Desflurane

Identification

Summary

Desflurane is a general inhalation anesthetic for inpatient and outpatient surgery in adults.

Brand Names
Suprane
Generic Name
Desflurane
DrugBank Accession Number
DB01189
Background

Desflurane, or I-653, a a volatile anesthetic that is more rapidly cleared and less metabolized than previous inhaled anesthetics such as methoxyflurane, sevoflurane, enflurane, or isoflurane.4,2,21. It was developed in the late 1980s out of a need for a more rapidly acting and rapidly cleared inhaled anesthetic.19,20

Desflurane was granted FDA approval on 18 September 1992.22

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 168.0378
Monoisotopic: 168.000983916
Chemical Formula
C3H2F6O
Synonyms
  • (±)-2-difluoromethyl 1,2,2,2-tetrafluoroethyl ether
  • 1,1,1,2-tetrafluoro-2-(difluoromethoxy)ethane
  • Desflurane
  • Desflurano
  • Desfluranum
  • Difluoromethyl 1,2,2,2-tetrafluoroethyl ether

Pharmacology

Indication

Desflurane is indicated for the induction and maintenance of anesthesia in adults, as well as the maintenance of anesthesia in pediatric patients.22

Pharmacology
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Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Desflurane is a general inhalation anesthetic.22 It has a short duration of action as it is rapidly cleared.22 Patients should be counselled regarding the risks of malignant hyperthermia, perioperative hyperkalemia, respiratory adverse reactions in pediatric patients, QTc prolongation, hepatobiliary disorders, pediatric neurotoxicity, and postoperative agitation in children.22

Mechanism of action

The mechanism of inhalational anesthetics is still not fully understood.5 They can block excitatory ion channels and increase the activity of inhibitory ion channels.5 The most notable agonism is at the GABAA channel.9 Desflurane is also an agonist of glycine receptors,10 antagonist of glutamate receptors,11 inducer of potassium voltage gated channels,12 and inhibits both NADH-ubiquinone oxioreductase chain 113 and calcium transporting ATPases.14

An older school of thought is the unitary theory of general anesthetic action, suggesting that desflurane affects the lipid bilayer of cells.5,7 Studies of other halogenated inhalational anesthetics have shown that the lipid bilayer spreads out more thinly as the anesthetic incorporates into the bilayer.6 However, the anesthetic does not bind to lipid heads or acyl chains of hydrocarbons in the bilayer.6 The effect of incorporating into the lipid bilayer is not well described.6,22 By incorporating into the lipid bilayer, anesthetics may introduce disorder in the lipids, leading to some indirect effect on ion channels.7 However, this theory remains controversial.8

TargetActionsOrganism
AGABA(A) Receptor
positive allosteric modulator
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
other/unknown
Humans
ANADH-ubiquinone oxidoreductase chain 1
inhibitor
Humans
ACalcium transporting ATPases
inhibitor
Humans
Absorption

Data regarding the Cmax, Tmax, and AUC of desflurane are not readily available.22

Volume of distribution

Desflurane has a median volume of distribution of 612 mL/kg.18

Protein binding

Desflurane is bound to human serum albumin in plasma.17

Metabolism

Desflurane is minimally defluorinated by CYP2E1,2 to the extent that serum fluoride levels do not increase above baseline levels.4

Hover over products below to view reaction partners

Route of elimination

Initially, desflurane is rapidly eliminated from the lungs.16 A small amount of the metabolite trifluoroacetic acid is eliminated in the urine3 and only 0.02% of an inhaled dose is recovered as urinary metabolites.22

Half-life

Desflurane has a terminal elimination half life of 8.16 ± 3.15 minutes.15

Clearance

A 26 g dose of desflurane is 90% eliminated from the brain after 33 hours.1 The metabolite trifluoroacetic acid has a urinary clearance rate of 0.169 ± 0.107 µmol/L.4

Adverse Effects
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Toxicity

Patients experiencing a desflurane overdose may experience deepening anesthesia, cardiac or respiratory depression.22 In the event of an overdose, patients may require symptomatic and supportive treatment to maintain airway, breathing, and circulation.22 Discontinue desflurane.22

