You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameAmobarbital
Accession NumberDB01351
TypeSmall Molecule
GroupsApproved, Illicit
Description

A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)

Structure
Thumb
Synonyms
5-Ethyl-5-(3-methylbutyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
5-Ethyl-5-(3-methylbutyl)barbituric acid
5-Ethyl-5-isoamylbarbituric acid
5-Ethyl-5-isopentylbarbituric acid
Amobarbital
Amylobarbitone
Amytal
Barbamil
Barbamyl
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amytal Sodium 500mgpowder for solution500 mgintramuscular; intravenousEli Lilly Canada Inc1939-12-312003-07-30Canada
Amytal Sodium Cap 60mgcapsule60 mgoralPharmascience Inc1951-12-312004-03-05Canada
Amytal Sodium Pulvule 222 0.2gmcapsule200 mgoralPharmascience Inc1939-12-312004-03-05Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Amytal Sodiuminjection, powder, lyophilized, for solution.5 g/5mLintramuscular; intravenousValeant Pharmaceuticals North America LLC2008-09-25Not applicableUs
Amytal Sodiuminjection, powder, lyophilized, for solution.5 g/5mLintramuscular; intravenousMarathon Pharmaceuticals, LLC2008-09-25Not applicableUs
International Brands
NameCompany
IsomytalNot Available
Brand mixtures
NameLabellerIngredients
Tuinal Pulvule 303Pharmascience Inc
Tuinal Pulvule 304Pharmascience Inc
Salts
Name/CASStructureProperties
Amobarbital sodium
ThumbNot applicableDBSALT001490
Categories
UNIIGWH6IJ239E
CAS number57-43-2
WeightAverage: 226.2722
Monoisotopic: 226.131742452
Chemical FormulaC11H18N2O3
InChI KeyInChIKey=VIROVYVQCGLCII-UHFFFAOYSA-N
InChI
InChI=1S/C11H18N2O3/c1-4-11(6-5-7(2)3)8(14)12-10(16)13-9(11)15/h7H,4-6H2,1-3H3,(H2,12,13,14,15,16)
IUPAC Name
5-ethyl-5-(3-methylbutyl)-1,3-diazinane-2,4,6-trione
SMILES
CCC1(CCC(C)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
IndicationNot Available
PharmacodynamicsNot Available
Mechanism of actionAmobarbital (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. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9254
Blood Brain Barrier+0.949
Caco-2 permeable-0.5913
P-glycoprotein substrateSubstrate0.6471
P-glycoprotein inhibitor INon-inhibitor0.5906
P-glycoprotein inhibitor IINon-inhibitor0.9426
Renal organic cation transporterNon-inhibitor0.9307
CYP450 2C9 substrateNon-substrate0.7591
CYP450 2D6 substrateNon-substrate0.9011
CYP450 3A4 substrateNon-substrate0.663
CYP450 1A2 substrateNon-inhibitor0.879
CYP450 2C9 inhibitorNon-inhibitor0.7603
CYP450 2D6 inhibitorNon-inhibitor0.9299
CYP450 2C19 inhibitorNon-inhibitor0.7269
CYP450 3A4 inhibitorNon-inhibitor0.9422
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9105
Ames testNon AMES toxic0.691
CarcinogenicityNon-carcinogens0.8925
BiodegradationNot ready biodegradable0.944
Rat acute toxicity2.9884 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9852
hERG inhibition (predictor II)Non-inhibitor0.8963
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionintramuscular; intravenous.5 g/5mL
Powder for solutionintramuscular; intravenous500 mg
Capsuleoral60 mg
Capsuleoral200 mg
Capsuleoral
Prices
Unit descriptionCostUnit
Amytal sodium 0.5 gram vial117.35USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point157 °CPhysProp
water solubility603 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.07HANSCH,C ET AL. (1995)
logS-2.57ADME Research, USCD
pKa7.84SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.897 mg/mLALOGPS
logP1.87ALOGPS
logP1.89ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity58 m3·mol-1ChemAxon
Polarizability23.45 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (8.4 KB)
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
MSMass Spectrum (Electron Ionization)splash10-0a4l-4900000000-8b443325c415e154ac85View in MoNA
1D NMR1H NMR SpectrumNot Available
1D NMR13C NMR SpectrumNot Available
References
Synthesis ReferenceNot Available
General References
  1. Kim HS, Wan X, Mathers DA, Puil E: Selective GABA-receptor actions of amobarbital on thalamic neurons. Br J Pharmacol. 2004 Oct;143(4):485-94. Epub 2004 Sep 20. [PubMed:15381635 ]
  2. Maynert EW: The alcoholic metabolites of pentobarbital and amobarbital in man. J Pharmacol Exp Ther. 1965 Oct;150(1):118-21. [PubMed:5855308 ]
  3. Tang BK, Kalow W, Grey AA: Amobarbital metabolism in man: N-glucoside formation. Res Commun Chem Pathol Pharmacol. 1978 Jul;21(1):45-53. [PubMed:684279 ]
  4. Soine PJ, Soine WH: High-performance liquid chromatographic determination of the diastereomers of 1-(beta-D-glucopyranosyl)amobarbital in urine. J Chromatogr. 1987 Nov 27;422:309-14. [PubMed:3437019 ]
  5. McCall WV: The addition of intravenous caffeine during an amobarbital interview. J Psychiatry Neurosci. 1992 Nov;17(5):195-7. [PubMed:1489761 ]
External Links
ATC CodesN05CA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Amobarbital.
