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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyIdentification
- Name
- Butabarbital
- Accession Number
- DB00237 (APRD00752)
- Type
- Small Molecule
- Groups
- Approved, Illicit
- 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
- Structure
Structure for Butabarbital (DB00237)
- 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
- Product Ingredients
Ingredient UNII CAS InChI Key Butabarbital sodium 9WTD50I918 143-81-7 QORQZMBCPRBCAB-UHFFFAOYSA-M - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataButisol Sodium Solution 30 mg/5mL Oral MedPointe Pharmaceuticals 2007-08-02 2007-08-02 US 
Butisol Sodium Tablet 50 mg/1 Oral MedPointe Pharmaceuticals 2007-08-02 2007-08-02 US Butisol Sodium Tablet 30 mg/1 Oral MEDA Pharmaceuticals 1939-08-01 2020-01-31 US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Learn more
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Phenazopyridine Hydrochloride, Hyoscyamine Hydrobromide, and Butabarbital Butabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1) Tablet, coated Oral Physicians Total Care, Inc. 2004-09-03 2011-06-30 US Phenazopyridine Plus Butabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1) Tablet, coated Oral Breckenridge Pharmaceutical, Inc. 2005-03-01 2011-02-28 US Pyrelle H.B. Butabarbital (15 mg/1) + Hyoscyamine hydrobromide (0.3 mg/1) + Phenazopyridine hydrochloride (150 mg/1) Tablet Oral Azur Pharma, Inc. 2004-01-01 2010-06-01 US - International/Other Brands
- Butalan / Butisol / Sarisol No. 2
- Categories
- UNII
- P0078O25A9
- CAS number
- 125-40-6
- Weight
- Average: 212.2456
Monoisotopic: 212.116092388 - Chemical Formula
- C10H16N2O3
- 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
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
- 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.
Target Actions Organism AGABA(A) Receptor positive allosteric modulatorHumans UNeuronal Acetylcholine (nACh) Receptor Subunits inhibitorHumans UGlutamate receptor 1 antagonistHumans UGlutamate receptor 2 antagonistHumans UGlutamate receptor 3 antagonistHumans UGlutamate receptor 4 antagonistHumans UGlutamate receptor ionotropic, kainate 1 antagonistHumans UGlutamate receptor ionotropic, kainate 2 antagonistHumans UGlutamate receptor ionotropic, kainate 3 antagonistHumans UGlutamate receptor ionotropic, kainate 4 antagonistHumans UGlutamate receptor ionotropic, kainate 5 antagonistHumans - 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
- 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.
Drug Interaction Unlock Additional Data(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Butabarbital. (S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Butabarbital. 1,10-Phenanthroline The therapeutic efficacy of Butabarbital can be decreased when used in combination with 1,10-Phenanthroline. 2,5-Dimethoxy-4-ethylthioamphetamine The risk or severity of adverse effects can be increased when Butabarbital is combined with 2,5-Dimethoxy-4-ethylthioamphetamine. 3-isobutyl-1-methyl-7H-xanthine The serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be decreased when it is combined with Butabarbital. 4-Bromo-2,5-dimethoxyamphetamine The risk or severity of adverse effects can be increased when Butabarbital is combined with 4-Bromo-2,5-dimethoxyamphetamine. 4-hydroxycoumarin The metabolism of 4-hydroxycoumarin can be increased when combined with Butabarbital. 4-Methoxyamphetamine The risk or severity of adverse effects can be increased when Butabarbital is combined with 4-Methoxyamphetamine. 5-methoxy-N,N-dimethyltryptamine The risk or severity of adverse effects can be increased when Butabarbital is combined with 5-methoxy-N,N-dimethyltryptamine. 6-O-benzylguanine The serum concentration of 6-O-benzylguanine can be decreased when it is combined with Butabarbital. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
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.
References
- General References
- 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]
- 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]
- 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]
- 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]
- 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]
- 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]
- MAYNERT EW, LOSIN L: The metabolism of butabarbital (butisol) in the dog. J Pharmacol Exp Ther. 1955 Nov;115(3):275-82. [PubMed:13272177]
- 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]
- 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]
- 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]
- 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]
- FDA Approved Drug Products: Butabarbital Oral Tablets and Solution [Link]
- External Links
- 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
- ATC Codes
- N05CB01 — Combinations of barbiturates
Clinical Trials
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
Form Route Strength Solution Oral 30 mg/5mL Tablet Oral 30 mg/1 Tablet Oral 50 mg/1 Tablet Oral Tablet, coated Oral Tablet Oral - Prices
Unit description Cost Unit Butisol sodium 50 mg tablet 2.46USD tablet Butisol sodium 30 mg tablet 1.89USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 166.5 °C PhysProp logP 1.65 WONG,O & MCKEOWN,RH (1988) - Predicted Properties
Property Value Source Water Solubility 1.39 mg/mL ALOGPS logP 1.7 ALOGPS logP 1.45 ChemAxon logS -2.2 ALOGPS pKa (Strongest Acidic) 8.48 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 2 ChemAxon Polar Surface Area 75.27 Å2 ChemAxon Rotatable Bond Count 3 ChemAxon Refractivity 53.4 m3·mol-1 ChemAxon Polarizability 21.41 Å3 ChemAxon Number of Rings 1 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 0.9324 Blood Brain Barrier + 0.9782 Caco-2 permeable - 0.6013 P-glycoprotein substrate Substrate 0.5938 P-glycoprotein inhibitor I Non-inhibitor 0.617 P-glycoprotein inhibitor II Non-inhibitor 0.961 Renal organic cation transporter Non-inhibitor 0.9465 CYP450 2C9 substrate Non-substrate 0.7719 CYP450 2D6 substrate Non-substrate 0.9014 CYP450 3A4 substrate Non-substrate 0.7098 CYP450 1A2 substrate Non-inhibitor 0.8775 CYP450 2C9 inhibitor Non-inhibitor 0.821 CYP450 2D6 inhibitor Non-inhibitor 0.933 CYP450 2C19 inhibitor Non-inhibitor 0.7828 CYP450 3A4 inhibitor Non-inhibitor 0.9203 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9458 Ames test Non AMES toxic 0.6458 Carcinogenicity Non-carcinogens 0.8533 Biodegradation Not ready biodegradable 0.9759 Rat acute toxicity 3.6803 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.99 hERG inhibition (predictor II) Non-inhibitor 0.9233
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Mass Spectrum (Electron Ionization) MS splash10-0a4l-6900000000-6e0cbc3d26c5541ad8eb Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- 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
- Barbiturate / N-acyl urea / Ureide / 1,3-diazinane / Dicarboximide / Urea / Carbonic acid derivative / Carboxylic acid derivative / Azacycle / Organic nitrogen compound
- Molecular Framework
- Aliphatic heteromonocyclic compounds
- External Descriptors
- barbiturates (CHEBI:3228)
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
- Mehta AK, Ticku MK: An update on GABAA receptors. Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217. [PubMed:10209232]
- 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
- 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]
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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]
- 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
- 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
- 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 May 14, 2020 05:46
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