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 Desflurane is combined with 1,2-Benzodiazepine.
AceclofenacThe risk or severity of hypertension can be increased when Desflurane is combined with Aceclofenac.
AcemetacinThe risk or severity of hypertension can be increased when Desflurane is combined with Acemetacin.
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Desflurane.
AcetophenazineThe risk or severity of adverse effects can be increased when Acetophenazine is combined with Desflurane.
Acetylsalicylic acidThe risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with Desflurane.
AclidiniumDesflurane may increase the central nervous system depressant (CNS depressant) activities of Aclidinium.
AcrivastineThe risk or severity of QTc prolongation can be increased when Desflurane is combined with Acrivastine.
AdenosineThe risk or severity of QTc prolongation can be increased when Desflurane is combined with Adenosine.
AgomelatineThe risk or severity of adverse effects can be increased when Desflurane is combined with Agomelatine.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DesfluraneLiquid100 % v/vRespiratory (inhalation)Blue Zone Technologies LtdNot applicableNot applicableCanada flag
SupraneLiquid240 mL/240mLRespiratory (inhalation)Baxter Healthcare Corporation1992-09-18Not applicableUS flag
SupraneLiquid240 mL/240mLRespiratory (inhalation)Baxter Healthcare Corporation1992-09-18Not applicableUS flag
SupraneLiquid240 mL/240mLRespiratory (inhalation)General Injectables & Vaccines, Inc2012-04-25Not applicableUS flag
SupraneLiquid1.5 g/1mLRespiratory (inhalation)Baxter Healthcare Corporation2006-08-142006-08-14US flag
SupraneLiquid240 mL/240mLRespiratory (inhalation)Baxter Healthcare Corporation1992-09-18Not applicableUS flag
SupraneLiquid100 % v/vRespiratory (inhalation)Baxter Laboratories1996-12-23Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DesfluraneLiquid240 mL/240mLRespiratory (inhalation)Sandoz Inc.2018-02-26Not applicableUS flag

Categories

ATC Codes
N01AB07 — Desflurane
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 / Hydrocarbon derivatives / Alkyl fluorides
Substituents
Aliphatic acyclic compound / Alkyl fluoride / Alkyl halide / Hydrocarbon derivative / Organic oxygen compound / Organofluoride / Organooxygen compound
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
organofluorine compound (CHEBI:4445)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
CRS35BZ94Q
CAS number
57041-67-5
InChI Key
DPYMFVXJLLWWEU-UHFFFAOYSA-N
InChI
InChI=1S/C3H2F6O/c4-1(3(7,8)9)10-2(5)6/h1-2H
IUPAC Name
2-(difluoromethoxy)-1,1,1,2-tetrafluoroethane
SMILES
FC(F)OC(F)C(F)(F)F

References

Synthesis Reference

Leonid A. Rozov, Chialang Huang, Gerald G. Vernice, "Synthesis of desflurane." U.S. Patent US5205914, issued June, 1991.

