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

(4 More Sources)

Publications:

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
Torchin CD et al., 1996, Stereoselective metabolism of a new anticonvulsant drug candidate, losigamone, by human liver microsomes., 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
Kimber-Trojnar Z et al., 2003, Perspectives of losigamone in epilepsy treatment., Pol J 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
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
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
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
Monnier N et al., 2005, Correlations between genotype and pharmacological, histological, functional, and clinical phenotypes in malignant hyperthermia susceptibility., Hum Mutat
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
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
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
Monsieurs KG et al., 1998, Gly341Arg mutation indicating malignant hyperthermia susceptibility: specific cause of chronically elevated serum creatine kinase activity., J Neurol Sci
Fagerlund TH et al., 1997, Discordance between malignant hyperthermia susceptibility and RYR1 mutation C1840T in two Scandinavian MH families exhibiting this mutation., Clin Genet
Manning BM et al., 1998, Novel mutations at a CpG dinucleotide in the ryanodine receptor in malignant hyperthermia., Hum Mutat
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
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
Lynch PJ et al., 1997, Identification of heterozygous and homozygous individuals with the novel RYR1 mutation Cys35Arg in a large kindred., Anesthesiology
Monsieurs KG et al., 1996, Malignant hyperthermia susceptibility in a patient with concomitant motor neuron disease., J Neurol Sci
Fagerlund T et al., 1996, RYR mutation G1021A (Gly341Arg) is not frequent in Danish and Swedish families with malignant hyperthermia susceptibility., Clin Genet
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
Quane KA et al., 1993, Mutations in the ryanodine receptor gene in central core disease and malignant hyperthermia., Nat Genet
Zhang Y et al., 1993, A mutation in the human ryanodine receptor gene associated with central core disease., Nat Genet
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 T et al., 1994, Search for three known mutations in the RYR1 gene in 48 Danish families with malignant hyperthermia., Clin Genet
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
Moroni I et al., 1995, Ryanodine receptor gene point mutation and malignant hyperthermia susceptibility., J Neurol
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)
Fagerlund TH et al., 1995, A search for three known RYR1 gene mutations in 41 Swedish families with predisposition to malignant hyperthermia., Clin Genet
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
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
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
Merritt A et al., 2017, Assessing the pathogenicity of RYR1 variants in malignant hyperthermia., Br J Anaesth
Kraeva N et al., 2017, Malignant hyperthermia susceptibility in patients with exertional rhabdomyolysis: a retrospective cohort study and updated systematic review., Can J Anaesth
Butala B et al., 2017, Muscular body build and male sex are independently associated with malignant hyperthermia susceptibility., Can J Anaesth
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
Voermans NC et al., 2016, RYR1-related rhabdomyolysis: A common but probably underdiagnosed manifestation of skeletal muscle ryanodine receptor dysfunction., Rev Neurol (Paris)
Lopez RJ et al., 2016, An RYR1 mutation associated with malignant hyperthermia is also associated with bleeding abnormalities., Sci Signal
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
Bamaga AK et al., 2016, Neuromuscular conditions associated with malignant hyperthermia in paediatric patients: A 25-year retrospective study., Neuromuscul Disord
Miyoshi H et al., 2015, Several Ryanodine Receptor Type 1 Gene Mutations of p.Arg2508 Are Potential Sources of Malignant Hyperthermia., Anesth Analg
Broman M et al., 2015, Malignant hyperthermia, a Scandinavian update., Acta Anaesthesiol Scand
Snoeck M et al., 2015, RYR1-related myopathies: a wide spectrum of phenotypes throughout life., Eur J Neurol
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
Potts LE et al., 2014, Improving awareness of nonanesthesia-related malignant hyperthermia presentations: a tale of two brothers., A A Case Rep
Forrest KM et al., 2015, RYR1-related malignant hyperthermia with marked cerebellar involvement - a paradigm of heat-induced CNS injury?, Neuromuscul Disord
