Identification

Name
Butabarbital
Accession Number
DB00237
Description

Butabarbital, or Butisol, is a fast onset barbiturate with short duration of action compared to other barbiturates.1,12 This makes butabarbital a useful drug for treating severe insomnia and pre-operative anxiety.1,12 Butabarbital is less commonly used in recent years, as more patients are typically prescribed benzodiazepines.3 Its short duration of action gives butabarbital a high abuse potential, comparable to secobarbital.1,2

Butabarbital was granted FDA approval on 5 June 1939.12

Type
Small Molecule
Groups
Approved, Illicit
Structure
Thumb
Weight
Average: 212.2456
Monoisotopic: 212.116092388
Chemical Formula
C10H16N2O3
Synonyms
  • 5-ethyl-5-(1-methylpropyl)-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-ethyl-5-(1-methylpropyl)barbituric acid
  • 5-sec-butyl-5-ethyl-2,4,6(1H,3H,5H)-pyrimidinetrione
  • 5-sec-butyl-5-ethylbarbituric acid
  • 5-sec-butyl-5-ethylpyrimidine-2,4,6(1H,3H,5H)-trione
  • Butabarbital
  • Secbutabarbital
  • Secbutabarbitale
  • Secbutabarbitalum

Pharmacology

Indication

Butabarbital is indicated for use as a sedative or hypnotic.12 Butabarbital should not be used to treat insomnia for longer than 2 weeks.12

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Butabarbital potentiates GABAergic neurons while inhibiting neuronal acetylcholine and glutamate receptors to produce sedation.8,10 Butabarbital is an intermediate acting barbiturate with a duration of action of approximately 6-8 hours.12 The therapeutic index is quite wide as doses vary considerably from patient to patient.12 Patients should be counselled regarding the risk of worsening insomnia, drowsiness, falls, and complex behaviour while not fully awake.12

Mechanism of action

Barbiturates like butabarbital potentiate GABA-A receptors and inhibit receptors for neuronal acetylcholine, and kainate.8,10 GABA-A receptors are predominantly on the post-synaptic membrane, and upon activation, open chloride channels to hyperpolarize the neuron and decreased firing rate.9 Potentiation of GABAergic neurons produces sedation.9 Inhibition of neuronal acetylcholine receptors10 and glutamate receptors of the kainate subtype11 desensitize their respective neurons, producing sedation.

TargetActionsOrganism
AGABA(A) Receptor
positive allosteric modulator
Humans
UNeuronal Acetylcholine (nACh) Receptor Subunits
inhibitor
Humans
UGlutamate receptor 1
antagonist
Humans
UGlutamate receptor 2
antagonist
Humans
UGlutamate receptor 3
antagonist
Humans
UGlutamate receptor 4
antagonist
Humans
UGlutamate receptor ionotropic, kainate 1
antagonist
Humans
UGlutamate receptor ionotropic, kainate 2
antagonist
Humans
UGlutamate receptor ionotropic, kainate 3
antagonist
Humans
UGlutamate receptor ionotropic, kainate 4
antagonist
Humans
UGlutamate receptor ionotropic, kainate 5
antagonist
Humans
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

Data regarding the protein binding of butbarbital is not readily available.12 However, barbiturates generally bind to serum albumin.4

Metabolism

Data regarding the metabolism of butabarbital in humans are not readily available. In dogs, butabarbital undergoes metabolism to a final glucuronide metabolite.7

Route of elimination

Barbiturates such as butabarbital are predominantly eliminated in the urine.5,6,12 In dogs, 3-5% of the dose is eliminated in the urine as the unchanged parent compound.7

Half-life

Butabarbital has a half life of 100 hours but its duration of action is only 6-8 hours.12

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Patients experiencing an overdose may present with unsteady gait, slurred speech, nystagmus, confusion, poor judgement, irritability, and insomnia.12 Acute overdoses may present as CNS depression, respiratory depression, oligouria, tachycardia, hypotension, low body temperature, coma, and shock.12 An extreme overdose can lead to a flat EEG, resembling death, that is reversible provided there is no hypoxic brain damage.12 Overdose can be treated with symptomatic and supportive treatment.12

