Halothane

Identification

Summary

Halothane is a general inhalation anesthetic used for the induction and maintenance of general anesthesia.

Generic Name
Halothane
DrugBank Accession Number
DB01159
Background

A nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. nitrous oxide is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required. (From AMA Drug Evaluations Annual, 1994, p178)

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Weight
Average: 197.382
Monoisotopic: 195.890225001
Chemical Formula
C2HBrClF3
Synonyms
  • 1-bromo-1-chloro-2,2,2-trifluoroethane
  • 1,1,1-trifluoro-2-bromo-2-chloroethane
  • 1,1,1-trifluoro-2-chloro-2-bromoethane
  • 2-bromo-2-chloro-1,1,1-trifluoroethane
  • 2,2,2-trifluoro-1-chloro-1-bromoethane
  • Alotano
  • Bromochlorotrifluoroethane
  • Halotano
  • Halothane
  • Halothanum

Pharmacology

Indication

For the induction and maintenance of general anesthesia

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Maintenance ofAnaesthesia therapy•••••••••••••••••••• ••••••••• ••••••
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Pharmacodynamics

Halothane is a general inhalation anesthetic used for induction and maintenance of general anesthesia. It reduces the blood pressure and frequently decreases the pulse rate and depresses respiration. 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

Halothane causes general anaethesia due to its actions on multiple ion channels, which ultimately depresses nerve conduction, breathing, cardiac contractility. Its immobilizing effects have been attributed to its binding to potassium channels in cholinergic neurons. Halothane's effect are also likely due to binding to NMDA and calcium channels, causing hyperpolarization.

TargetActionsOrganism
APotassium channel subfamily K member 3
binder
Humans
APotassium channel subfamily K member 9
binder
Humans
AGABA(A) Receptor
positive allosteric modulator
Humans
APlasma membrane calcium-transporting ATPase
inhibitor
Humans
UCalcium-activated potassium channel subunit alpha-1
inhibitor
Humans
UGlutamate receptor ionotropic, NMDA 3A
antagonist
Humans
UGlutamate receptor ionotropic, NMDA 3B
antagonist
Humans
UGlutamate receptor ionotropic, NMDA 2A
antagonist
Humans
UGlycine receptor subunit alpha-1
allosteric modulator
Humans
URhodopsin
other
Humans
UG protein-activated inward rectifier potassium channel 2
inhibitor
Humans
UG protein-activated inward rectifier potassium channel 1
inhibitor
Humans
UNADH-ubiquinone oxidoreductase chain 1
inhibitor
Humans
UIntermediate conductance calcium-activated potassium channel protein 4
inhibitor
Humans
UGamma-aminobutyric acid receptor subunit alpha-1
other/unknown
Humans
UGuanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
other/unknown
Humans
UNeuropeptide S receptor
other/unknown
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism

Halothane is metabolized in the liver, primarily by CYP2E1, and to a lesser extent by CYP3A4 and CYP2A6.

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Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
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Toxicity

Toxic effects of halothane include malignant hyperthermia and hepatitis.

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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Halothane is combined with 1,2-Benzodiazepine.
AbaloparatideThe risk or severity of adverse effects can be increased when Halothane is combined with Abaloparatide.
AbametapirThe serum concentration of Halothane can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Halothane can be increased when combined with Abatacept.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Halothane.
Food Interactions
No interactions found.

Products

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International/Other Brands
Fluothane (Ayerst) / Ftorotan / Halotan (Jugoremedija) / Narcotan (Zentiva)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Fluothane AnestheticLiquidRespiratory (inhalation)Ayerst Laboratories1958-12-311996-09-10Canada flag
Fluothane Liq Inh 1000mg/gmLiquid1 g / gRespiratory (inhalation)Wyeth Ayerst Canada Inc.1994-12-311997-08-14Canada flag
HalothaneSolution99.99 %Respiratory (inhalation)Bimeda Mtc Animal Health Inc1975-12-312018-07-27Canada flag
Halothane Liq 99.9%Liquid99.9 %Respiratory (inhalation)Halocarbon Laboratories, A Division Of Halocarbon Products Corp1971-12-312010-06-14Canada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
HalothaneInhalant250 mL/250mLRespiratory (inhalation)Hospira, Inc.1975-05-302012-07-26US flag

