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Economics

Properties

Spectra

Taxonomy

Isoflurane

Targets (10)Enzymes (3)Carriers (1)Biointeractions (13)

Identification

Name

Isoflurane

Accession Number

DB00753 (APRD00212)

Type

Small Molecule

Groups

Approved, Vet approved

Description

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

Structure

Similar Structures

Synonyms

1-chloro-2,2,2-trifluoroethyl difluoromethyl ether
Isoflurane
Isoflurano
Isofluranum

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Unlock Additional Data
Forane	Liquid	100 %	Respiratory (inhalation)	Baxter Laboratories	1996-12-31	Not applicable
Forane	Inhalant	1 mL/1mL	Respiratory (inhalation)	Baxter Laboratories	1979-12-18	Not applicable
Forane Liq Inh	Liquid		Respiratory (inhalation)	Ohmeda Pharmaceutical Products, Division Of Boc Canada Limited	1994-12-31	1996-09-26
Isoflurane USP	Liquid		Respiratory (inhalation)	Fresenius Kabi	1997-11-14	Not applicable
Isoflurane USP	Liquid		Respiratory (inhalation)	Abbvie	1993-12-31	2016-03-21
Isoflurane USP	Liquid		Respiratory (inhalation)	Halocarbon Laboratories, A Division Of Halocarbon Products Corp	2004-11-03	2019-03-22
Isoflurane USP	Liquid		Respiratory (inhalation)	Technilab Pharma Inc.	1999-01-21	2008-08-05

Additional Data Available

Application Number

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

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Product Code

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

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Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
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Isoflurane	Liquid	1 mL/1mL	Respiratory (inhalation)	Piramal Critical Care, Inc.	2011-10-07	Not applicable
Isoflurane	Liquid	1 mL/1mL	Respiratory (inhalation)	Halocarbon Products Corp.	1999-10-20	Not applicable
Isoflurane	Liquid	1 mL/1mL	Respiratory (inhalation)	Piramal Critical Care Inc	2013-11-13	Not applicable
Isoflurane	Liquid	1 mL/1mL	Respiratory (inhalation)	Hospira, Inc.	2005-08-01	2012-03-01
Terrell	Liquid	1 mL/1mL	Respiratory (inhalation)	Piramal Critical Care Inc	2012-03-21	Not applicable
Terrell	Liquid	1 mL/1mL	Respiratory (inhalation)	Piramal Critical Care Inc	2010-02-28	Not applicable

Additional Data Available

Application Number

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

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Product Code

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

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International/Other Brands

Aerrane (Baxter) / Forene (Abbott) / Isocane (Lunan) / Isorane (Abbott)

Categories

UNII

CYS9AKD70P

CAS number

26675-46-7

Weight

Average: 184.492
Monoisotopic: 183.971433418

Chemical Formula

C₃H₂ClF₅O

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

Pharmacology

Indication

For induction and maintenance of general anesthesia.

Associated Therapies

Anesthesia induction and maintenance therapy

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.

Target	Actions	Organism
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 (anion channel)	positive allosteric modulator	Humans
UNeuronal acetylcholine receptor subunit alpha-4	antagonist	Humans
UNeuronal acetylcholine receptor subunit beta-2	antagonist	Humans

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Additional Data Available

Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available

Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available

Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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

Toxicity

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

Affected organisms

Humans and other mammals

Pathways

Not Available

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Voltage-dependent L-type calcium channel subunit alpha-1S	---	Not Available	c.3257G>A / c.520C>T	ADR Inferred	Malignant hyperthermia.	Details
Ryanodine receptor 1	---	Not Available	c.103T>C / c.487C>T … show all	ADR Inferred	Malignant 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.

Drug	Interaction
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1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid	The risk or severity of hypertension can be increased when Isoflurane is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid.
1-benzylimidazole	The risk or severity of hypertension can be increased when Isoflurane is combined with 1-benzylimidazole.
1,10-Phenanthroline	The therapeutic efficacy of Isoflurane can be decreased when used in combination with 1,10-Phenanthroline.
2,5-Dimethoxy-4-ethylamphetamine	The risk or severity of hypertension can be increased when Isoflurane is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine	The risk or severity of adverse effects can be increased when Isoflurane is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine	The risk or severity of adverse effects can be increased when Isoflurane is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine	The risk or severity of adverse effects can be increased when Isoflurane is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine	The risk or severity of adverse effects can be increased when Isoflurane is combined with 5-methoxy-N,N-dimethyltryptamine.
7-Nitroindazole	The risk or severity of adverse effects can be increased when Isoflurane is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline	7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Isoflurane.

