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Identification
- Summary
Enflurane is a halogenated inhalational anesthetic agent used for the induction and maintenance of anesthesia and for analgesia during labor and delivery.
- Generic Name
- Enflurane
- DrugBank Accession Number
- DB00228
- Background
Enflurane is a halogenated inhalational anesthetic initially approved by the FDA in 1972. Since this date, it has been withdrawn from the US market.18,19 Unlike its other inhalational anesthetic counterparts including isoflurane and halothane, enflurane is known to induce seizure activity. In addition, it is known to cause increased cardio depressant effects when compared to other inhaled anesthetics.5
- Type
- Small Molecule
- Groups
- Approved, Investigational, Vet approved
- Structure
Structure for Enflurane (DB00228)
- Weight
- Average: 184.492
Monoisotopic: 183.971433418 - Chemical Formula
- C3H2ClF5O
- Synonyms
- 2-chloro-1,1,2-trifluoroethyl difluoromethyl ether
- Alyrane
- Efrane
- Enflurane
- Enflurano
- Enfluranum
- Methylflurether
- External IDs
- Anesthetic 347
- OHIO 347
- R-E-235CA2
Pharmacology
- Indication
Enflurane may be used for both the induction and maintenance of general anesthesia. It can also be used to induce analgesia for vaginal delivery. Low concentrations of enflurane can also be used as an adjunct to general anesthetic drugs during delivery by Cesarean section.18
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used as adjunct in combination for therapy Analgesia •••••••••••• •••••• Maintenance of Analgesia •••••••••••• •••••• Maintenance of Analgesia •••••••••••• •••••• Maintenance of General anaesthesia •••••••••••• •••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Enflurane rapidly induces anesthesia via the stimulation of inhibitory neural channels and the inhibition of excitatory neural channels. Muscle relaxation, obtundation of pharyngeal and laryngeal reflexes, and lowering of blood pressure are some of the main pharmacodynamic effects of this drug.17 Enflurane also decreases cardiac muscle contractility.5
High concentrations of enflurane may lead to uterine relaxation and increase the risk of uterine bleeding during delivery.17 Rare but clinically significant elevations in ALT may indicate hepatoxicity from the use of enflurane.3 In some susceptible patients, enflurane may cause malignant hyperthermia.17
- Mechanism of action
The mechanism of action of enflurane is not completely established.17 Studies on rats indicate that enflurane binds to GABAA and glycine receptors, causing depressant effects at the ventral neural horn. It has been reported that 30% of the central nervous system depressant effects on the spinal cord after enflurane is administered are caused by the (GABA-A) receptor while binding to glycine receptors is responsible for about 20 % of the depressant effects.2 The relevance of these findings to humans is unknown. Other studies have found that enflurane binds to the calcium channels in the cardiac sarcoplasmic reticulum causing cardio depressant effects.7,8,9 Other studies support that this drug potentiates glycine receptors, which results in central nervous system depressant effects.12,11
Target Actions Organism AGABA(A) Receptor potentiatorHumans AVoltage-dependent calcium channel inhibitoractivatorHumans AGlycine receptor subunit alpha-1 potentiatorHumans UVoltage-gated Potassium Channels inhibitoractivatorUCalcium-transporting ATPase type 2C member 1 inhibitorHumans UGlutamate (NMDA) receptor antagonistHumans USarcoplasmic/endoplasmic reticulum calcium ATPase 1 inhibitorstimulatorHumans - Absorption
Enflurane is rapidly absorbed into the circulation through the lungs.14,18 The minimum alveolar concentration is oxygen is 1.68%.5
- Volume of distribution
Enflurane distributes to the brain, blood, and subcutaneous fat.13
- Protein binding
The plasma protein binding for enflurane is 97%.16
- Metabolism