US5205914
General References
  1. Lockwood G: Theoretical context-sensitive elimination times for inhalation anaesthetics. Br J Anaesth. 2010 May;104(5):648-55. doi: 10.1093/bja/aeq051. Epub 2010 Mar 16. [Article]
  2. 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]
  3. Koblin DD: Characteristics and implications of desflurane metabolism and toxicity. Anesth Analg. 1992 Oct;75(4 Suppl):S10-6. [Article]
  4. Sutton TS, Koblin DD, Gruenke LD, Weiskopf RB, Rampil IJ, Waskell L, Eger EI 2nd: Fluoride metabolites after prolonged exposure of volunteers and patients to desflurane. Anesth Analg. 1991 Aug;73(2):180-5. doi: 10.1213/00000539-199108000-00011. [Article]
  5. Khan J, Liu M: Desflurane . [Article]
  6. Tu K, Tarek M, Klein ML, Scharf D: Effects of anesthetics on the structure of a phospholipid bilayer: molecular dynamics investigation of halothane in the hydrated liquid crystal phase of dipalmitoylphosphatidylcholine. Biophys J. 1998 Nov;75(5):2123-34. doi: 10.1016/S0006-3495(98)77655-6. [Article]
  7. Krasowski MD: Contradicting a unitary theory of general anesthetic action: a history of three compounds from 1901 to 2001. Bull Anesth Hist. 2003 Jul;21(3):1, 4-8, 21 passim. doi: 10.1016/s1522-8649(03)50031-2. [Article]
  8. Herold KF, Sanford RL, Lee W, Andersen OS, Hemmings HC Jr: Clinical concentrations of chemically diverse general anesthetics minimally affect lipid bilayer properties. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3109-3114. doi: 10.1073/pnas.1611717114. Epub 2017 Mar 6. [Article]
  9. Ton HT, Phan TX, Abramyan AM, Shi L, Ahern GP: Identification of a putative binding site critical for general anesthetic activation of TRPA1. Proc Natl Acad Sci U S A. 2017 Apr 4;114(14):3762-3767. doi: 10.1073/pnas.1618144114. Epub 2017 Mar 20. [Article]
  10. 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]
  11. 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]
  12. 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]
  13. 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]
  14. Kosk-Kosicka D: Plasma membrane Ca(2+)-ATPase as a target for volatile anesthetics. Adv Pharmacol. 1994;31:313-22. [Article]
  15. Behne M, Wilke HJ, Lischke V: Recovery and pharmacokinetic parameters of desflurane, sevoflurane, and isoflurane in patients undergoing urologic procedures. J Clin Anesth. 1999 Sep;11(6):460-5. doi: 10.1016/s0952-8180(99)00082-3. [Article]
  16. Lu CC, Tsai CS, Hu OY, Chen RM, Chen TL, Ho ST, Gan TJ: Pharmacokinetics of desflurane elimination from respiratory gas and blood during the 20 minutes after cardiac surgery. J Formos Med Assoc. 2013 Apr;112(4):185-92. doi: 10.1016/j.jfma.2012.01.017. Epub 2012 May 20. [Article]
  17. 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]
  18. Wissing H, Kuhn I, Rietbrock S, Fuhr U: Pharmacokinetics of inhaled anaesthetics in a clinical setting: comparison of desflurane, isoflurane and sevoflurane. Br J Anaesth. 2000 Apr;84(4):443-9. doi: 10.1093/oxfordjournals.bja.a013467. [Article]
  19. Eger EI 2nd: Partition coefficients of I-653 in human blood, saline, and olive oil. Anesth Analg. 1987 Oct;66(10):971-3. [Article]
  20. Eger EI 2nd, Johnson BH: Rates of awakening from anesthesia with I-653, halothane, isoflurane, and sevoflurane: a test of the effect of anesthetic concentration and duration in rats. Anesth Analg. 1987 Oct;66(10):977-82. [Article]
  21. Eger EI 3rd: Stability of I-653 in soda lime. Anesth Analg. 1987 Oct;66(10):983-5. [Article]
  22. FDA Approved Drug Products: Suprane (Desflurane) Inhalational Liquid [Link]
Human Metabolome Database
HMDB0015320
KEGG Drug
D00546
KEGG Compound
C07519
PubChem Compound
42113
PubChem Substance
46505270
ChemSpider
38403
RxNav
27340
ChEBI
4445
ChEMBL
CHEMBL1200733
Therapeutic Targets Database
DAP000693
PharmGKB
PA164749136
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Desflurane
AHFS Codes
  • 28:04.16 — Inhalation Anesthetics
FDA label
Download (174 KB)
MSDS
Download (51.1 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedBasic ScienceAnaesthesia therapy / BMI >30 kg/m21
4CompletedBasic ScienceAnesthesia; Bariatric Surgery1
4CompletedDiagnosticAnaesthesia1
4CompletedDiagnosticOxygen Saturation1
4CompletedDiagnosticPostoperative Delirium1
4CompletedHealth Services ResearchEmergence Agitation1
4CompletedOtherAnaesthesia therapy1
4CompletedOtherLung Volume Reduction Surgery1
4CompletedPreventionEnd Stage Liver Diseases1
4CompletedPreventionEnd Stage Renal Disease (ESRD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Baxter International Inc.
  • General Injectables and Vaccines Inc.
Dosage Forms
FormRouteStrength
SolutionRespiratory (inhalation)
AerosolRespiratory (inhalation)100 ml/100ml
InhalantRespiratory (inhalation)
LiquidRespiratory (inhalation)1.5 g/1mL
LiquidRespiratory (inhalation)100 % v/v
LiquidRespiratory (inhalation)240 mL/240mL
LiquidRespiratory (inhalation)
SolutionRespiratory (inhalation)100 mL
Prices
Unit descriptionCostUnit
Suprane inhalation liquid0.76USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5617906No1997-04-082014-10-08US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
boiling point (°C)22.8 °Chttps://imgcdn.mckesson.com/CumulusWeb/Click_and_learn/SDS_9BAXAC_SUPRANE_INH_LIQ_240ML_6CT.pdf
water solubilityNegligibleNot Available
Predicted Properties
PropertyValueSource
Water Solubility3.54 mg/mLALOGPS
logP2.19ALOGPS
logP2.4ChemAxon
logS-1.7ALOGPS
pKa (Strongest Acidic)18.87ChemAxon
pKa (Strongest Basic)-4.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area9.23 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity18.12 m3·mol-1ChemAxon
Polarizability7.89 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9974
Blood Brain Barrier+0.9941
Caco-2 permeable+0.626
P-glycoprotein substrateNon-substrate0.883
P-glycoprotein inhibitor INon-inhibitor0.9415
P-glycoprotein inhibitor IINon-inhibitor0.9027
Renal organic cation transporterNon-inhibitor0.9311
CYP450 2C9 substrateNon-substrate0.8676
CYP450 2D6 substrateNon-substrate0.919
CYP450 3A4 substrateNon-substrate0.7556
CYP450 1A2 substrateNon-inhibitor0.6194
CYP450 2C9 inhibitorNon-inhibitor0.836
CYP450 2D6 inhibitorNon-inhibitor0.9466
CYP450 2C19 inhibitorNon-inhibitor0.707
CYP450 3A4 inhibitorNon-inhibitor0.9604
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8921
Ames testNon AMES toxic0.9042
CarcinogenicityCarcinogens 0.7045
BiodegradationNot ready biodegradable0.9566
Rat acute toxicity1.2690 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9724
hERG inhibition (predictor II)Non-inhibitor0.909
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
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