Additional Data Available

Extended Description

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

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Severity

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

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Evidence Level

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

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Action

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

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Food Interactions

Not Available

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

External Links

Human Metabolome Database: HMDB0014891
KEGG Drug: D00545
KEGG Compound: C07518
PubChem Compound: 3763
PubChem Substance: 46505880
ChemSpider: 3631
BindingDB: 217353
ChEBI: 6015
ChEMBL: CHEMBL1256
Therapeutic Targets Database: DAP001033
PharmGKB: PA450106
HET: ICF
RxList: RxList Drug Page
Wikipedia: Isoflurane

ATC Codes

N01AB06 — Isoflurane

AHFS Codes

28:04.16 — Inhalation Anesthetics

FDA label

Download (99.6 KB)

MSDS

Download (37 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
1	Completed	Diagnostic	Adjunct to general anesthesia therapy	1
1	Completed	Treatment	Adverse Effect of Intravenous Anesthetics	1
1	Recruiting	Screening	Heart Diseases	1
2	Completed	Diagnostic	Kidney Transplant; Complications	1
2	Completed	Treatment	Opioid-Related Disorders / Substance-Related Disorders	2
2, 3	Active Not Recruiting	Treatment	Myocardial Injury	1
2, 3	Unknown Status	Prevention	Focus of Study is to Assess the Smooth LMA Removal by Measuring the Adverse Airway Outcomes Like; Airway Obstruction, Laryngospasm and Bronchospasm	1
3	Completed	Treatment	Renal Function After Partial Nephrectomy	1
3	Not Yet Recruiting	Treatment	Anaesthesia therapy	1
3	Terminated	Prevention	Hydrocephaly / Therapeutic Agent Toxicity	1
3	Withdrawn	Treatment	Inguinal Hernias	1
4	Completed	Diagnostic	Alzheimers Disease / Post Operative Cognitive Dysfunction / Postoperative Delirium	1
4	Completed	Diagnostic	Postoperative Delirium	1
4	Completed	Diagnostic	Pulmonary Hypertension (PH)	1
4	Completed	Supportive Care	Acute Subdural Hematoma	1
4	Completed	Supportive Care	DNA Damage / Patients in Good Health / Types of General Anesthesia	1
4	Completed	Supportive Care	Patients in Good Health	1
4	Completed	Treatment	Advanced Chronic Rhinosinusitis	1
4	Completed	Treatment	Coronary Artery Bypass Graft Surgery Patients / Surgery, Cardiac	1
4	Completed	Treatment	Myocardial Reperfusion Injury	1
4	Completed	Treatment	Neoplasms, Breast	1
4	Completed	Treatment	Strokes / Subarachnoid Hemorrhage	1
4	Enrolling by Invitation	Treatment	Anesthesia Complication / Hemodynamics Instability / Ileus paralytic / Nausea / Postoperative pain / Vomiting	1
4	Not Yet Recruiting	Treatment	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD)	1
4	Recruiting	Other	Cancer Colorectal / Cancer Melanoma Skin / Cancer Prostate / Cancer, Breast / Cancer, Other / Lung Cancers	1
4	Recruiting	Prevention	Delirium	1
4	Recruiting	Treatment	Coronary Artery Bypass Graft Triple Vessel	1
4	Terminated	Diagnostic	Ventricular Dysfunction / Young Healthy Adults	1
4	Terminated	Prevention	Delirium on Emergence	1
4	Terminated	Treatment	Arterial Hypotension	1
4	Terminated	Treatment	Disorder; Heart, Functional, Postoperative, Cardiac Surgery / Heart; Dysfunction Postoperative, Cardiac Surgery	1
4	Terminated	Treatment	Renal Failure	1
4	Unknown Status	Treatment	Perioperative Blood Glucose and Insulin	1
4	Withdrawn	Treatment	Sleep	1
Not Available	Active Not Recruiting	Prevention	Alzheimer's Disease (AD) / Dementias	1
Not Available	Active Not Recruiting	Prevention	Anesthesia; Adverse Effect / Congenital Heart Disease (CHD) / Neurodevelopmental Disorders	1
Not Available	Active Not Recruiting	Treatment	Intubated Requiring Sedation for Greater Than 48 Hours	1
Not Available	Completed	Not Available	Anaesthesia	1
Not Available	Completed	Not Available	Neurotoxic Effect of Sevoflurane‑Based Anaesthesia	1
Not Available	Completed	Not Available	Off Pump Coronary Artery Bypass Graft	1
Not Available	Completed	Basic Science	Pharmacokinetics of Inhaled Anesthetics	1
Not Available	Completed	Basic Science	Postoperative Cognitive Dysfunction	1
Not Available	Completed	Health Services Research	Delayed Recovery From Anaesthesia	1
Not Available	Completed	Health Services Research	Intensive Care Unit Syndrome	1
Not Available	Completed	Prevention	Arterial Hypotension	1
Not Available	Completed	Prevention	Post-Operative Nausea and Vomiting (PONV)	1
Not Available	Completed	Prevention	Surgery, Cardiac	1
Not Available	Completed	Treatment	Cervical Spondylosis / Knee Osteoarthritis (Knee OA) / Lumbar Spondylosis / Osteoarthritis, Hip	1
Not Available	Completed	Treatment	Ischaemic Heart Diseases / Valvular Heart Disease	1
Not Available	Completed	Treatment	Postoperative pain	1
Not Available	Completed	Treatment	Adjunct to general anesthesia therapy	1
Not Available	Enrolling by Invitation	Basic Science	Cancer Larynx / Total Laryngectomy	1
Not Available	Not Yet Recruiting	Treatment	Colonic Neoplasms	1
Not Available	Recruiting	Treatment	Sepsis	1
Not Available	Terminated	Not Available	Abdominal Aortic Aneurysms (AAA) / Open Thoracoabdominal Aneurysm Repair / Thoracoabdominal Aneursym Repair With Cardiopulmonary Bypass / Thoracoabdominal Aneursym Stent / Thoracoabdominal Aneurysm Repair With Cardiopulmonary Bypass / Thoracoabdominal Aneurysm Stent	1
Not Available	Terminated	Diagnostic	Parkinson's Disease (PD)	1
Not Available	Terminated	Treatment	Liver Diseases	1
Not Available	Unknown Status	Health Services Research	Duration of Hospitalization	1
Not Available	Unknown Status	Supportive Care	Adjunct to general anesthesia therapy	1

