DGIdb - HALOTHANE Drug Record

HALOTHANE chembl:CHEMBL931 Approved

Alternate Names:

HALOTHANE
RHIDIALOTHAN
FLUOTHANE
BROMOCHLOROTRIFLUOROETHANE
2,2,2-TRIFLUORO-1-CHLORO-1-BROMOETHANE
1,1,1-TRIFLUORO-2-CHLORO-2-BROMOETHANE
2-BROMO-2-CHLORO-1,1,1-TRIFLUOROETHANE
PHTHOROTHANUM
1-BROMO-1-CHLORO-2,2,2-TRIFLUOROETHANE
1,1,1-TRIFLUORO-2-BROMO-2-CHLOROETHANE
HALON-2311
NARCOTANE
RHODIALOTHAN
drugbank:01159
chemidplus:151-67-7
chembl:CHEMBL931
rxcui:5095
pubchem.compound:3562

Drug Info:

Year of Approval	1958
Drug Class	anesthetics, inhalation
FDA Approval	1958
Drug Class	small molecule
Drug Indications	Anesthetics, Inhalation
Drug Categories	agents that produce hypertension
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 substrates
Drug Categories	nmda receptor antagonists

(5 More Sources)

Publications:

Ishizawa et al., 2000, Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling., Biochemistry
Streiff et al., 2003, Effect of halothane on the guanosine 5' triphosphate binding activity of G-protein alphai subunits., Anesthesiology
Ishizawa et al., 2002, G protein-coupled receptors as direct targets of inhaled anesthetics., Mol. Pharmacol.
Pearce RE et al., 2002, Pathways of carbamazepine bioactivation in vitro I. Characterization of human cytochromes P450 responsible for the formation of 2- and 3-hydroxylated metabolites., Drug Metab Dispos
Di YM et al., 2009, Structure, function, regulation and polymorphism of human cytochrome P450 2A6., Curr Drug Metab
Restrepo JG et al., 2009, Polymorphic drug metabolism in anaesthesia., Curr Drug Metab
Komatsu T et al., 2000, Formation of a dihydroxy metabolite of phenytoin in human liver microsomes/cytosol: roles of cytochromes P450 2C9, 2C19, and 3A4., Drug Metab Dispos
Kimber-Trojnar Z et al., 2003, Perspectives of losigamone in epilepsy treatment., Pol J Pharmacol
Torchin CD et al., 1996, Stereoselective metabolism of a new anticonvulsant drug candidate, losigamone, by human liver microsomes., Drug Metab Dispos
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Hanley et al., 2002, Halothane, isoflurane and sevoflurane inhibit NADH:ubiquinone oxidoreductase (complex I) of cardiac mitochondria., J. Physiol. (Lond.)
Pandit et al., 2010, Halothane and sevoflurane exert different degrees of inhibition on carotid body glomus cell intracellular Ca2+ response to hypoxia., Adv. Exp. Med. Biol.
Lazarenko et al., 2010, Motoneuronal TASK channels contribute to immobilizing effects of inhalational general anesthetics., J. Neurosci.
Schofield et al., 2004, Alanine-scanning mutagenesis in the signature disulfide loop of the glycine receptor alpha 1 subunit: critical residues for activation and modulation., Biochemistry
Namba et al., 2000, Inhibition of the human intermediate conductance Ca(2+)-activated K(+) channel, hIK1, by volatile anesthetics., Eur. J. Pharmacol.
Berman et al., 2000, The Protein Data Bank., Nucleic Acids Res.
Perouansky et al., 1996, Halothane blocks synaptic excitation of inhibitory interneurons., Anesthesiology
Nishikawa K et al., 2002, Volatile anesthetic actions on the GABAA receptors: contrasting effects of alpha 1(S270) and beta 2(N265) point mutations., Neuropharmacology
Nishikawa K et al., 2003, 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
Hara et al., 2005, The effects of anesthetics and ethanol on alpha2 adrenoceptor subtypes expressed with G protein-coupled inwardly rectifying potassium channels in Xenopus oocytes., Anesth. Analg.
Milovic et al., 2004, The sensitivity of G protein-activated K+ channels toward halothane is essentially determined by the C terminus., J. Biol. Chem.
Yamakura et al., 2001, Differential effects of general anesthetics on G protein-coupled inwardly rectifying and other potassium channels., Anesthesiology
Weigl et al., 2001, G protein-gated inwardly rectifying potassium channels are targets for volatile anesthetics., Mol. Pharmacol.
Monnier N et al., 2005, Correlations between genotype and pharmacological, histological, functional, and clinical phenotypes in malignant hyperthermia susceptibility., Hum Mutat
Monnier N et al., 2002, Presence of two different genetic traits in malignant hyperthermia families: implication for genetic analysis, diagnosis, and incidence of malignant hyperthermia susceptibility., Anesthesiology
Weiss RG et al., 2004, Functional analysis of the R1086H malignant hyperthermia mutation in the DHPR reveals an unexpected influence of the III-IV loop on skeletal muscle EC coupling., Am J Physiol Cell Physiol