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirButabarbital may decrease the excretion rate of Abacavir which could result in a higher serum level.
AcarboseButabarbital may decrease the excretion rate of Acarbose which could result in a higher serum level.
AcebutololButabarbital may increase the hypotensive activities of Acebutolol.
AceclofenacAceclofenac may decrease the excretion rate of Butabarbital which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Butabarbital which could result in a higher serum level.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Butabarbital.
AcetaminophenThe metabolism of Acetaminophen can be increased when combined with Butabarbital.
AcetazolamideThe risk or severity of adverse effects can be increased when Butabarbital is combined with Acetazolamide.
AcetophenazineThe risk or severity of adverse effects can be increased when Butabarbital is combined with Acetophenazine.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Butabarbital which could result in a higher serum level.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Avoid alcohol. Concomitant use of alcohol and barbiturates may lead to increased.

Products

Product Ingredients
IngredientUNIICASInChI Key
Butabarbital sodium9WTD50I918143-81-7QORQZMBCPRBCAB-UHFFFAOYSA-M
International/Other Brands
Butalan / Butisol / Sarisol No. 2
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Butisol SodiumTablet50 mg/1OralMedPointe Pharmaceuticals2007-08-022007-08-02US flag
Butisol SodiumTablet30 mg/1OralMEDA Pharmaceuticals1939-08-012020-01-31US flag
Butisol SodiumSolution30 mg/5mLOralMedPointe Pharmaceuticals2007-08-022007-08-02US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Phenazopyridine Hydrochloride, Hyoscyamine Hydrobromide, and ButabarbitalButabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1)Tablet, coatedOralPhysicians Total Care, Inc.2004-09-032011-06-30US flag
Phenazopyridine PlusButabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1)Tablet, coatedOralBreckenridge Pharmaceutical, Inc.2005-03-012011-02-28US flag
Pyrelle H.B.Butabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1)TabletOralAzur Pharma, Inc.2004-01-012010-06-01US flag

Categories

ATC Codes
N05CB01 — Combinations of barbiturates
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This 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.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazines
Sub Class
Pyrimidines and pyrimidine derivatives
Direct Parent
Barbituric acid derivatives
Alternative Parents
N-acyl ureas / Diazinanes / Dicarboximides / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
1,3-diazinane / Aliphatic heteromonocyclic compound / Azacycle / Barbiturate / Carbonic acid derivative / Carbonyl group / Carboxylic acid derivative / Dicarboximide / Hydrocarbon derivative / N-acyl urea
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
barbiturates (CHEBI:3228)

Chemical Identifiers

UNII
P0078O25A9
CAS number
125-40-6
InChI Key
ZRIHAIZYIMGOAB-UHFFFAOYSA-N
InChI
InChI=1S/C10H16N2O3/c1-4-6(3)10(5-2)7(13)11-9(15)12-8(10)14/h6H,4-5H2,1-3H3,(H2,11,12,13,14,15)
IUPAC Name
5-(butan-2-yl)-5-ethyl-1,3-diazinane-2,4,6-trione
SMILES
CCC(C)C1(CC)C(=O)NC(=O)NC1=O

