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HALOTHANE Drug Record

  • Summary
  • Interactions
  • Claims
  • 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:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2021-04-13