Stewart SL et al., 2001, Identification of the Arg1086His mutation in the alpha subunit of the voltage-dependent calcium channel (CACNA1S) in a North American family with malignant hyperthermia., Clin Genet
Yoshimura et al., 2003, Dual effects of hexanol and halothane on the regulation of calcium sensitivity in airway smooth muscle., Anesthesiology
Zang et al., 2000, [Effect of halothane on the muscarinic potassium current of the heart]., Sheng Li Xue Bao
Broman M et al., 2015, Malignant hyperthermia, a Scandinavian update., Acta Anaesthesiol Scand
Sei Y et al., 2002, Patients with malignant hyperthermia demonstrate an altered calcium control mechanism in B lymphocytes., Anesthesiology
Bamaga AK et al., 2016, Neuromuscular conditions associated with malignant hyperthermia in paediatric patients: A 25-year retrospective study., Neuromuscul Disord
Fagerlund T et al., 1996, RYR mutation G1021A (Gly341Arg) is not frequent in Danish and Swedish families with malignant hyperthermia susceptibility., Clin Genet
Rueffert H et al., 2009, Mild clinical and histopathological features in patients who carry the frequent and causative malignant hyperthermia RyR1 mutation p.Thr2206Met., Clin Neuropathol
Heytens L, 2007, Molecular genetic detection of susceptibility to malignant hyperthermia in Belgian families., Acta Anaesthesiol Belg
Quane KA et al., 1994, Mutation screening of the RYR1 gene in malignant hyperthermia: detection of a novel Tyr to Ser mutation in a pedigree with associated central cores., Genomics
Tong J et al., 1997, Caffeine and halothane sensitivity of intracellular Ca2+ release is altered by 15 calcium release channel (ryanodine receptor) mutations associated with malignant hyperthermia and/or central core disease., J Biol Chem
Broman M et al., 2011, Screening of the ryanodine 1 gene for malignant hyperthermia causative mutations by high resolution melt curve analysis., Anesth Analg
Monnier N et al., 2000, An autosomal dominant congenital myopathy with cores and rods is associated with a neomutation in the RYR1 gene encoding the skeletal muscle ryanodine receptor., Hum Mol Genet
Chamley D et al., 2000, Malignant hyperthermia in infancy and identification of novel RYR1 mutation., Br J Anaesth
Tammaro A et al., 2011, Novel missense mutations and unexpected multiple changes of RYR1 gene in 75 malignant hyperthermia families., Clin Genet
Potts LE et al., 2014, Improving awareness of nonanesthesia-related malignant hyperthermia presentations: a tale of two brothers., A A Case Rep
Carpenter D et al., 2009, Genetic variation in RYR1 and malignant hyperthermia phenotypes., Br J Anaesth
Broman M et al., 2015, Next-generation DNA sequencing of a Swedish malignant hyperthermia cohort., Clin Genet
Wehner M et al., 2002, Increased sensitivity to 4-chloro-m-cresol and caffeine in primary myotubes from malignant hyperthermia susceptible individuals carrying the ryanodine receptor 1 Thr2206Met (C6617T) mutation., Clin Genet
Girard T et al., 2001, Genotype-phenotype comparison of the Swiss malignant hyperthermia population., Hum Mutat
Freiermuth D et al., 2013, Difficult diagnosis of malignant hyperthermia during laparoscopic surgery., Eur J Anaesthesiol
Muniz VP et al., 2003, Screening for mutations in the RYR1 gene in families with malignant hyperthermia., J Mol Neurosci
Lynch PJ et al., 1997, Identification of heterozygous and homozygous individuals with the novel RYR1 mutation Cys35Arg in a large kindred., Anesthesiology
Wehner M et al., 2003, Calcium release from sarcoplasmic reticulum is facilitated in human myotubes derived from carriers of the ryanodine receptor type 1 mutations Ile2182Phe and Gly2375Ala., Genet Test
Carpenter D et al., 2009, Analysis of RYR1 haplotype profile in patients with malignant hyperthermia., Ann Hum Genet
Snoeck M et al., 2015, RYR1-related myopathies: a wide spectrum of phenotypes throughout life., Eur J Neurol
Fagerlund T et al., 1994, Search for three known mutations in the RYR1 gene in 48 Danish families with malignant hyperthermia., Clin Genet
Sambuughin N et al., 2001, North American malignant hyperthermia population: screening of the ryanodine receptor gene and identification of novel mutations., Anesthesiology
Anderson AA et al., 2008, Identification and biochemical characterization of a novel ryanodine receptor gene mutation associated with malignant hyperthermia., Anesthesiology