Enflurane is metabolized by the CYP2E1 enzyme in the liver to produce inorganic fluoride ions, the major metabolite of enflurane metabolism.10 One reference indicates that enflurane is only 2-5% eliminated after oxidative metabolism in the liver, however more recent evidence suggests that about 9% is eliminated via hepatic oxidation.5
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- Route of elimination
Metabolism accounts for 5-9% of enflurane elimination, sometimes causing nephrotoxicity. Excretion through the skin is believed to be minimal.5
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
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The LD50 of enflurane in rats is 14000 ppm/3 hour(s) when inhaled.20 There is limited information in the literature about enflurane overdose. Hepatotoxicity, cardiotoxicity, nephrotoxicity, and neurotoxicity are expected.18 One report in the literature of an enflurane overdose describes an accidental fatal overdose in a 21-year-old male.13 About 72 hours after death, high amounts of enflurane were found in the brain, blood, and subcutaneous fat. Gas chromatographic studies revealed enflurane concentrations of 350 mg/l-1 in the brain, 130 mg/l-1 in the blood, and 100 mg/l-1 in the subcutaneous fat.13
In the event of an enflurane overdose, immediately stop the administration of enflurane, establish a patent airway, and administer pure oxygen by assisted or controlled ventilation.18
- 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 Integrate drug-drug
interactions in your software1,2-Benzodiazepine The risk or severity of CNS depression can be increased when Enflurane is combined with 1,2-Benzodiazepine. Abatacept The metabolism of Enflurane can be increased when combined with Abatacept. Acebutolol Enflurane may increase the cardiodepressant activities of Acebutolol. Acetaminophen Enflurane may increase the hepatotoxic activities of Acetaminophen. Acetazolamide The risk or severity of CNS depression can be increased when Enflurane is combined with Acetazolamide. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Alyrane (Baxter) / Compound 347 (Dexa Medica) / Endurane (Singapore Pharmawealth Lifesciences) / Enfluran (Cristália)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enflurane Liquid 99.9 % Respiratory (inhalation) Abbvie 1993-12-31 2012-11-02 Canada 
Ethrane Liquid 125 mL/125mL Respiratory (inhalation) Baxter Laboratories 1972-08-28 2012-12-01 US 
Ethrane Liq Inh Liquid 100 % Respiratory (inhalation) Ohmeda Pharmaceutical Products, Division Of Boc Canada Limited 1996-09-18 1997-08-25 Canada Ethrane Liquid Inh Liquid 100 % Respiratory (inhalation) Baxter Laboratories 1997-02-20 2004-08-05 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Enflurane Liquid 1 mL/1mL Respiratory (inhalation) Piramal Critical Care Inc 1994-07-29 2014-09-28 US
Categories
- ATC Codes
- N01AB04 — Enflurane
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as organofluorides. These are compounds containing a chemical bond between a carbon atom and a fluorine atom.
- Kingdom
- Organic compounds
- Super Class
- Organohalogen compounds
- Class
- Organofluorides
- Sub Class
- Not Available
- Direct Parent
- Organofluorides
- Alternative Parents
- Organooxygen compounds / Organochlorides / Hydrocarbon derivatives / Alkyl fluorides / Alkyl chlorides
- Substituents
- Aliphatic acyclic compound / Alkyl chloride / Alkyl fluoride / Alkyl halide / Hydrocarbon derivative / Organic oxygen compound / Organochloride / Organofluoride / Organooxygen compound
- Molecular Framework
- Aliphatic acyclic compounds
- External Descriptors
- organofluorine compound, organochlorine compound, ether (CHEBI:4792)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 91I69L5AY5
- CAS number
- 13838-16-9
- InChI Key
- JPGQOUSTVILISH-UHFFFAOYSA-N
- InChI
- InChI=1S/C3H2ClF5O/c4-1(5)3(8,9)10-2(6)7/h1-2H
- IUPAC Name
- 2-chloro-1-(difluoromethoxy)-1,1,2-trifluoroethane
- SMILES
- FC(F)OC(F)(F)C(F)Cl
References
- Synthesis Reference
Terrell, R.C.; U.S. Patents 3,469,011; September 23,1969 and 3,527,813; September 8, 1970; both assigned to Air Reduction Company, Incorporated.
