities of Torasemide.
TrandolaprilButethal may increase the hypotensive activities of Trandolapril.
TriamtereneButethal may increase the hypotensive activities of Triamterene.
TrimipramineThe metabolism of Trimipramine can be increased when combined with Butethal.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Butethal.
Valproic AcidThe serum concentration of Butethal can be increased when it is combined with Valproic Acid.
ValsartanButethal may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Butethal.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Butethal.
WarfarinThe metabolism of Warfarin can be increased when combined with Butethal.
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. 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 ]
  6. 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 ]
  7. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
potentiator
General Function:
Inhibitory extracellular ligand-gated ion channel activity
Specific Function:
GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
Gene Name:
GABRA2
Uniprot ID:
P47869
Molecular Weight:
51325.85 Da
References
  1. 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