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

Form	Route	Strength
Inhalant	Respiratory (inhalation)	1 mL/1mL
Liquid	Respiratory (inhalation)	100 %
Liquid	Respiratory (inhalation)	1 mL/1mL
Liquid	Respiratory (inhalation)

Prices

Unit description	Cost	Unit
Forane liquid	0.24USD	ml

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Not Available

Properties

State

Liquid

Experimental Properties

Property	Value	Source
melting point (°C)	48-48.5	U.S. Patent 3,535,388.
boiling point (°C)	48.5 °C	PhysProp
water solubility	4470 mg/L (at 37 °C)	YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP	2.06	HANSCH,C ET AL. (1995)

Predicted Properties

Property	Value	Source
Water Solubility	3.56 mg/mL	ALOGPS
logP	2.3	ALOGPS
logP	2.84	ChemAxon
logS	-1.7	ALOGPS
pKa (Strongest Basic)	-4.7	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	23.04 m³·mol^-1	ChemAxon
Polarizability	9.73 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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Download (7.33 KB)

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Mass Spectrum (Electron Ionization)	MS	splash10-0udi-9300000000-c134e176400bbe7073c2
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 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: Organic oxygen compound / Hydrocarbon derivative / Organooxygen compound / Organofluoride / Organochloride / Alkyl halide / Alkyl fluoride / Alkyl chloride / Aliphatic acyclic compound
Molecular Framework: Aliphatic acyclic compounds
External Descriptors: organofluorine compound (CHEBI:6015)