Chelu MG et al., 2006, Heat- and anesthesia-induced malignant hyperthermia in an RyR1 knock-in mouse., FASEB J
Serfas KD et al., 1996, Comparison of the segregation of the RYR1 C1840T mutation with segregation of the caffeine/halothane contracture test results for malignant hyperthermia susceptibility in a large Manitoba Mennonite family., Anesthesiology
Tanabe T et al., 2008, Malignant hyperthermia susceptibility diagnosed with a family-specific ryanodine receptor gene type 1 mutation., J Anesth
Kraeva N et al., 2017, Malignant hyperthermia susceptibility in patients with exertional rhabdomyolysis: a retrospective cohort study and updated systematic review., Can J Anaesth
Oyamada H et al., 2002, Novel mutations in C-terminal channel region of the ryanodine receptor in malignant hyperthermia patients., Jpn J Pharmacol
Girard T et al., 2008, Molecular genetic testing to diagnose malignant hyperthermia susceptibility., J Clin Anesth
Fortunato G et al., 1999, A case of discordance between genotype and phenotype in a malignant hyperthermia family., Eur J Hum Genet
Fiege M et al., 2002, Results of contracture tests with halothane, caffeine, and ryanodine depend on different malignant hyperthermia-associated ryanodine receptor gene mutations., Anesthesiology
Sambuughin N et al., 2001, Identification and functional characterization of a novel ryanodine receptor mutation causing malignant hyperthermia in North American and South American families., Neuromuscul Disord
Yang T et al., 2006, Pharmacologic and functional characterization of malignant hyperthermia in the R163C RyR1 knock-in mouse., Anesthesiology
Robinson R et al., 2006, Mutations in RYR1 in malignant hyperthermia and central core disease., Hum Mutat
Zhang Y et al., 1993, A mutation in the human ryanodine receptor gene associated with central core disease., Nat Genet
Brinkmeier H et al., 1999, Malignant hyperthermia causing Gly2435Arg mutation of the ryanodine receptor facilitates ryanodine-induced calcium release in myotubes., Br J Anaesth
Kossugue PM et al., 2007, Central core disease due to recessive mutations in RYR1 gene: is it more common than described?, Muscle Nerve
Quane KA et al., 1997, Detection of a novel mutation at amino acid position 614 in the ryanodine receptor in malignant hyperthermia., Br J Anaesth
Girard T et al., 2006, Perinatal diagnosis of malignant hyperthermia susceptibility., Anesthesiology
Galli L et al., 2006, Frequency and localization of mutations in the 106 exons of the RYR1 gene in 50 individuals with malignant hyperthermia., Hum Mutat
Tobin JR et al., 2001, Malignant hyperthermia and apparent heat stroke., JAMA
Li W et al., 2017, Sudden death due to malignant hyperthermia with a mutation of RYR1: autopsy, morphology and genetic analysis., Forensic Sci Med Pathol
Manning BM et al., 1998, Novel mutations at a CpG dinucleotide in the ryanodine receptor in malignant hyperthermia., Hum Mutat
Fletcher JE et al., 1995, Genotype and phenotype relationships for mutations in the ryanodine receptor in patients referred for diagnosis of malignant hyperthermia., Br J Anaesth
Dlamini N et al., 2013, Mutations in RYR1 are a common cause of exertional myalgia and rhabdomyolysis., Neuromuscul Disord
Monsieurs KG et al., 1998, Gly341Arg mutation indicating malignant hyperthermia susceptibility: specific cause of chronically elevated serum creatine kinase activity., J Neurol Sci
Schiemann AH et al., 2014, Functional characterization of 2 known ryanodine receptor mutations causing malignant hyperthermia., Anesth Analg
Roux-Buisson N et al., 2016, Identification of variants of the ryanodine receptor type 1 in patients with exertional heat stroke and positive response to the malignant hyperthermia in vitro contracture test., Br J Anaesth
Galli L et al., 2002, Mutations in the RYR1 gene in Italian patients at risk for malignant hyperthermia: evidence for a cluster of novel mutations in the C-terminal region., Cell Calcium
Sei Y et al., 2004, Malignant hyperthermia in North America: genetic screening of the three hot spots in the type I ryanodine receptor gene., Anesthesiology
Wu S et al., 2006, Central core disease is due to RYR1 mutations in more than 90% of patients., Brain
Kraeva N et al., 2011, Ryanodine receptor type 1 gene mutations found in the Canadian malignant hyperthermia population., Can J Anaesth