- General References
- Quail AW: Modern inhalational anaesthetic agents. A review of halothane, isoflurane and enflurane. Med J Aust. 1989 Jan 16;150(2):95-102. [Article]
- Grasshoff C, Antkowiak B: Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats. Br J Anaesth. 2006 Nov;97(5):687-94. doi: 10.1093/bja/ael239. Epub 2006 Sep 13. [Article]
- Authors unspecified: Enflurane . [Article]
- Berger JM, Stirt JA, Sullivan SF: Enflurane, halothane, and aminophylline--uptake and pharmacokinetics. Anesth Analg. 1983 Aug;62(8):733-7. [Article]
- Dale O, Brown BR Jr: Clinical pharmacokinetics of the inhalational anaesthetics. Clin Pharmacokinet. 1987 Mar;12(3):145-67. doi: 10.2165/00003088-198712030-00001. [Article]
- Sleigh JW, Vizuete JA, Voss L, Steyn-Ross A, Steyn-Ross M, Marcuccilli CJ, Hudetz AG: The electrocortical effects of enflurane: experiment and theory. Anesth Analg. 2009 Oct;109(4):1253-62. doi: 10.1213/ANE.0b013e3181add06b. [Article]
- Connelly TJ, Coronado R: Activation of the Ca2+ release channel of cardiac sarcoplasmic reticulum by volatile anesthetics. Anesthesiology. 1994 Aug;81(2):459-69. doi: 10.1097/00000542-199408000-00025. [Article]
- Eskinder H, Rusch NJ, Supan FD, Kampine JP, Bosnjak ZJ: The effects of volatile anesthetics on L- and T-type calcium channel currents in canine cardiac Purkinje cells. Anesthesiology. 1991 May;74(5):919-26. doi: 10.1097/00000542-199105000-00018. [Article]
- Haworth RA, Goknur AB: Inhibition of sodium/calcium exchange and calcium channels of heart cells by volatile anesthestics. Anesthesiology. 1995 May;82(5):1255-65. doi: 10.1097/00000542-199505000-00021. [Article]
- Kharasch ED, Thummel KE, Mautz D, Bosse S: Clinical enflurane metabolism by cytochrome P450 2E1. Clin Pharmacol Ther. 1994 Apr;55(4):434-40. doi: 10.1038/clpt.1994.53. [Article]
- Krasowski MD, Harrison NL: The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations. Br J Pharmacol. 2000 Feb;129(4):731-43. [Article]
- Borghese CM: The molecular pharmacology of volatile anesthetics. Int Anesthesiol Clin. 2015 Spring;53(2):28-39. doi: 10.1097/AIA.0000000000000060. [Article]
- Jacob B, Heller C, Daldrup T, Burrig KF, Barz J, Bonte W: Fatal accidental enflurane intoxication. J Forensic Sci. 1989 Nov;34(6):1408-12. [Article]
- Torri G: Uptake and elimination of enflurane (Ethrane) at constant inspired and alveolar concentration. Acta Anaesthesiol Belg. 1974 May;25(2):190-7. [Article]
- Njoku D, Laster MJ, Gong DH, Eger EI 2nd, Reed GF, Martin JL: Biotransformation of halothane, enflurane, isoflurane, and desflurane to trifluoroacetylated liver proteins: association between protein acylation and hepatic injury. Anesth Analg. 1997 Jan;84(1):173-8. doi: 10.1097/00000539-199701000-00031. [Article]
- John D. Current M.D. (n/A). Pharmacology for Anesthetists: anesthesia and adjuvants. N/A.
- NIH StatPearls: Enflurane [Link]
- FDA Approved Products: Efrane (enflurane) liquid for inhalation [Link]
- FDA approval status, Enflurane [Link]
- Matheson Gas MSDS: Enflurane [Link]
- External Links
- MSDS
- Download (64.9 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Treatment General Anesthesia 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Abbott laboratories hosp products div
- Piramal critical care inc
- Baxter healthcare corp anesthesia critical care
- Packagers
- Apothecon
- Baxter International Inc.
