Isoflurane

Identification

Summary

Isoflurane is an inhaled general anesthetic used in surgery.

Brand Names
Forane, Terrell
Generic Name
Isoflurane
DrugBank Accession Number
DB00753
Background

A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 184.492
Monoisotopic: 183.971433418
Chemical Formula
C3H2ClF5O
Synonyms
  • 1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
  • Isoflurane
  • Isoflurano
  • Isofluranum

Pharmacology

Indication

For induction and maintenance of general anesthesia.

Pharmacology
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Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Isoflurane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.

Mechanism of action

Isoflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Isoflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. Also appears to bind the D subunit of ATP synthase and NADH dehydogenase. Isoflurane also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor and the glycine receptor.

TargetActionsOrganism
AGamma-aminobutyric acid receptor subunit alpha-1
agonist
Humans
ACalcium-transporting ATPase type 2C member 1
inhibitor
Humans
AGlycine receptor subunit alpha-1
agonist
Humans
AGlutamate receptor 1
antagonist
Humans
APotassium voltage-gated channel subfamily A member 1
inducer
Humans
UATP synthase subunit delta, mitochondrial
unknown
Humans
UCalmodulin
other/unknown
Humans
AGABA(A) Receptor
positive allosteric modulator
Humans
UNeuronal acetylcholine receptor subunit alpha-4
antagonist
Humans
UNeuronal acetylcholine receptor subunit beta-2
antagonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Minimal

Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

LC50=15300 ppm/3 hrs (inhalation by rat)

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
Voltage-dependent L-type calcium channel subunit alpha-1S---Not Availablec.3257G>A / c.520C>TADR InferredMalignant hyperthermia.Details
Ryanodine receptor 1---Not Availablec.103T>C / c.487C>T  … show all ADR InferredMalignant hyperthermia.Details

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
1,2-BenzodiazepineThe risk or severity of adverse effects can be increased when Isoflurane is combined with 1,2-Benzodiazepine.
AbametapirThe serum concentration of Isoflurane can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Isoflurane can be increased when combined with Abatacept.
AcebutololIsoflurane may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of hypertension can be increased when Isoflurane is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Isoflurane is combined with Acemetacin.
AcetaminophenIsoflurane may increase the hepatotoxic activities of Acetaminophen.
AcetazolamideThe risk or severity of adverse effects can be increased when Isoflurane is combined with Acetazolamide.
AcetophenazineThe risk or severity of adverse effects can be increased when Isoflurane is combined with Acetophenazine.
Acetylsalicylic acidThe risk or severity of hypertension can be increased when Isoflurane is combined with Acetylsalicylic acid.
Interactions
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Food Interactions
No interactions found.

Products

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International/Other Brands
Aerrane (Baxter) / Forene (Abbott) / Isocane (Lunan) / Isorane (Abbott)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ForaneInhalant1 mL/1mLRespiratory (inhalation)Baxter Healthcare Corporation1979-12-18Not applicableUS flag
ForaneLiquid100 %Respiratory (inhalation)Baxter Laboratories1996-12-31Not applicableCanada flag
Forane Liq InhLiquid100 %Respiratory (inhalation)Ohmeda Pharmaceutical Products, Division Of Boc Canada Limited1994-12-311996-09-26Canada flag
Isoflurane USPLiquid99.9 %Respiratory (inhalation)Abbvie1993-12-312016-03-21Canada flag
Isoflurane USPLiquid99.9 %Respiratory (inhalation)Fresenius Kabi1997-11-14Not applicableCanada flag
Isoflurane USPLiquid99.9 %Respiratory (inhalation)Halocarbon Laboratories, A Division Of Halocarbon Products Corp2004-11-032019-03-22Canada flag
Isoflurane USPLiquid100 %Respiratory (inhalation)Technilab Pharma Inc.1999-01-212008-08-05Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
IsofluraneLiquid1 mL/1mLRespiratory (inhalation)Hospira, Inc.2005-08-012012-03-01US flag
IsofluraneLiquid1 mL/1mLRespiratory (inhalation)Halocarbon Life Sciences, LLC1999-10-20Not applicableUS flag
IsofluraneLiquid1 mL/1mLRespiratory (inhalation)Piramal Critical Care Inc2013-11-13Not applicableUS flag
IsofluraneLiquid1 mL/1mLRespiratory (inhalation)Piramal Critical Care, Inc.2011-10-07Not applicableUS flag
TerrellLiquid1 mL/1mLRespiratory (inhalation)Piramal Critical Care Inc2010-02-28Not applicableUS flag
TerrellLiquid1 mL/1mLRespiratory (inhalation)Piramal Critical Care Inc2012-03-21Not applicableUS flag