Categories

ATC Codes
N01AB01 — Halothane
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
Organochlorides / Organobromides / Hydrocarbon derivatives / Alkyl fluorides / Alkyl chlorides / Alkyl bromides
Substituents
Aliphatic acyclic compound / Alkyl bromide / Alkyl chloride / Alkyl fluoride / Alkyl halide / Hydrocarbon derivative / Organobromide / Organochloride / Organofluoride
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
haloalkane (CHEBI:5615)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
UQT9G45D1P
CAS number
151-67-7
InChI Key
BCQZXOMGPXTTIC-UHFFFAOYSA-N
InChI
InChI=1S/C2HBrClF3/c3-1(4)2(5,6)7/h1H
IUPAC Name
2-bromo-2-chloro-1,1,1-trifluoroethane
SMILES
[H]C(Cl)(Br)C(F)(F)F

References

Synthesis Reference

U.S. Patents 2,849,502, 2,921,098, 2,959,624, 3,082,263.

General References
  1. Bovill JG: Inhalation anaesthesia: from diethyl ether to xenon. Handb Exp Pharmacol. 2008;(182):121-42. doi: 10.1007/978-3-540-74806-9_6. [Article]
Human Metabolome Database
HMDB0015290
KEGG Drug
D00542
KEGG Compound
C07515
PubChem Compound
3562
PubChem Substance
46506589
ChemSpider
3441
BindingDB
50112212
RxNav
5095
ChEBI
5615
ChEMBL
CHEMBL931
Therapeutic Targets Database
DAP000692
PharmGKB
PA449845
Guide to Pharmacology
GtP Drug Page
PDBe Ligand
HLT
RxList
RxList Drug Page
Wikipedia
Halothane
MSDS
Download (55.2 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
Not AvailableCompletedTreatmentGeneral Anesthesia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Halocarbon Laboratories
  • Hospira Inc.
Dosage Forms
FormRouteStrength
AerosolRespiratory (inhalation)
LiquidRespiratory (inhalation)100 %
LiquidRespiratory (inhalation)
LiquidRespiratory (inhalation)1 g / g
SolutionRespiratory (inhalation)100 mL
InhalantRespiratory (inhalation)250 mL/250mL
SolutionRespiratory (inhalation)99.09 mg
SolutionRespiratory (inhalation)99.99 %
LiquidRespiratory (inhalation)99.9 %
Prices
Unit descriptionCostUnit
Halothane 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)50-50.5U.S. Patents 2,849,502, 2,921,098, 2,959,624, 3,082,263.
boiling point (°C)50.2 °CPhysProp
water solubility4070 mg/L (at 25 °C)HORVATH,AL ET AL. (1999)
logP2.30HANSCH,C ET AL. (1995)
logS-1.71ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility3.81 mg/mLALOGPS
logP2.5ALOGPS
logP2.12Chemaxon
logS-1.7ALOGPS
Physiological Charge0Chemaxon
Hydrogen Acceptor Count0Chemaxon
Hydrogen Donor Count0Chemaxon
Polar Surface Area0 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity24.63 m3·mol-1Chemaxon
Polarizability9.78 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+0.9895
Caco-2 permeable+0.6141
P-glycoprotein substrateNon-substrate0.9007
P-glycoprotein inhibitor INon-inhibitor0.9628
P-glycoprotein inhibitor IINon-inhibitor0.945
Renal organic cation transporterNon-inhibitor0.9183
CYP450 2C9 substrateNon-substrate0.8374
CYP450 2D6 substrateSubstrate0.8031
CYP450 3A4 substrateNon-substrate0.7086
CYP450 1A2 substrateNon-inhibitor0.6027
CYP450 2C9 inhibitorNon-inhibitor0.7607
CYP450 2D6 inhibitorNon-inhibitor0.943
CYP450 2C19 inhibitorNon-inhibitor0.6841
CYP450 3A4 inhibitorNon-inhibitor0.9545
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8808
Ames testNon AMES toxic0.9132
CarcinogenicityCarcinogens 0.711
BiodegradationNot ready biodegradable0.9741
Rat acute toxicity1.7199 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9686
hERG inhibition (predictor II)Non-inhibitor0.9034
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (8.57 KB)
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-00mk-2900000000-b9380ce034e632d13402