- Minrad Inc.
- Rx Elite
- Dosage Forms
Form Route Strength Liquid Respiratory (inhalation) 1 mL/1mL Liquid Respiratory (inhalation) 99.9 % Solution Respiratory (inhalation) 250 ml Solution Respiratory (inhalation) 100 mL Solution Oral 100 mL Liquid Respiratory (inhalation) 125 mL/125mL Liquid Respiratory (inhalation) 100 % - Prices
Unit description Cost Unit Ethrane inhalation 0.55USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 48.5 https://www.chemicalbook.com/ChemicalProductProperty_US_CB8437691.aspx boiling point (°C) 56.5 Terrell, R.C.; U.S. Patents 3,469,011; September 23,1969 and 3,527,813; September 8, 1970; both assigned to Air Reduction Company, Incorporated. logP 2.10 HANSCH,C & LEO,AJ (1985) - Predicted Properties
Property Value Source Water Solubility 3.9 mg/mL ALOGPS logP 2.24 ALOGPS logP 2.8 Chemaxon logS -1.7 ALOGPS pKa (Strongest Basic) -5 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 1 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 9.23 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 23.07 m3·mol-1 Chemaxon Polarizability 9.74 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.994 Caco-2 permeable + 0.6125 P-glycoprotein substrate Non-substrate 0.8919 P-glycoprotein inhibitor I Non-inhibitor 0.9553 P-glycoprotein inhibitor II Non-inhibitor 0.9297 Renal organic cation transporter Non-inhibitor 0.9293 CYP450 2C9 substrate Non-substrate 0.8407 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Non-substrate 0.7179 CYP450 1A2 substrate Non-inhibitor 0.5701 CYP450 2C9 inhibitor Non-inhibitor 0.8112 CYP450 2D6 inhibitor Non-inhibitor 0.9408 CYP450 2C19 inhibitor Non-inhibitor 0.5794 CYP450 3A4 inhibitor Non-inhibitor 0.9604 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8702 Ames test Non AMES toxic 0.9132 Carcinogenicity Carcinogens 0.7574 Biodegradation Not ready biodegradable 0.9642 Rat acute toxicity 1.3804 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9576 hERG inhibition (predictor II) Non-inhibitor 0.9032
Spectra
- Mass Spec (NIST)
- Download (7.54 KB)
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 104.9977594 predictedDarkChem Lite v0.1.0 [M-H]- 132.50061 predictedDeepCCS 1.0 (2019) [M+H]+ 105.7755594 predictedDarkChem Lite v0.1.0 [M+H]+ 134.80386 predictedDeepCCS 1.0 (2019) [M+Na]+ 105.4604594 predictedDarkChem Lite v0.1.0 [M+Na]+ 143.08226 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Alpha subunit of the heteropentameric ligand-gated chloride channel gated by Gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (PubMed:23909897, PubMed:25489750, PubMed:29950725, PubMed:30602789). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) (PubMed:29950725, PubMed:30602789). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (PubMed:23909897, PubMed:29950725, PubMed:30602789). Alpha-1/GABRA1-containing GABAARs are largely synaptic (By similarity). Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission (By similarity). GABAARs containing alpha-1 and beta-2 or -3 subunits exhibit synaptogenic activity; the gamma-2 subunit being necessary but not sufficient to induce rapid synaptic contacts formation (PubMed:23909897, PubMed:25489750). GABAARs function also as histamine receptor where histamine binds at the interface of two neighboring beta subunits and potentiates GABA response (By similarity). GABAARs containing alpha, beta and epsilon subunits also permit spontaneous chloride channel activity while preserving the structural information required for GABA-gated openings (By similarity). Alpha-1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Together with rho subunits, may also control neuronal and glial GABAergic transmission in the cerebellum (By similarity)
- Specific Function
- Gaba-a receptor activity
Components:
References
- Franks NP: Molecular targets underlying general anaesthesia. Br J Pharmacol. 2006 Jan;147 Suppl 1:S72-81. [Article]
- Grasshoff C, Antkowiak B: Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats. Br J Anaesth. 2006 Nov;97(5):687-94. doi: 10.1093/bja/ael239. Epub 2006 Sep 13. [Article]
- Greenblatt EP, Meng X: Divergence of volatile anesthetic effects in inhibitory neurotransmitter receptors. Anesthesiology. 2001 Jun;94(6):1026-33. [Article]
- ChEMBL Compound Report Card [Link]
- NIH StatPearls: Enflurane [Link]
- FDA Approved Products: Efrane (enflurane) liquid for inhalation [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- InhibitorActivator
- Curator comments
- Enflurane has been shown to increase the opening of the calcium channel in cardiac cells during in vitro studies.