Categories

ATC Codes
N01AB06 — Isoflurane
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 (CHEBI:6015)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
CYS9AKD70P
CAS number
26675-46-7
InChI Key
PIWKPBJCKXDKJR-UHFFFAOYSA-N
InChI
InChI=1S/C3H2ClF5O/c4-1(3(7,8)9)10-2(5)6/h1-2H
IUPAC Name
2-chloro-2-(difluoromethoxy)-1,1,1-trifluoroethane
SMILES
FC(F)OC(Cl)C(F)(F)F

References

Synthesis Reference

Leonid A. Rozov, Fernando Quiroz, Gerald G. Vernice, "Preparation of isoflurane." U.S. Patent US5416244, issued March, 1973.

US5416244
General References
Not Available
Human Metabolome Database
HMDB0014891
KEGG Drug
D00545
KEGG Compound
C07518
PubChem Compound
3763
PubChem Substance
46505880
ChemSpider
3631
BindingDB
217353
RxNav
6026
ChEBI
6015
ChEMBL
CHEMBL1256
Therapeutic Targets Database
DAP001033
PharmGKB
PA450106
PDBe Ligand
ICF
RxList
RxList Drug Page
Wikipedia
Isoflurane
FDA label
Download (99.6 KB)
MSDS
Download (37 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedDiagnosticAlzheimer's Disease (AD) / POCD - Postoperative Cognitive Dysfunction / Postoperative Delirium (POD)1
4CompletedDiagnosticPostoperative Delirium (POD)1
4CompletedDiagnosticPulmonary Hypertension (PH)1
4CompletedSupportive CareDNA Damage / Patients in Good Health / Types of General Anesthesia1
4CompletedSupportive CareHematoma, Subdural, Acute1
4CompletedSupportive CarePatients in Good Health1
4CompletedTreatmentAdvanced Chronic Rhinosinusitis1
4CompletedTreatmentCerebrovascular Accident / Subarachnoid Hemorrhage1
4CompletedTreatmentCoronary Artery Bypass Grafting (CABG) / Surgery, Cardiac1
4CompletedTreatmentNeoplasms, Breast1