AldesleukinAmobarbital may increase the hypotensive activities of Aldesleukin.
AmitriptylineThe metabolism of Amitriptyline can be increased when combined with Amobarbital.
AmlodipineThe metabolism of Amlodipine can be increased when combined with Amobarbital.
AmrinoneThe metabolism of Amrinone can be increased when combined with Amobarbital.
AzelastineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Amobarbital.
BepridilThe metabolism of Bepridil can be increased when combined with Amobarbital.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
BuprenorphineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
ChloramphenicolThe metabolism of Amobarbital can be decreased when combined with Chloramphenicol.
ChlorotrianiseneThe therapeutic efficacy of Chlorotrianisene can be decreased when used in combination with Amobarbital.
CyclosporineThe metabolism of Cyclosporine can be increased when combined with Amobarbital.
DicoumarolThe metabolism of Dicoumarol can be increased when combined with Amobarbital.
DoxycyclineThe serum concentration of Doxycycline can be decreased when it is combined with Amobarbital.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
EthanolAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FelbamateThe serum concentration of Amobarbital can be increased when it is combined with Felbamate.
FelodipineThe metabolism of Felodipine can be increased when combined with Amobarbital.
FlunarizineThe metabolism of Flunarizine can be increased when combined with Amobarbital.
GabapentinThe metabolism of Gabapentin can be increased when combined with Amobarbital.
GriseofulvinThe serum concentration of Griseofulvin can be decreased when it is combined with Amobarbital.
HydrocodoneAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
IsradipineThe metabolism of Isradipine can be increased when combined with Amobarbital.
LamotrigineThe metabolism of Lamotrigine can be increased when combined with Amobarbital.
LercanidipineThe metabolism of Lercanidipine can be increased when combined with Amobarbital.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Amobarbital.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
MethotrimeprazineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MetyrosineAmobarbital may increase the sedative activities of Metyrosine.
MianserinMianserin may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
MirtazapineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
NicardipineThe metabolism of Nicardipine can be increased when combined with Amobarbital.
NicotineThe metabolism of Nicotine can be increased when combined with Amobarbital.
NimodipineThe metabolism of Nimodipine can be increased when combined with Amobarbital.
NisoldipineThe metabolism of Nisoldipine can be increased when combined with Amobarbital.
NitrendipineThe metabolism of Nitrendipine can be increased when combined with Amobarbital.
NorethisteroneThe therapeutic efficacy of Norethindrone can be decreased when used in combination with Amobarbital.
OrphenadrineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Amobarbital is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
PerhexilineThe metabolism of Perhexiline can be increased when combined with Amobarbital.
PethidineAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Pethidine.
PramipexoleAmobarbital may increase the sedative activities of Pramipexole.
PrenylamineThe metabolism of Prenylamine can be increased when combined with Amobarbital.
PrimidoneThe risk or severity of adverse effects can be increased when Primidone is combined with Amobarbital.
PropacetamolThe metabolism of Propacetamol can be increased when combined with Amobarbital.
PyridoxineThe metabolism of Amobarbital can be increased when combined with Pyridoxine.
RifabutinThe metabolism of Amobarbital can be increased when combined with Rifabutin.
RisedronateThe metabolism of Risedronate can be increased when combined with Amobarbital.
RopiniroleAmobarbital may increase the sedative activities of Ropinirole.
RotigotineAmobarbital may increase the sedative activities of Rotigotine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Amobarbital.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
SomatostatinThe risk or severity of adverse effects can be increased when Somatostatin is combined with Amobarbital.
SuvorexantAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
TeniposideThe serum concentration of Teniposide can be decreased when it is combined with Amobarbital.
ThalidomideAmobarbital 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 Amobarbital.
TrichlormethiazideAmobarbital may increase the orthostatic hypotensive activities of Trichlormethiazide.
UlipristalThe serum concentration of Ulipristal can be decreased when it is combined with Amobarbital.
Valproic AcidThe serum concentration of Amobarbital can be increased when it is combined with Valproic Acid.
ValsartanAmobarbital may increase the hypotensive activities of Valsartan.
VerapamilThe metabolism of Verapamil can be increased when combined with Amobarbital.
VoriconazoleThe serum concentration of Voriconazole can be decreased when it is combined with Amobarbital.
ZolpidemAmobarbital may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
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. 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 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Comments
comments powered by Disqus
Drug created on July 06, 2007 13:48 / Updated on August 17, 2016 12:23