- General Function
- Regulatory subunit of the voltage-gated calcium channel that gives rise to L-type calcium currents in skeletal muscle. Regulates channel inactivation kinetics
- Specific Function
- Calcium channel regulator activity
Components:
References
- Connelly TJ, Coronado R: Activation of the Ca2+ release channel of cardiac sarcoplasmic reticulum by volatile anesthetics. Anesthesiology. 1994 Aug;81(2):459-69. doi: 10.1097/00000542-199408000-00025. [Article]
- Eskinder H, Rusch NJ, Supan FD, Kampine JP, Bosnjak ZJ: The effects of volatile anesthetics on L- and T-type calcium channel currents in canine cardiac Purkinje cells. Anesthesiology. 1991 May;74(5):919-26. doi: 10.1097/00000542-199105000-00018. [Article]
- Haworth RA, Goknur AB: Inhibition of sodium/calcium exchange and calcium channels of heart cells by volatile anesthestics. Anesthesiology. 1995 May;82(5):1255-65. doi: 10.1097/00000542-199505000-00021. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- General Function
- Glycine receptors are ligand-gated chloride channels (PubMed:23994010, PubMed:25730860). Channel opening is triggered by extracellular glycine (PubMed:14551753, PubMed:16144831, PubMed:2155780, PubMed:22715885, PubMed:22973015, PubMed:25973519, PubMed:7920629, PubMed:9009272). Channel opening is also triggered by taurine and beta-alanine (PubMed:16144831, PubMed:9009272). Channel characteristics depend on the subunit composition; heteropentameric channels are activated by lower glycine levels and display faster desensitization (PubMed:14551753). Plays an important role in the down-regulation of neuronal excitability (PubMed:8298642, PubMed:9009272). Contributes to the generation of inhibitory postsynaptic currents (PubMed:25445488). Channel activity is potentiated by ethanol (PubMed:25973519). Potentiation of channel activity by intoxicating levels of ethanol contribute to the sedative effects of ethanol (By similarity)
- Specific Function
- Extracellularly glycine-gated chloride channel activity
- Gene Name
- GLRA1
- Uniprot ID
- P23415
- Uniprot Name
- Glycine receptor subunit alpha-1
- Molecular Weight
- 52623.35 Da
References
- Borghese CM: The molecular pharmacology of volatile anesthetics. Int Anesthesiol Clin. 2015 Spring;53(2):28-39. doi: 10.1097/AIA.0000000000000060. [Article]
- Krasowski MD, Harrison NL: The actions of ether, alcohol and alkane general anaesthetics on GABAA and glycine receptors and the effects of TM2 and TM3 mutations. Br J Pharmacol. 2000 Feb;129(4):731-43. [Article]
- Grasshoff C, Antkowiak B: Effects of isoflurane and enflurane on GABAA and glycine receptors contribute equally to depressant actions on spinal ventral horn neurones in rats. Br J Anaesth. 2006 Nov;97(5):687-94. doi: 10.1093/bja/ael239. Epub 2006 Sep 13. [Article]
- NIH StatPearls: Enflurane [Link]
- ChEMBL Compound Report Card [Link]
- Kind
- Protein group
- Organism
- Not Available
- Pharmacological action
- Unknown
- Actions
- InhibitorActivator
- General Function
- A-type voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes in the brain (PubMed:15454437). Mediates A-type current I(SA) in suprachiasmatic nucleus (SCN) neurons. Exhibits a low-threshold A-type current with a hyperpolarized steady-state inactivation midpoint and the recovery process was steeply voltage-dependent, with recovery being markedly faster at more negative potentials. May regulates repetitive firing rates in the suprachiasmatic nucleus (SCN) neurons and circadian rhythms in neuronal excitability and behavior. Contributes to the regulation of the circadian rhythm of action potential firing in suprachiasmatic nucleus neurons, which regulates the circadian rhythm of locomotor activity. The regulatory subunit KCNIP1 modulates the kinetics of channel inactivation, increases the current amplitudes and accelerates recovery from inactivation, shifts activation in a depolarizing direction (By similarity). The regulatory subunit DPP10 decreases the voltage sensitivity of the inactivation channel gating (PubMed:15454437)