Rueffert H et al., 2001, Determination of a positive malignant hyperthermia (MH) disposition without the in vitro contracture test in families carrying the RYR1 Arg614Cys mutation., Clin Genet
Robinson RL et al., 2002, RYR1 mutations causing central core disease are associated with more severe malignant hyperthermia in vitro contracture test phenotypes., Hum Mutat
Girard T et al., 2008, A fulminant malignant hyperthermia episode in a patient with ryanodine receptor gene mutation p.Tyr522Ser., Anesth Analg
Levano S et al., 2009, Increasing the number of diagnostic mutations in malignant hyperthermia., Hum Mutat
Joseph MR et al., 2017, Intraoperative Presentation of Malignant Hyperthermia (Confirmed by RYR1 Gene Mutation, c.7522C>T; p.R2508C) Leads to Diagnosis of King-Denborough Syndrome in a Child With Hypotonia and Dysmorphic Features: A Case Report., A A Case Rep
Quane KA et al., 1993, Mutations in the ryanodine receptor gene in central core disease and malignant hyperthermia., Nat Genet
Rueffert H et al., 2002, Mutation screening in the ryanodine receptor 1 gene (RYR1) in patients susceptible to malignant hyperthermia who show definite IVCT results: identification of three novel mutations., Acta Anaesthesiol Scand
Gencik M et al., 2000, Novel mutation in the RYR1 gene (R2454C) in a patient with malignant hyperthermia., Hum Mutat
Ibarra M CA et al., 2006, Malignant hyperthermia in Japan: mutation screening of the entire ryanodine receptor type 1 gene coding region by direct sequencing., Anesthesiology
Ichihara Y et al., 2000, [Preliminary report: first identification of known mutation in the ryanodine receptor gene in a Japanese malignant hyperthermia pedigree]., Masui
Lopez RJ et al., 2016, An RYR1 mutation associated with malignant hyperthermia is also associated with bleeding abnormalities., Sci Signal
Rueffert H et al., 2004, Spontaneous occurrence of the disposition to malignant hyperthermia., Anesthesiology
Tammaro A et al., 2003, Scanning for mutations of the ryanodine receptor (RYR1) gene by denaturing HPLC: detection of three novel malignant hyperthermia alleles., Clin Chem
McWilliams S et al., 2002, Novel skeletal muscle ryanodine receptor mutation in a large Brazilian family with malignant hyperthermia., Clin Genet
Miyoshi H et al., 2015, Several Ryanodine Receptor Type 1 Gene Mutations of p.Arg2508 Are Potential Sources of Malignant Hyperthermia., Anesth Analg
Larach MG et al., 2014, Malignant hyperthermia deaths related to inadequate temperature monitoring, 2007-2012: a report from the North American malignant hyperthermia registry of the malignant hyperthermia association of the United States., Anesth Analg
Butala B et al., 2017, Muscular body build and male sex are independently associated with malignant hyperthermia susceptibility., Can J Anaesth
Rueffert H et al., 2001, Homozygous and heterozygous Arg614Cys mutations (1840C-->T) in the ryanodine receptor gene co-segregate with malignant hyperthermia susceptibility in a German family., Br J Anaesth
Rüffert H et al., 2002, [Current aspects of the diagnosis of malignant hyperthermia]., Anaesthesist
Migita T et al., 2009, Functional analysis of ryanodine receptor type 1 p.R2508C mutation in exon 47., J Anesth
Gillies RL et al., 2015, Analysis of the entire ryanodine receptor type 1 and alpha 1 subunit of the dihydropyridine receptor (CACNA1S) coding regions for variants associated with malignant hyperthermia in Australian families., Anaesth Intensive Care
Monsieurs KG et al., 1996, Malignant hyperthermia susceptibility in a patient with concomitant motor neuron disease., J Neurol Sci
Nelson EP et al., 2018, Management of a Patient With a History of Nonanesthesia-Related Malignant Hyperthermia Undergoing Laparoscopic Cholecystectomy: A Case Report., A A Pract
Voermans NC et al., 2016, RYR1-related rhabdomyolysis: A common but probably underdiagnosed manifestation of skeletal muscle ryanodine receptor dysfunction., Rev Neurol (Paris)
Moroni I et al., 1995, Ryanodine receptor gene point mutation and malignant hyperthermia susceptibility., J Neurol
Quane KA et al., 1994, Detection of a novel common mutation in the ryanodine receptor gene in malignant hyperthermia: implications for diagnosis and heterogeneity studies., Hum Mol Genet
Fagerlund TH et al., 1997, Discordance between malignant hyperthermia susceptibility and RYR1 mutation C1840T in two Scandinavian MH families exhibiting this mutation., Clin Genet