Mass Spectrum (Electron Ionization)MSsplash10-014j-2900000000-e961932e23eafc2cc0a5
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0900000000-634ac5a75ce25aefe3a3
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0900000000-d1c062299d2fe297943d
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0002-0900000000-926f10e647f6a54dff14
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0900000000-d1c062299d2fe297943d
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-1900000000-a7b7af40f3f0196b2a22
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0900000000-d1c062299d2fe297943d
1H NMR Spectrum1D NMRNot Applicable
13C NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-92.2673365
predicted
DarkChem Lite v0.1.0
[M-H]-123.5616
predicted
DeepCCS 1.0 (2019)
[M+H]+125.54355
predicted
DeepCCS 1.0 (2019)
[M+Na]+133.83778
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
S100 protein binding
Specific Function
pH-dependent, voltage-insensitive, background potassium channel protein. Rectification direction results from potassium ion concentration on either side of the membrane. Acts as an outward rectifie...
Gene Name
KCNK3
Uniprot ID
O14649
Uniprot Name
Potassium channel subfamily K member 3
Molecular Weight
43517.665 Da
References
  1. Lazarenko RM, Willcox SC, Shu S, Berg AP, Jevtovic-Todorovic V, Talley EM, Chen X, Bayliss DA: Motoneuronal TASK channels contribute to immobilizing effects of inhalational general anesthetics. J Neurosci. 2010 Jun 2;30(22):7691-704. doi: 10.1523/JNEUROSCI.1655-10.2010. [Article]
  2. Pandit JJ, Buckler KJ: Halothane and sevoflurane exert different degrees of inhibition on carotid body glomus cell intracellular Ca2+ response to hypoxia. Adv Exp Med Biol. 2010;669:201-4. doi: 10.1007/978-1-4419-5692-7_40. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Voltage-gated potassium channel activity
Specific Function
pH-dependent, voltage-insensitive, background potassium channel protein.
Gene Name
KCNK9
Uniprot ID
Q9NPC2
Uniprot Name
Potassium channel subfamily K member 9
Molecular Weight
42263.485 Da
References
  1. Lazarenko RM, Willcox SC, Shu S, Berg AP, Jevtovic-Todorovic V, Talley EM, Chen X, Bayliss DA: Motoneuronal TASK channels contribute to immobilizing effects of inhalational general anesthetics. J Neurosci. 2010 Jun 2;30(22):7691-704. doi: 10.1523/JNEUROSCI.1655-10.2010. [Article]
  2. Pandit JJ, Buckler KJ: Halothane and sevoflurane exert different degrees of inhibition on carotid body glomus cell intracellular Ca2+ response to hypoxia. Adv Exp Med Biol. 2010;669:201-4. doi: 10.1007/978-1-4419-5692-7_40. [Article]
Kind
Protein group
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Catalyzes the hydrolysis of ATP coupled with the transport of calcium from the cytoplasm to the extracellular space thereby maintaining intracellular calcium homeostasis. Plays a role in blood pressure regulation through regulation of intracellular calcium concentration and nitric oxide production leading to regulation of vascular smooth muscle cells vasoconstriction. Positively regulates bone mineralization through absorption of calcium from the intestine. Plays dual roles in osteoclast differentiation and survival by regulating RANKL-induced calcium oscillations in preosteoclasts and mediating calcium extrusion in mature osteoclasts (By similarity). Regulates insulin sensitivity through calcium/calmodulin signaling pathway by regulating AKT1 activation and NOS3 activation in endothelial cells (PubMed:29104511).
Specific Function
Atp binding