- Specific Function
- A-type (transient outward) potassium channel activity
Components:
References
- Matchett GA, Allard MW, Martin RD, Zhang JH: Neuroprotective effect of volatile anesthetic agents: molecular mechanisms. Neurol Res. 2009 Mar;31(2):128-34. doi: 10.1179/174313209X393546. [Article]
- Friederich P, Benzenberg D, Trellakis S, Urban BW: Interaction of volatile anesthetics with human Kv channels in relation to clinical concentrations. Anesthesiology. 2001 Oct;95(4):954-8. doi: 10.1097/00000542-200110000-00026. [Article]
- Namba T, Ishii TM, Ikeda M, Hisano T, Itoh T, Hirota K, Adelman JP, Fukuda K: Inhibition of the human intermediate conductance Ca(2+)-activated K(+) channel, hIK1, by volatile anesthetics. Eur J Pharmacol. 2000 Apr 28;395(2):95-101. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- ATP-driven pump that supplies the Golgi apparatus with Ca(2+) and Mn(2+) ions, both essential cofactors for processing and trafficking of newly synthesized proteins in the secretory pathway (PubMed:12707275, PubMed:16192278, PubMed:20439740, PubMed:21187401, PubMed:30923126). Within a catalytic cycle, acquires Ca(2+) or Mn(2+) ions on the cytoplasmic side of the membrane and delivers them to the lumenal side. The transfer of ions across the membrane is coupled to ATP hydrolysis and is associated with a transient phosphorylation that shifts the pump conformation from inward-facing to outward-facing state (PubMed:16192278, PubMed:16332677, PubMed:30923126). Plays a primary role in the maintenance of Ca(2+) homeostasis in the trans-Golgi compartment with a functional impact on Golgi and post-Golgi protein sorting as well as a structural impact on cisternae morphology (PubMed:14632183, PubMed:20439740). Responsible for loading the Golgi stores with Ca(2+) ions in keratinocytes, contributing to keratinocyte differentiation and epidermis integrity (PubMed:10615129, PubMed:14632183, PubMed:20439740). Participates in Ca(2+) and Mn(2+) ions uptake into the Golgi store of hippocampal neurons and regulates protein trafficking required for neural polarity (By similarity). May also play a role in the maintenance of Ca(2+) and Mn(2+) homeostasis and signaling in the cytosol while preventing cytotoxicity (PubMed:21187401)
- Specific Function
- Atp binding
- Gene Name
- ATP2C1
- Uniprot ID
- P98194
- Uniprot Name
- Calcium-transporting ATPase type 2C member 1
- Molecular Weight
- 100576.42 Da
References
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:26875626, PubMed:26919761, PubMed:28105280, PubMed:28126851, PubMed:7685113). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:26919761)
- Specific Function
- Amyloid-beta binding
Components:
References
- Dildy-Mayfield JE, Eger EI 2nd, Harris RA: Anesthetics produce subunit-selective actions on glutamate receptors. J Pharmacol Exp Ther. 1996 Mar;276(3):1058-65. [Article]
- Cheng G, Kendig JJ: Enflurane directly depresses glutamate AMPA and NMDA currents in mouse spinal cord motor neurons independent of actions on GABAA or glycine receptors. Anesthesiology. 2000 Oct;93(4):1075-84. doi: 10.1097/00000542-200010000-00032. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorStimulator
- Curator comments
- Data regarding this target action are limited in the literature.