Drugtargets
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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. Mohler H, Fritschy JM, Rudolph U: A new benzodiazepine pharmacology. J Pharmacol Exp Ther. 2002 Jan;300(1):2-8. [Article]
  2. Riss J, Cloyd J, Gates J, Collins S: Benzodiazepines in epilepsy: pharmacology and pharmacokinetics. Acta Neurol Scand. 2008 Aug;118(2):69-86. doi: 10.1111/j.1600-0404.2008.01004.x. Epub 2008 Mar 31. [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. 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. 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
Other/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. 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
Inhibitor
Curator comments
This action is based on the activity of other volatile anesthetics on this target. It is a potential target for desflurane.
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. 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]
  2. Kayser EB, Suthammarak W, Morgan PG, Sedensky MM: Isoflurane selectively inhibits distal mitochondrial complex I in Caenorhabditis elegans. Anesth Analg. 2011 Jun;112(6):1321-9. doi: 10.1213/ANE.0b013e3182121d37. Epub 2011 Apr 5. [Article]
Kind
Protein group
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.

Components:
References
  1. Kosk-Kosicka D: Plasma membrane Ca(2+)-ATPase as a target for volatile anesthetics. Adv Pharmacol. 1994;31:313-22. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
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]

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. 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 June 13, 2021 16:24