Components:
References
  1. Lopez MM, Kosk-Kosicka D: How do volatile anesthetics inhibit Ca(2+)-ATPases? J Biol Chem. 1995 Nov 24;270(47):28239-45. [Article]
  2. Brennan LK, Froemming GR, Ohlendieck K: Effect of halothane on the oligomerization of the sarcoplasmic reticulum Ca(2+)-ATPase. Biochem Biophys Res Commun. 2000 May 19;271(3):770-6. doi: 10.1006/bbrc.2000.2688. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Voltage-gated potassium channel activity
Specific Function
Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activati...
Gene Name
KCNMA1
Uniprot ID
Q12791
Uniprot Name
Calcium-activated potassium channel subunit alpha-1
Molecular Weight
137558.115 Da
References
  1. 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]
  2. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein phosphatase 2a binding
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May ...
Gene Name
GRIN3A
Uniprot ID
Q8TCU5
Uniprot Name
Glutamate receptor ionotropic, NMDA 3A
Molecular Weight
125464.07 Da
References
  1. Perouansky M, Kirson ED, Yaari Y: Halothane blocks synaptic excitation of inhibitory interneurons. Anesthesiology. 1996 Dec;85(6):1431-8; discussion 29A. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Nmda glutamate receptor activity
Specific Function
NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine.
Gene Name
GRIN3B
Uniprot ID
O60391
Uniprot Name
Glutamate receptor ionotropic, NMDA 3B
Molecular Weight
112990.98 Da
References
  1. Perouansky M, Kirson ED, Yaari Y: Halothane blocks synaptic excitation of inhibitory interneurons. Anesthesiology. 1996 Dec;85(6):1431-8; discussion 29A. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
NMDA receptor subtype of glutamate-gated ion channels possesses high calcium permeability and voltage-dependent sensitivity to magnesium. Activation requires binding of agonist to both types of sub...
Gene Name
GRIN2A
Uniprot ID
Q12879
Uniprot Name
Glutamate receptor ionotropic, NMDA 2A
Molecular Weight
165281.215 Da
References
  1. Perouansky M, Kirson ED, Yaari Y: Halothane blocks synaptic excitation of inhibitory interneurons. Anesthesiology. 1996 Dec;85(6):1431-8; discussion 29A. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Allosteric modulator
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. Schofield CM, Trudell JR, Harrison NL: Alanine-scanning mutagenesis in the signature disulfide loop of the glycine receptor alpha 1 subunit: critical residues for activation and modulation. Biochemistry. 2004 Aug 10;43(31):10058-63. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other
General Function
Photoreceptor activity
Specific Function
Photoreceptor required for image-forming vision at low light intensity. Required for photoreceptor cell viability after birth. Light-induced isomerization of 11-cis to all-trans retinal triggers a ...
Gene Name
RHO
Uniprot ID
P08100
Uniprot Name
Rhodopsin
Molecular Weight
38892.335 Da
References
  1. Ishizawa Y, Sharp R, Liebman PA, Eckenhoff RG: Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling. Biochemistry. 2000 Jul 25;39(29):8497-502. [Article]
  2. Keller C, Grimm C, Wenzel A, Hafezi F, Reme C: Protective effect of halothane anesthesia on retinal light damage: inhibition of metabolic rhodopsin regeneration. Invest Ophthalmol Vis Sci. 2001 Feb;42(2):476-80. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Inward rectifier potassium channel activity
Specific Function
This potassium channel may be involved in the regulation of insulin secretion by glucose and/or neurotransmitters acting through G-protein-coupled receptors. Inward rectifier potassium channels are...
Gene Name
KCNJ6
Uniprot ID
P48051
Uniprot Name
G protein-activated inward rectifier potassium channel 2
Molecular Weight
48450.96 Da
References
  1. Milovic S, Steinecker-Frohnwieser B, Schreibmayer W, Weigl LG: The sensitivity of G protein-activated K+ channels toward halothane is essentially determined by the C terminus. J Biol Chem. 2004 Aug 13;279(33):34240-9. Epub 2004 Jun 2. [Article]
  2. Hara K, Yamakura T, Sata T, Harris RA: The effects of anesthetics and ethanol on alpha2 adrenoceptor subtypes expressed with G protein-coupled inwardly rectifying potassium channels in Xenopus oocytes. Anesth Analg. 2005 Nov;101(5):1381-8. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
G-protein activated inward rectifier potassium channel activity
Specific Function
This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their...
Gene Name
KCNJ3
Uniprot ID
P48549
Uniprot Name
G protein-activated inward rectifier potassium channel 1
Molecular Weight
56602.84 Da
References
  1. Weigl LG, Schreibmayer W: G protein-gated inwardly rectifying potassium channels are targets for volatile anesthetics. Mol Pharmacol. 2001 Aug;60(2):282-9. [Article]
  2. Yamakura T, Lewohl JM, Harris RA: Differential effects of general anesthetics on G protein-coupled inwardly rectifying and other potassium channels. Anesthesiology. 2001 Jul;95(1):144-53. [Article]