Pharmacoeconomics

Manufacturers
  • Baxter healthcare corp anesthesia critical care
  • Halocarbon products corp
  • Hospira inc
  • Marsam pharmaceuticals llc
  • Piramal critical care inc
  • Rhodia ltd
Packagers
  • Apothecon
  • Baxter International Inc.
  • Halocarbon Laboratories
  • Hospira Inc.
  • Minrad Inc.
  • Nicholas Pirmal India Ltd. Uk
  • Rhodia Organique Fine Ltd.
  • Rx Elite
Dosage Forms
FormRouteStrength
InhalantRespiratory (inhalation)100 %
InhalantRespiratory (inhalation)250 %
AerosolRespiratory (inhalation)
InhalantRespiratory (inhalation)1 mL/1mL
LiquidRespiratory (inhalation)100 %
SolutionRespiratory (inhalation)100 ml/100ml
LiquidRespiratory (inhalation)1 mL/1mL
SolutionNasal100 %
LiquidRespiratory (inhalation)99.9 %
SolutionRespiratory (inhalation)100 %
SolutionRespiratory (inhalation)100 mL
SolutionRespiratory (inhalation)
LiquidRespiratory (inhalation)
AerosolRespiratory (inhalation)100 ml/1bottle
AerosolRespiratory (inhalation)250 ml/1bottle
LiquidNasal100 ml/1bottle
Prices
Unit descriptionCostUnit
Forane liquid0.24USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Liquid
Experimental Properties
PropertyValueSource
melting point (°C)48-48.5U.S. Patent 3,535,388.
boiling point (°C)48.5 °CPhysProp
water solubility4470 mg/L (at 37 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP2.06HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility3.56 mg/mLALOGPS
logP2.3ALOGPS
logP2.84ChemAxon
logS-1.7ALOGPS
pKa (Strongest Basic)-4.7ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area9.23 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity23.04 m3·mol-1ChemAxon
Polarizability9.73 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.994
Caco-2 permeable+0.6125
P-glycoprotein substrateNon-substrate0.8919
P-glycoprotein inhibitor INon-inhibitor0.9553
P-glycoprotein inhibitor IINon-inhibitor0.9297
Renal organic cation transporterNon-inhibitor0.9293
CYP450 2C9 substrateNon-substrate0.8407
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.7179
CYP450 1A2 substrateNon-inhibitor0.5701
CYP450 2C9 inhibitorNon-inhibitor0.8112
CYP450 2D6 inhibitorNon-inhibitor0.9408
CYP450 2C19 inhibitorNon-inhibitor0.5794
CYP450 3A4 inhibitorNon-inhibitor0.9604
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8702
Ames testNon AMES toxic0.9132
CarcinogenicityCarcinogens 0.7574
BiodegradationNot ready biodegradable0.9642
Rat acute toxicity1.3804 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9576
hERG inhibition (predictor II)Non-inhibitor0.9032
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.33 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Mass Spectrum (Electron Ionization)MSsplash10-0udi-9300000000-c134e176400bbe7073c2
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