Targets

Details1. Gamma-aminobutyric acid receptor subunit alpha-1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]
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. [PubMed:20826568]
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. [PubMed:20097266]

Details2. Calcium-transporting ATPase type 2C member 1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]
Kosk-Kosicka D, Roszczynska G: Inhibition of plasma membrane Ca(2+)-ATPase activity by volatile anesthetics. Anesthesiology. 1993 Oct;79(4):774-80. [PubMed:8214757]

Details3. Glycine receptor subunit alpha-1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]
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. Epub 2006 Sep 13. [PubMed:16973644]

Details4. Glutamate receptor 1

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

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. [PubMed:17207582]
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. [PubMed:8786535]

Details5. Potassium voltage-gated channel subfamily A member 1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]
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. [PubMed:19298752]

Details6. ATP synthase subunit delta, mitochondrial

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]

Details7. Calmodulin

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

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. [PubMed:15845548]
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. [PubMed:16129978]
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. [PubMed:17229152]

Details8. GABA-A receptor (anion channel) (Protein Group)

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:

Name	UniProt ID
Gamma-aminobutyric acid receptor subunit alpha-1	P14867
Gamma-aminobutyric acid receptor subunit alpha-2	P47869
Gamma-aminobutyric acid receptor subunit alpha-3	P34903
Gamma-aminobutyric acid receptor subunit alpha-4	P48169
Gamma-aminobutyric acid receptor subunit alpha-5	P31644
Gamma-aminobutyric acid receptor subunit alpha-6	Q16445
Gamma-aminobutyric acid receptor subunit beta-1	P18505
Gamma-aminobutyric acid receptor subunit beta-2	P47870
Gamma-aminobutyric acid receptor subunit beta-3	P28472
Gamma-aminobutyric acid receptor subunit delta	O14764
Gamma-aminobutyric acid receptor subunit epsilon	P78334
Gamma-aminobutyric acid receptor subunit gamma-1	Q8N1C3
Gamma-aminobutyric acid receptor subunit gamma-2	P18507
Gamma-aminobutyric acid receptor subunit gamma-3	Q99928
Gamma-aminobutyric acid receptor subunit pi	O00591
Gamma-aminobutyric acid receptor subunit theta	Q9UN88

References

ChEMBL Compound Report Card [Link]

Details9. Neuronal acetylcholine receptor subunit alpha-4

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

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. [PubMed:20660787]
Flood P, Sonner JM, Gong D, Coates KM: Isoflurane hyperalgesia is modulated by nicotinic inhibition. Anesthesiology. 2002 Jul;97(1):192-8. [PubMed:12131122]
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. [PubMed:15618790]

Details10. Neuronal acetylcholine receptor subunit beta-2

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

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. [PubMed:20660787]
Flood P, Sonner JM, Gong D, Coates KM: Isoflurane hyperalgesia is modulated by nicotinic inhibition. Anesthesiology. 2002 Jul;97(1):192-8. [PubMed:12131122]
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. [PubMed:15618790]

Enzymes

Details1. Cytochrome P450 2E1

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

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. [PubMed:8214760]
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. [PubMed:10078678]
Flockhart Table of Drug Interactions [Link]

Details2. Cytochrome P450 2B6

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate
Inhibitor
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

Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
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. [PubMed:7720526]
Potential CYP2B6 Substrates, Inhibitors, Inudcers (https://ctep.cancer.gov/protocoldevelopment/docs/cyp2b6.doc) [File]

Details3. NADH-ubiquinone oxidoreductase chain 1

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

Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
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. [PubMed:17016423]
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. [PubMed:12411515]

Carriers

Details1. Serum albumin

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

Liu R, Eckenhoff RG: Weak polar interactions confer albumin binding site selectivity for haloether anesthetics. Anesthesiology. 2005 Apr;102(4):799-805. [PubMed:15791110]
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. [PubMed:15449957]

Drug created on June 13, 2005 07:24 / Updated on October 22, 2019 18:27

Isoflurane

Identification

Structure for Isoflurane (DB00753)

Pharmacology

Interactions

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

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Components:

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Enzymes

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Carriers

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