References

General References
  1. DRIPPS RD: Selective utilization of barbiturates as illustrated by a study of butabarbital sodium. J Am Med Assoc. 1948 Jan 15;139(3):148-50. [PubMed:18103391]
  2. Zawertailo LA, Busto UE, Kaplan HL, Greenblatt DJ, Sellers EM: Comparative abuse liability and pharmacological effects of meprobamate, triazolam, and butabarbital. J Clin Psychopharmacol. 2003 Jun;23(3):269-80. doi: 10.1097/01.jcp.0000084031.22282.24. [PubMed:12826989]
  3. Lopez-Munoz F, Ucha-Udabe R, Alamo C: The history of barbiturates a century after their clinical introduction. Neuropsychiatr Dis Treat. 2005 Dec;1(4):329-43. [PubMed:18568113]
  4. GOLDBAUM LR, SMITH PK: The interaction of barbiturates with serum albumin and its possible relation to their disposition and pharmacological actions. J Pharmacol Exp Ther. 1954 Jun;111(2):197-209. [PubMed:13175102]
  5. Martin-Biosca Y, Sagrado S, Villaneuva-Camanas RM, Medina-Hernandez MJ: Determination of barbiturates in urine by micellar liquid chromatography and direct injection of sample. J Pharm Biomed Anal. 1999 Nov;21(2):331-8. doi: 10.1016/s0731-7085(99)00147-8. [PubMed:10703988]
  6. Tang-Liu DD, Tozer TN, Riegelman S: Dependence of renal clearance on urine flow: a mathematical model and its application. J Pharm Sci. 1983 Feb;72(2):154-8. doi: 10.1002/jps.2600720215. [PubMed:6834253]
  7. MAYNERT EW, LOSIN L: The metabolism of butabarbital (butisol) in the dog. J Pharmacol Exp Ther. 1955 Nov;115(3):275-82. [PubMed:13272177]
  8. 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]
  9. Davies JA: Mechanisms of action of antiepileptic drugs. Seizure. 1995 Dec;4(4):267-71. doi: 10.1016/s1059-1311(95)80003-4. [PubMed:8719918]
  10. Dodson BA, Braswell LM, Miller KW: Barbiturates bind to an allosteric regulatory site on nicotinic acetylcholine receptor-rich membranes. Mol Pharmacol. 1987 Jul;32(1):119-26. [PubMed:3600612]
  11. Jane DE, Lodge D, Collingridge GL: Kainate receptors: pharmacology, function and therapeutic potential. Neuropharmacology. 2009 Jan;56(1):90-113. doi: 10.1016/j.neuropharm.2008.08.023. Epub 2008 Aug 28. [PubMed:18793656]
  12. FDA Approved Drug Products: Butabarbital Oral Tablets and Solution [Link]
Human Metabolome Database
HMDB0014382
KEGG Drug
D03180
KEGG Compound
C07827
PubChem Compound
2479
PubChem Substance
46505051
ChemSpider
2385
RxNav
477631
ChEBI
3228
ChEMBL
CHEMBL449
Therapeutic Targets Database
DAP000667
PharmGKB
PA164743463
Drugs.com
Drugs.com Drug Page
Wikipedia
Butabarbital

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount

Pharmacoeconomics

Manufacturers
  • Medpointe pharmaceuticals medpointe healthcare inc
  • Alpharma us pharmaceuticals division
  • Wockhardt eu operations (swiss) ag
  • Lannett co inc
  • Meda pharmaceuticals inc
  • Halsey drug co inc
  • Cm bundy co
  • Sandoz inc
  • Solvay pharmaceuticals
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Whiteworth towne paulsen inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Marshall pharmacal corp
  • West ward pharmaceutical corp
Packagers
  • C.O. Truxton Inc.
  • Chattem Chemicals Inc.
  • Meda AB
Dosage Forms
FormRouteStrength
SolutionOral30 mg/5mL
TabletOral30 mg/1
TabletOral50 mg/1
TabletOral
Tablet, coatedOral
TabletOral
Prices
Unit descriptionCostUnit
Butisol sodium 50 mg tablet2.46USD tablet
Butisol sodium 30 mg tablet1.89USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)166.5 °CPhysProp
logP1.65WONG,O & MCKEOWN,RH (1988)
Predicted Properties
PropertyValueSource
Water Solubility1.39 mg/mLALOGPS
logP1.7ALOGPS
logP1.45ChemAxon
logS-2.2ALOGPS
pKa (Strongest Acidic)8.48ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area75.27 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity53.4 m3·mol-1ChemAxon
Polarizability21.41 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9324
Blood Brain Barrier+0.9782
Caco-2 permeable-0.6013
P-glycoprotein substrateSubstrate0.5938
P-glycoprotein inhibitor INon-inhibitor0.617
P-glycoprotein inhibitor IINon-inhibitor0.961
Renal organic cation transporterNon-inhibitor0.9465
CYP450 2C9 substrateNon-substrate0.7719
CYP450 2D6 substrateNon-substrate0.9014
CYP450 3A4 substrateNon-substrate0.7098
CYP450 1A2 substrateNon-inhibitor0.8775
CYP450 2C9 inhibitorNon-inhibitor0.821
CYP450 2D6 inhibitorNon-inhibitor0.933
CYP450 2C19 inhibitorNon-inhibitor0.7828
CYP450 3A4 inhibitorNon-inhibitor0.9203
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9458
Ames testNon AMES toxic0.6458
CarcinogenicityNon-carcinogens0.8533
BiodegradationNot ready biodegradable0.9759
Rat acute toxicity3.6803 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.99
hERG inhibition (predictor II)Non-inhibitor0.9233
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0a4l-6900000000-6e0cbc3d26c5541ad8eb
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Positive allosteric modulator
General Function
Inhibitory extracellular ligand-gated ion channel activity
Specific Function
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...