Drugtargets2
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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
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...
Gene Name
GABRA1
Uniprot ID
P14867
Uniprot Name
Gamma-aminobutyric acid receptor subunit alpha-1
Molecular Weight
51801.395 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. McCracken ML, Borghese CM, Trudell JR, Harris RA: A transmembrane amino acid in the GABAA receptor beta2 subunit critical for the actions of alcohols and anesthetics. J Pharmacol Exp Ther. 2010 Dec;335(3):600-6. doi: 10.1124/jpet.110.170472. Epub 2010 Sep 8. [Article]
  4. Seo K, Seino H, Yoshikawa H, Petrenko AB, Baba H, Fujiwara N, Someya G, Kawano Y, Maeda T, Matsuda M, Kanematsu T, Hirata M: Genetic reduction of GABA(A) receptor gamma2 subunit expression potentiates the immobilizing action of isoflurane. Neurosci Lett. 2010 Mar 12;472(1):1-4. doi: 10.1016/j.neulet.2010.01.031. Epub 2010 Jan 25. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Signal transducer activity
Specific Function
This magnesium-dependent enzyme catalyzes the hydrolysis of ATP coupled with the transport of the calcium.
Gene Name
ATP2C1
Uniprot ID
P98194
Uniprot Name
Calcium-transporting ATPase type 2C member 1
Molecular Weight
100576.42 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Kosk-Kosicka D, Roszczynska G: Inhibition of plasma membrane Ca(2+)-ATPase activity by volatile anesthetics. Anesthesiology. 1993 Oct;79(4):774-80. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Transmitter-gated ion channel activity
Specific Function
The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
Gene Name
GLRA1
Uniprot ID
P23415
Uniprot Name
Glycine receptor subunit alpha-1
Molecular Weight
52623.35 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
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. Guo L, Wang Y: Glutamate stimulates glutamate receptor interacting protein 1 degradation by ubiquitin-proteasome system to regulate surface expression of GluR2. Neuroscience. 2007 Mar 2;145(1):100-9. Epub 2007 Jan 3. [Article]
  2. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inducer
General Function
Voltage-gated potassium channel activity
Specific Function
Voltage-gated potassium channel that mediates transmembrane potassium transport in excitable membranes, primarily in the brain and the central nervous system, but also in the kidney (PubMed:1990381...
Gene Name
KCNA1
Uniprot ID
Q09470
Uniprot Name
Potassium voltage-gated channel subfamily A member 1
Molecular Weight
56465.01 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Unknown
General Function
Transporter activity
Specific Function
Mitochondrial membrane ATP synthase (F(1)F(0) ATP synthase or Complex V) produces ATP from ADP in the presence of a proton gradient across the membrane which is generated by electron transport comp...
Gene Name
ATP5D
Uniprot ID
P30049
Uniprot Name
ATP synthase subunit delta, mitochondrial
Molecular Weight
17489.755 Da
References
  1. Pravdic D, Hirata N, Barber L, Sedlic F, Bosnjak ZJ, Bienengraeber M: Complex I and ATP synthase mediate membrane depolarization and matrix acidification by isoflurane in mitochondria. Eur J Pharmacol. 2012 Sep 5;690(1-3):149-57. doi: 10.1016/j.ejphar.2012.07.003. Epub 2012 Jul 11. [Article]
  2. Bains R, Moe MC, Vinje ML, Berg-Johnsen J: Isoflurane-induced depolarization of neural mitochondria increases with age. Acta Anaesthesiol Scand. 2009 Jan;53(1):85-92. doi: 10.1111/j.1399-6576.2008.01823.x. Epub 2008 Nov 12. [Article]
  3. Bains R, Moe MC, Larsen GA, Berg-Johnsen J, Vinje ML: Volatile anaesthetics depolarize neural mitochondria by inhibiton of the electron transport chain. Acta Anaesthesiol Scand. 2006 May;50(5):572-9. doi: 10.1111/j.1399-6576.2006.00988.x. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Titin binding
Specific Function
Calmodulin mediates the control of a large number of enzymes, ion channels, aquaporins and other proteins by Ca(2+). Among the enzymes to be stimulated by the calmodulin-Ca(2+) complex are a number...
Gene Name
CALM1
Uniprot ID
P0DP23
Uniprot Name
Calmodulin
Molecular Weight
16837.47 Da
References
  1. Fan RS, Jacamo RO, Jiang X, Sinnett-Smith J, Rozengurt E: G protein-coupled receptor activation rapidly stimulates focal adhesion kinase phosphorylation at Ser-843. Mediation by Ca2+, calmodulin, and Ca2+/calmodulin-dependent kinase II. J Biol Chem. 2005 Jun 24;280(25):24212-20. Epub 2005 Apr 21. [Article]