- General Function
- Key regulator of striated muscle performance by acting as the major Ca(2+) ATPase responsible for the reuptake of cytosolic Ca(2+) into the sarcoplasmic reticulum. Catalyzes the hydrolysis of ATP coupled with the translocation of calcium from the cytosol to the sarcoplasmic reticulum lumen (By similarity). Contributes to calcium sequestration involved in muscular excitation/contraction (PubMed:10914677)
- Specific Function
- Atp binding
- Gene Name
- ATP2A1
- Uniprot ID
- O14983
- Uniprot Name
- Sarcoplasmic/endoplasmic reticulum calcium ATPase 1
- Molecular Weight
- 110251.36 Da
References
- Kosk-Kosicka D, Roszczynska G: Inhibition of plasma membrane Ca(2+)-ATPase activity by volatile anesthetics. Anesthesiology. 1993 Oct;79(4):774-80. [Article]
- Blanck TJ, Peterson CV, Baroody B, Tegazzin V, Lou J: Halothane, enflurane, and isoflurane stimulate calcium leakage from rabbit sarcoplasmic reticulum. Anesthesiology. 1992 May;76(5):813-21. doi: 10.1097/00000542-199205000-00021. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of fatty acids (PubMed:10553002, PubMed:18577768). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10553002, PubMed:18577768). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates fatty acids specifically at the omega-1 position displaying the highest catalytic activity for saturated fatty acids (PubMed:10553002, PubMed:18577768). May be involved in the oxidative metabolism of xenobiotics (Probable)
- Specific Function
- 4-nitrophenol 2-monooxygenase activity
- Gene Name
- CYP2E1
- Uniprot ID
- P05181
- Uniprot Name
- Cytochrome P450 2E1
- Molecular Weight
- 56848.42 Da
References
- Garton KJ, Yuen P, Meinwald J, Thummel KE, Kharasch ED: Stereoselective metabolism of enflurane by human liver cytochrome P450 2E1. Drug Metab Dispos. 1995 Dec;23(12):1426-30. [Article]
- Kharasch ED, Thummel KE, Mautz D, Bosse S: Clinical enflurane metabolism by cytochrome P450 2E1. Clin Pharmacol Ther. 1994 Apr;55(4):434-40. doi: 10.1038/clpt.1994.53. [Article]
- Njoku D, Laster MJ, Gong DH, Eger EI 2nd, Reed GF, Martin JL: Biotransformation of halothane, enflurane, isoflurane, and desflurane to trifluoroacetylated liver proteins: association between protein acylation and hepatic injury. Anesth Analg. 1997 Jan;84(1):173-8. doi: 10.1097/00000539-199701000-00031. [Article]
- Flockhart Table of Drug Interactions [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- Antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Liu R, Eckenhoff RG: Weak polar interactions confer albumin binding site selectivity for haloether anesthetics. Anesthesiology. 2005 Apr;102(4):799-805. [Article]
- Sawas AH, Pentyala SN, Rebecchi MJ: Binding of volatile anesthetics to serum albumin: measurements of enthalpy and solvent contributions. Biochemistry. 2004 Oct 5;43(39):12675-85. [Article]
- Dale O, Nilsen OG: Displacement of some basic drugs from human serum proteins by enflurane, halothane and their major metabolites. An in vitro study. Br J Anaesth. 1984 May;56(5):535-42. doi: 10.1093/bja/56.5.535. [Article]
Drug created at June 13, 2005 13:24 / Updated at August 02, 2024 07:24