Components:
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 group
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Receptor binding
Specific Function
Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an i...

Components:
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
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Pdz domain binding
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 co...
Gene Name
GRIA1
Uniprot ID
P42261
Uniprot Name
Glutamate receptor 1
Molecular Weight
101505.245 Da
References
  1. 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]
  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
Humans
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 ne...
Gene Name
GRIA2
Uniprot ID
P42262
Uniprot Name
Glutamate receptor 2
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
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Extracellular-glutamate-gated ion channel 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 ne...
Gene Name
GRIA3
Uniprot ID
P42263
Uniprot Name
Glutamate receptor 3
Molecular Weight
101155.975 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
Humans
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 ne...
Gene Name
GRIA4
Uniprot ID
P48058
Uniprot Name
Glutamate receptor 4
Molecular Weight
100870.085 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
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Voltage-gated cation channel 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 co...
Gene Name
GRIK1
Uniprot ID
P39086
Uniprot Name
Glutamate receptor ionotropic, kainate 1
Molecular Weight
103979.665 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
Humans
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 co...
Gene Name
GRIK2
Uniprot ID
Q13002
Uniprot Name
Glutamate receptor ionotropic, kainate 2
Molecular Weight
102582.475 Da
References
  1. Yamakura T, Bertaccini E, Trudell JR, Harris RA: Anesthetics and ion channels: molecular models and sites of action. Annu Rev Pharmacol Toxicol. 2001;41:23-51. [PubMed:11264449]
  2. Krasowski MD, Harrison NL: General anaesthetic actions on ligand-gated ion channels. Cell Mol Life Sci. 1999 Aug 15;55(10):1278-303. [PubMed:10487207]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Kainate selective 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 ne...
Gene Name
GRIK3
Uniprot ID
Q13003
Uniprot Name
Glutamate receptor ionotropic, kainate 3
Molecular Weight
104036.06 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
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Kainate selective glutamate receptor activity
Specific Function
Receptor for glutamate. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors tha...
Gene Name
GRIK4
Uniprot ID
Q16099
Uniprot Name
Glutamate receptor ionotropic, kainate 4
Molecular Weight
107244.485 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
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Kainate selective glutamate receptor activity
Specific Function
Receptor for glutamate. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. The postsynaptic actions of Glu are mediated by a variety of receptors tha...
Gene Name
GRIK5
Uniprot ID
Q16478
Uniprot Name
Glutamate receptor ionotropic, kainate 5
Molecular Weight
109263.695 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]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. GOLDBAUM LR, SMITH PK: The interaction of barbiturates with serum albumin and its possible relation to their disposition and pharmacological actions. J Pharmacol Exp Ther. 1954 Jun;111(2):197-209. [PubMed:13175102]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Xenobiotic transporter activity
Specific Function
Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including b...
Gene Name
SLC2A1
Uniprot ID
P11166
Uniprot Name
Solute carrier family 2, facilitated glucose transporter member 1
Molecular Weight
54083.325 Da
References
  1. Haspel HC, Stephenson KN, Davies-Hill T, El-Barbary A, Lobo JF, Croxen RL, Mougrabi W, Koehler-Stec EM, Fenstermacher JD, Simpson IA: Effects of barbiturates on facilitative glucose transporters are pharmacologically specific and isoform selective. J Membr Biol. 1999 May 1;169(1):45-53. doi: 10.1007/pl00005900. [PubMed:10227851]

Drug created on June 13, 2005 07:24 / Updated on September 03, 2020 19:02

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