Sambuughin N et al., 2005, Screening of the entire ryanodine receptor type 1 coding region for sequence variants associated with malignant hyperthermia susceptibility in the north american population., Anesthesiology
Wehner M et al., 2004, Functional characterization of malignant hyperthermia-associated RyR1 mutations in exon 44, using the human myotube model., Neuromuscul Disord
Hogan K et al., 1992, A cysteine-for-arginine substitution (R614C) in the human skeletal muscle calcium release channel cosegregates with malignant hyperthermia., Anesth Analg
Brown RL et al., 2000, A novel ryanodine receptor mutation and genotype-phenotype correlation in a large malignant hyperthermia New Zealand Maori pedigree., Hum Mol Genet
Taylor A et al., 2012, A study of a family with the skeletal muscle RYR1 mutation (c.7354C>T) associated with central core myopathy and malignant hyperthermia susceptibility., J Clin Neurosci
Forrest KM et al., 2015, RYR1-related malignant hyperthermia with marked cerebellar involvement - a paradigm of heat-induced CNS injury?, Neuromuscul Disord
Zhou H et al., 2007, Molecular mechanisms and phenotypic variation in RYR1-related congenital myopathies., Brain
Merritt A et al., 2017, Assessing the pathogenicity of RYR1 variants in malignant hyperthermia., Br J Anaesth
Steinfath M et al., 2002, Evidence for a spontaneous C1840-T mutation in the RYR1 gene after DNA fingerprinting in a malignant hyperthermia susceptible family., Naunyn Schmiedebergs Arch Pharmacol
Gillard EF et al., 1991, A substitution of cysteine for arginine 614 in the ryanodine receptor is potentially causative of human malignant hyperthermia., Genomics
Broman M et al., 2007, Malignant hyperthermia and central core disease causative mutations in Swedish patients., Acta Anaesthesiol Scand
Gillies RL et al., 2008, Identification of genetic mutations in Australian malignant hyperthermia families using sequencing of RYR1 hotspots., Anaesth Intensive Care
Brandt A et al., 1999, Screening of the ryanodine receptor gene in 105 malignant hyperthermia families: novel mutations and concordance with the in vitro contracture test., Hum Mol Genet
Chan B et al., 2011, RYR1-related central core myopathy in a Chinese adolescent boy., Hong Kong Med J
Yeh HM et al., 2005, Denaturing high performance liquid chromatography screening of ryanodine receptor type 1 gene in patients with malignant hyperthermia in Taiwan and identification of a novel mutation (Y522C)., Anesth Analg
Fagerlund TH et al., 1995, A search for three known RYR1 gene mutations in 41 Swedish families with predisposition to malignant hyperthermia., Clin Genet
Zullo A et al., 2009, Functional characterization of ryanodine receptor (RYR1) sequence variants using a metabolic assay in immortalized B-lymphocytes., Hum Mutat
Roesl C et al., 2014, Functional characterisation of the R2452W ryanodine receptor variant associated with malignant hyperthermia susceptibility., Cell Calcium
Steinfath M et al., 1995, C1840-T mutation in the human skeletal muscle ryanodine receptor gene: frequency in northern German families susceptible to malignant hyperthermia and the relationship to in vitro contracture response., J Mol Med (Berl)
Newmark JL et al., 2007, Delayed onset of malignant hyperthermia without creatine kinase elevation in a geriatric, ryanodine receptor type 1 gene compound heterozygous patient., Anesthesiology
Loke JC et al., 2003, Detection of a novel ryanodine receptor subtype 1 mutation (R328W) in a malignant hyperthermia family by sequencing of a leukocyte transcript., Anesthesiology
Broman M et al., 2009, Mutation screening of the RYR1-cDNA from peripheral B-lymphocytes in 15 Swedish malignant hyperthermia index cases., Br J Anaesth
Gillard EF et al., 1992, Polymorphisms and deduced amino acid substitutions in the coding sequence of the ryanodine receptor (RYR1) gene in individuals with malignant hyperthermia., Genomics
Kaufmann A et al., 2012, Novel double and single ryanodine receptor 1 variants in two Austrian malignant hyperthermia families., Anesth Analg
Keller et al., 2001, Protective effect of halothane anesthesia on retinal light damage: inhibition of metabolic rhodopsin regeneration., Invest. Ophthalmol. Vis. Sci.
Lopez et al., 1995, How do volatile anesthetics inhibit Ca(2+)-ATPases?, J. Biol. Chem.
Brennan LK et al., 2000, Effect of halothane on the oligomerization of the sarcoplasmic reticulum Ca(2+)-ATPase., Biochem Biophys Res Commun