  3. Milovic S, Steinecker-Frohnwieser B, Schreibmayer W, Weigl LG: The sensitivity of G protein-activated K+ channels toward halothane is essentially determined by the C terminus. J Biol Chem. 2004 Aug 13;279(33):34240-9. Epub 2004 Jun 2. [Article]
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Protein phosphatase binding
Specific Function
Forms a voltage-independent potassium channel that is activated by intracellular calcium (PubMed:26148990). Activation is followed by membrane hyperpolarization which promotes calcium influx. Requi...
Gene Name
KCNN4
Uniprot ID
O15554
Uniprot Name
Intermediate conductance calcium-activated potassium channel protein 4
Molecular Weight
47695.12 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. 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
Other/unknown
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. Nishikawa K, Jenkins A, Paraskevakis I, Harrison NL: Volatile anesthetic actions on the GABAA receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations. Neuropharmacology. 2002 Mar;42(3):337-45. doi: 10.1016/s0028-3908(01)00189-7. [Article]
  2. Nishikawa K, Harrison NL: The actions of sevoflurane and desflurane on the gamma-aminobutyric acid receptor type A: effects of TM2 mutations in the alpha and beta subunits. Anesthesiology. 2003 Sep;99(3):678-84. doi: 10.1097/00000542-200309000-00024. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Signal transducer activity
Specific Function
Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity...
Gene Name
GNG2
Uniprot ID
P59768
Uniprot Name
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
Molecular Weight
7850.03 Da
References
  1. Ishizawa Y, Sharp R, Liebman PA, Eckenhoff RG: Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling. Biochemistry. 2000 Jul 25;39(29):8497-502. [Article]
  2. Zang WJ, Yu XJ, Zang YM: [Effect of halothane on the muscarinic potassium current of the heart]. Sheng Li Xue Bao. 2000 Apr;52(2):175-8. [Article]
  3. Yoshimura H, Jones KA, Perkins WJ, Warner DO: Dual effects of hexanol and halothane on the regulation of calcium sensitivity in airway smooth muscle. Anesthesiology. 2003 Apr;98(4):871-80. [Article]
  4. Streiff J, Jones K, Perkins WJ, Warner DO, Jones KA: Effect of halothane on the guanosine 5' triphosphate binding activity of G-protein alphai subunits. Anesthesiology. 2003 Jul;99(1):105-11. [Article]
  5. Milovic S, Steinecker-Frohnwieser B, Schreibmayer W, Weigl LG: The sensitivity of G protein-activated K+ channels toward halothane is essentially determined by the C terminus. J Biol Chem. 2004 Aug 13;279(33):34240-9. Epub 2004 Jun 2. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
General Function
Vasopressin receptor activity
Specific Function
G-protein coupled receptor for neuropeptide S (NPS) (PubMed:16790440). Promotes mobilization of intracellular Ca(2+) stores (PubMed:16790440). Inhibits cell growth in response to NPS binding (PubMe...
Gene Name
NPSR1
Uniprot ID
Q6W5P4
Uniprot Name
Neuropeptide S receptor
Molecular Weight
42686.28 Da
References
  1. Ishizawa Y, Sharp R, Liebman PA, Eckenhoff RG: Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling. Biochemistry. 2000 Jul 25;39(29):8497-502. [Article]
  2. Ishizawa Y, Pidikiti R, Liebman PA, Eckenhoff RG: G protein-coupled receptors as direct targets of inhaled anesthetics. Mol Pharmacol. 2002 May;61(5):945-52. [Article]
  3. Streiff J, Jones K, Perkins WJ, Warner DO, Jones KA: Effect of halothane on the guanosine 5' triphosphate binding activity of G-protein alphai subunits. Anesthesiology. 2003 Jul;99(1):105-11. [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. Restrepo JG, Garcia-Martin E, Martinez C, Agundez JA: Polymorphic drug metabolism in anaesthesia. Curr Drug Metab. 2009 Mar;10(3):236-46. [Article]
  2. Spracklin DK, Hankins DC, Fisher JM, Thummel KE, Kharasch ED: Cytochrome P450 2E1 is the principal catalyst of human oxidative halothane metabolism in vitro. J Pharmacol Exp Ther. 1997 Apr;281(1):400-11. [Article]
  3. Flockhart Table of Drug Interactions [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-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 performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Restrepo JG, Garcia-Martin E, Martinez C, Agundez JA: Polymorphic drug metabolism in anaesthesia. Curr Drug Metab. 2009 Mar;10(3):236-46. [Article]
  2. Spracklin DK, Thummel KE, Kharasch ED: Human reductive halothane metabolism in vitro is catalyzed by cytochrome P450 2A6 and 3A4. Drug Metab Dispos. 1996 Sep;24(9):976-83. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Restrepo JG, Garcia-Martin E, Martinez C, Agundez JA: Polymorphic drug metabolism in anaesthesia. Curr Drug Metab. 2009 Mar;10(3):236-46. [Article]
  2. Raunio H, Rautio A, Gullsten H, Pelkonen O: Polymorphisms of CYP2A6 and its practical consequences. Br J Clin Pharmacol. 2001 Oct;52(4):357-63. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 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]

Carriers

Details
1. 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
  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 at June 13, 2005 13:24 / Updated at March 18, 2024 16:48