  2. Bickler PE, Zhan X, Fahlman CS: Isoflurane preconditions hippocampal neurons against oxygen-glucose deprivation: role of intracellular Ca2+ and mitogen-activated protein kinase signaling. Anesthesiology. 2005 Sep;103(3):532-9. [Article]
  3. Sazonova OV, Blishchenko EY, Tolmazova AG, Khachin DP, Leontiev KV, Karelin AA, Ivanov VT: Stimulation of fibroblast proliferation by neokyotorphin requires Ca influx and activation of PKA, CaMK II and MAPK/ERK. FEBS J. 2007 Jan;274(2):474-84. [Article]
Kind
Protein
Organism
Humans
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 permeabl...
Gene Name
CHRNA4
Uniprot ID
P43681
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-4
Molecular Weight
69956.47 Da
References
  1. Brannigan G, LeBard DN, Henin J, Eckenhoff RG, Klein ML: Multiple binding sites for the general anesthetic isoflurane identified in the nicotinic acetylcholine receptor transmembrane domain. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14122-7. doi: 10.1073/pnas.1008534107. Epub 2010 Jul 26. [Article]
  2. Flood P, Sonner JM, Gong D, Coates KM: Isoflurane hyperalgesia is modulated by nicotinic inhibition. Anesthesiology. 2002 Jul;97(1):192-8. [Article]
  3. Yamashita M, Mori T, Nagata K, Yeh JZ, Narahashi T: Isoflurane modulation of neuronal nicotinic acetylcholine receptors expressed in human embryonic kidney cells. Anesthesiology. 2005 Jan;102(1):76-84. [Article]
Kind
Protein
Organism
Humans
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 permeabl...
Gene Name
CHRNB2
Uniprot ID
P17787
Uniprot Name
Neuronal acetylcholine receptor subunit beta-2
Molecular Weight
57018.575 Da
References
  1. Brannigan G, LeBard DN, Henin J, Eckenhoff RG, Klein ML: Multiple binding sites for the general anesthetic isoflurane identified in the nicotinic acetylcholine receptor transmembrane domain. Proc Natl Acad Sci U S A. 2010 Aug 10;107(32):14122-7. doi: 10.1073/pnas.1008534107. Epub 2010 Jul 26. [Article]
  2. Flood P, Sonner JM, Gong D, Coates KM: Isoflurane hyperalgesia is modulated by nicotinic inhibition. Anesthesiology. 2002 Jul;97(1):192-8. [Article]
  3. Yamashita M, Mori T, Nagata K, Yeh JZ, Narahashi T: Isoflurane modulation of neuronal nicotinic acetylcholine receptors expressed in human embryonic kidney cells. Anesthesiology. 2005 Jan;102(1):76-84. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
Molecular Weight
56848.42 Da
References
  1. Kharasch ED, Thummel KE: Identification of cytochrome P450 2E1 as the predominant enzyme catalyzing human liver microsomal defluorination of sevoflurane, isoflurane, and methoxyflurane. Anesthesiology. 1993 Oct;79(4):795-807. [Article]
  2. Kharasch ED, Hankins DC, Cox K: Clinical isoflurane metabolism by cytochrome P450 2E1. Anesthesiology. 1999 Mar;90(3):766-71. doi: 10.1097/00000542-199903000-00019. [Article]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
  2. Baker MT, Olson MJ, Wang Y, Ronnenberg WC Jr, Johnson JT, Brady AN: Isoflurane-chlorodifluoroethene interaction in human liver microsomes. Role of cytochrome P4502B6 in potentiation of haloethene metabolism. Drug Metab Dispos. 1995 Jan;23(1):60-4. [Article]
  3. Potential CYP2B6 Substrates, Inhibitors, Inudcers (https://ctep.cancer.gov/protocoldevelopment/docs/cyp2b6.doc) [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Nadh dehydrogenase (ubiquinone) activity
Specific Function
Core subunit of the mitochondrial membrane respiratory chain NADH dehydrogenase (Complex I) that is believed to belong to the minimal assembly required for catalysis. Complex I functions in the tra...
Gene Name
MT-ND1
Uniprot ID
P03886
Uniprot Name
NADH-ubiquinone oxidoreductase chain 1
Molecular Weight
35660.055 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [Article]
  3. Hanley PJ, Ray J, Brandt U, Daut J: Halothane, isoflurane and sevoflurane inhibit NADH:ubiquinone oxidoreductase (complex I) of cardiac mitochondria. J Physiol. 2002 Nov 1;544(Pt 3):687-93. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. Liu R, Eckenhoff RG: Weak polar interactions confer albumin binding site selectivity for haloether anesthetics. Anesthesiology. 2005 Apr;102(4):799-805. [Article]
  2. 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]

Drug created on June 13, 2005 13:24 / Updated on October 22, 2021 23:18