HALOTHANE RYR1

Interaction Score: 8.47

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25989378 12411786 26951757 8828983 19919814 17710899 7829078 9334205 21965348 11063719 10823104 20681998 25611019 19648156 25256590 12220451 11668625 23736090 14500992 9066328 14641996 18945287 25960145 7889656 11575529 18212565 16284304 8602662 18306019 28326467 11928716 18502356 10352931 12151923 11525881 17122579 16917943 8220422 10700782 16163667 17226826 9389851 16732128 16835904 11448278 29101530 9450902 7547049 23628358 9543323 24361844 26994242 12208234 15448513 16621918 21455645 11553045 12124989 19020143 19191329 27918309 8220423 12059893 10612851 16732084 10793526 27382027 15108991 12709367 12123492 26381711 25268394 28063098 11493496 12434264 12411788 19685112 25735680 8902717 29608462 27663056 7751854 8012359 9520251 15731587 15210166 1510267 10888602 22030266 25466363 17483490 28403410 12237752 1774074 17081152 18564801 10484775 21282829 16244001 7586638 19191333 25086907 7633940 17667581 12883402 19346234 1354642 22415532

Sources:
PharmGKB
HALOTHANE GNG2

Interaction Score: 7.93

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
10913255 12657848 11961592 15175324 12826849

Sources:
DrugBank
HALOTHANE ATP2B1

Interaction Score: 3.96

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
7499320 10814537

Sources:
DrugBank
HALOTHANE KCNK13

Interaction Score: 1.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction studied at ~5 mM

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALOTHANE KCNK12

Interaction Score: 1.32

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
HALOTHANE ATP5D

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial
HALOTHANE KCNK9

Interaction Score: 0.83

Interaction Types & Directionality:

activator (activating)

binder

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Details of Interaction studied at 1-5 mM

PMIDs:
20217349 20519544

Sources:
DrugBank GuideToPharmacology ChemblInteractions
HALOTHANE KCNN4

Interaction Score: 0.75

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10794813 17139284 17016423

Sources:
DrugBank
HALOTHANE KCNK3

Interaction Score: 0.73

Interaction Types & Directionality:

activator (activating)

binder

Interaction Info:

Specific Action of the Ligand None

Details of Interaction studied at 1-10 mM

Endogenous Drug? False

PMIDs:
20217349 20519544

Sources:
DrugBank GuideToPharmacology ChemblInteractions
HALOTHANE RHO

Interaction Score: 0.66

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
10913255 11157886

Sources:
DrugBank
HALOTHANE KCNJ3

Interaction Score: 0.66

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
11465552 15175324 11455015

Sources:
DrugBank
HALOTHANE KCNK5

Interaction Score: 0.66

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
HALOTHANE MT-ND1

Interaction Score: 0.53

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17139284 17016423 12411515

Sources:
DrugBank
HALOTHANE KCNJ6

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16243998 15175324

Sources:
DrugBank
HALOTHANE KCNK10

Interaction Score: 0.44

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Details of Interaction studied at 1-5 mM

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
HALOTHANE CYP2A6

Interaction Score: 0.33

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12386121 19702528 19442086 11038165 14704462 8886611

Sources:
PharmGKB
HALOTHANE KCNK18

Interaction Score: 0.26

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Potassium channel subfamily K member 18 opener

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE KCNK2

Interaction Score: 0.24

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Potassium channel subfamily K member 2 opener

Direct Interaction yes

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions
HALOTHANE KCNMA1

Interaction Score: 0.22

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10794813 10592235

Sources:
DrugBank
HALOTHANE GLRA1

Interaction Score: 0.2

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

Direct Interaction yes

PMIDs:
15287733 17139284 17016423

Sources:
DrugBank ChemblInteractions
HALOTHANE CACNA1S

Interaction Score: 0.17

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16163667 12411788 15201141 11260227

Sources:
PharmGKB
HALOTHANE GRIN3B

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8968191

Sources:
DrugBank
HALOTHANE GLRB

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GRIN2A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8968191

Sources:
DrugBank
HALOTHANE GRIN3A

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
8968191

Sources:
DrugBank
HALOTHANE NPSR1

Interaction Score: 0.06

Interaction Types & Directionality:

other/unknown

Interaction Info:

PMIDs:
10913255 12826849 11961111

Sources:
DrugBank
HALOTHANE GABRA1

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

other/unknown

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
11897112 12960553 17139284 17016423

Sources:
DrugBank ChemblInteractions
HALOTHANE GABRQ

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRP

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRE

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRD

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRG1

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRB1

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRB3

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRG2

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRB2

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRG3

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA4

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA6

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA5

Interaction Score: 0.02

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA2

Interaction Score: 0.01

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE GABRA3

Interaction Score: 0.01

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HALOTHANE HSD17B10

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01159

Version: 5.1.7

Alternate Names:

HALOTHANE DrugBank Drug Name

151-67-7 CAS Number

Fluothane Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups vet_approved

Publications:

Ishizawa et al., 2000, Halothane binding to a G protein coupled receptor in retinal membranes by photoaffinity labeling., Biochemistry

Streiff et al., 2003, Effect of halothane on the guanosine 5' triphosphate binding activity of G-protein alphai subunits., Anesthesiology

Ishizawa et al., 2002, G protein-coupled receptors as direct targets of inhaled anesthetics., Mol. Pharmacol.

TEND: HALOTHANE
- Version: 01-August-2011
Alternate Names:

HALOTHANE Primary Drug Name

Drug Info:

Drug Class anesthetics, inhalation

Year of Approval 1958

Publications:
TdgClinicalTrial: HALOTHANE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications Anesthetics, Inhalation

Drug Class small molecule

FDA Approval 1958

Publications:

PharmGKB: halothane

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Monnier N et al., 2005, Correlations between genotype and pharmacological, histological, functional, and clinical phenotypes in malignant hyperthermia susceptibility., Hum Mutat

Monnier N et al., 2002, Presence of two different genetic traits in malignant hyperthermia families: implication for genetic analysis, diagnosis, and incidence of malignant hyperthermia susceptibility., Anesthesiology

Weiss RG et al., 2004, Functional analysis of the R1086H malignant hyperthermia mutation in the DHPR reveals an unexpected influence of the III-IV loop on skeletal muscle EC coupling., Am J Physiol Cell Physiol

TTD: Halothane
- Version: 2020.06.01
Alternate Names:

D0D8VE TTD Drug ID

Drug Info:

Publications:
DTC: HALOTHANE
- Version: 02-September-2020
Alternate Names:

CHEMBL931 ChEMBL Drug ID

Drug Info:

Publications:
GuideToPharmacology: 135650346
- Version: 29-September-2020
Alternate Names:

HALOTHANE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL931
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL931
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	None
Details of Interaction	studied at ~5 mM
Endogenous Drug?	False

Direct Interaction?	True
Endogenous Drug?	False
Details of Interaction	studied at 1-5 mM

Mechanism of Interaction	Potassium channel subfamily K member 18 opener
Direct Interaction	yes

Mechanism of Interaction	Potassium channel subfamily K member 2 opener
Direct Interaction	yes
Specific Action of the Ligand	None

Mechanism of Interaction	Glycine receptor (alpha-1/beta) positive modulator
Direct Interaction	yes

Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator
Direct Interaction	yes

HALOTHANE	DrugBank Drug Name
151-67-7	CAS Number
Fluothane	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	vet_approved

Trial Name	-
Novel drug target	Established target

activator (activating)
binder

activator (activating)
binder

HALOTHANE Drug Record

HALOTHANE chembl:CHEMBL931 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Sources: PharmGKB

Interaction Types & Directionality: other/unknown

Interaction Info:

PMIDs: 10913255 12657848 11961592 15175324 12826849

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 7499320 10814537

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand None Details of Interaction studied at ~5 mM Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand None Endogenous Drug? False Direct Interaction? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17139284 17016423

Sources: TEND TdgClinicalTrial

Interaction Types & Directionality: activator (activating) binder

Interaction Info: Direct Interaction? True Endogenous Drug? False Details of Interaction studied at 1-5 mM

PMIDs: 20217349 20519544

Sources: DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10794813 17139284 17016423

Sources: DrugBank

Interaction Types & Directionality: activator (activating) binder

Interaction Info: Specific Action of the Ligand None Details of Interaction studied at 1-10 mM Endogenous Drug? False

PMIDs: 20217349 20519544

Sources: DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: other/unknown

Interaction Info:

PMIDs: 10913255 11157886

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 11465552 15175324 11455015

Sources: DrugBank

Interaction Types & Directionality: activator (activating)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17139284 17016423 12411515

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 16243998 15175324

Sources: DrugBank

Interaction Types & Directionality: activator (activating)

Interaction Info: Direct Interaction? True Endogenous Drug? False Details of Interaction studied at 1-5 mM

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12386121 19702528 19442086 11038165 14704462 8886611

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Mechanism of Interaction Potassium channel subfamily K member 18 opener Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: activator (activating)

Interaction Info: Mechanism of Interaction Potassium channel subfamily K member 2 opener Direct Interaction yes Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10794813 10592235

Sources: DrugBank

Interaction Types & Directionality:

n/a

Sources:
PharmGKB

Interaction Types & Directionality:

other/unknown

PMIDs:
10913255 12657848 11961592 15175324 12826849

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
7499320 10814537

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Details of Interaction studied at ~5 mM

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TEND TdgClinicalTrial

Interaction Types & Directionality:

activator (activating)

binder

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Details of Interaction studied at 1-5 mM

PMIDs:
20217349 20519544

Sources:
DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10794813 17139284 17016423

Sources:
DrugBank

Interaction Types & Directionality:

activator (activating)

binder

Interaction Info:

Specific Action of the Ligand None

Details of Interaction studied at 1-10 mM

Endogenous Drug? False

PMIDs:
20217349 20519544

Sources:
DrugBank GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

other/unknown

PMIDs:
10913255 11157886

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
11465552 15175324 11455015

Sources:
DrugBank

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17139284 17016423 12411515

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
16243998 15175324

Sources:
DrugBank

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Details of Interaction studied at 1-5 mM

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
12386121 19702528 19442086 11038165 14704462 8886611

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Potassium channel subfamily K member 18 opener

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Mechanism of Interaction Potassium channel subfamily K member 2 opener

Direct Interaction yes

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10794813 10592235

Sources:
DrugBank

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

Direct Interaction yes

PMIDs:
15287733 17139284 17016423

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16163667 12411788 15201141 11260227

Sources:
PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
8968191

Sources:
DrugBank

Interaction Types & Directionality:

n/a

Interaction Info:

Mechanism of Interaction Glycine receptor (alpha-1/beta) positive modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)