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
Broman M et al., 2015, Next-generation DNA sequencing of a Swedish malignant hyperthermia cohort., Clin Genet
Roesl C et al., 2014, Functional characterisation of the R2452W ryanodine receptor variant associated with malignant hyperthermia susceptibility., Cell Calcium
Schiemann AH et al., 2014, Functional characterization of 2 known ryanodine receptor mutations causing malignant hyperthermia., Anesth Analg
Freiermuth D et al., 2013, Difficult diagnosis of malignant hyperthermia during laparoscopic surgery., Eur J Anaesthesiol
Dlamini N et al., 2013, Mutations in RYR1 are a common cause of exertional myalgia and rhabdomyolysis., Neuromuscul Disord
Kaufmann A et al., 2012, Novel double and single ryanodine receptor 1 variants in two Austrian malignant hyperthermia families., Anesth Analg
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
Broman M et al., 2011, Screening of the ryanodine 1 gene for malignant hyperthermia causative mutations by high resolution melt curve analysis., Anesth Analg
Kraeva N et al., 2011, Ryanodine receptor type 1 gene mutations found in the Canadian malignant hyperthermia population., Can J Anaesth
Chan B et al., 2011, RYR1-related central core myopathy in a Chinese adolescent boy., Hong Kong Med J
Tammaro A et al., 2011, Novel missense mutations and unexpected multiple changes of RYR1 gene in 75 malignant hyperthermia families., 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
Migita T et al., 2009, Functional analysis of ryanodine receptor type 1 p.R2508C mutation in exon 47., J Anesth
Carpenter D et al., 2009, Genetic variation in RYR1 and malignant hyperthermia phenotypes., Br J Anaesth
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
Zullo A et al., 2009, Functional characterization of ryanodine receptor (RYR1) sequence variants using a metabolic assay in immortalized B-lymphocytes., Hum Mutat
Levano S et al., 2009, Increasing the number of diagnostic mutations in malignant hyperthermia., Hum Mutat
Girard T et al., 2008, A fulminant malignant hyperthermia episode in a patient with ryanodine receptor gene mutation p.Tyr522Ser., Anesth Analg
Carpenter D et al., 2009, Analysis of RYR1 haplotype profile in patients with malignant hyperthermia., Ann Hum Genet
Gillies RL et al., 2008, Identification of genetic mutations in Australian malignant hyperthermia families using sequencing of RYR1 hotspots., Anaesth Intensive Care
Girard T et al., 2008, Molecular genetic testing to diagnose malignant hyperthermia susceptibility., J Clin Anesth
Tanabe T et al., 2008, Malignant hyperthermia susceptibility diagnosed with a family-specific ryanodine receptor gene type 1 mutation., J Anesth
Anderson AA et al., 2008, Identification and biochemical characterization of a novel ryanodine receptor gene mutation associated with malignant hyperthermia., Anesthesiology
Gillard EF et al., 1991, A substitution of cysteine for arginine 614 in the ryanodine receptor is potentially causative of human malignant hyperthermia., Genomics
Heytens L, 2007, Molecular genetic detection of susceptibility to malignant hyperthermia in Belgian families., Acta Anaesthesiol Belg
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
Zhou H et al., 2007, Molecular mechanisms and phenotypic variation in RYR1-related congenital myopathies., Brain
Kossugue PM et al., 2007, Central core disease due to recessive mutations in RYR1 gene: is it more common than described?, Muscle Nerve
Yang T et al., 2006, Pharmacologic and functional characterization of malignant hyperthermia in the R163C RyR1 knock-in mouse., Anesthesiology
Broman M et al., 2007, Malignant hyperthermia and central core disease causative mutations in Swedish patients., Acta Anaesthesiol Scand
Robinson R et al., 2006, Mutations in RYR1 in malignant hyperthermia and central core disease., Hum Mutat
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
Girard T et al., 2006, Perinatal diagnosis of malignant hyperthermia susceptibility., Anesthesiology
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
Wu S et al., 2006, Central core disease is due to RYR1 mutations in more than 90% of patients., Brain
Chelu MG et al., 2006, Heat- and anesthesia-induced malignant hyperthermia in an RyR1 knock-in mouse., FASEB 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
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
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
Wehner M et al., 2004, Functional characterization of malignant hyperthermia-associated RyR1 mutations in exon 44, using the human myotube model., Neuromuscul Disord
Rueffert H et al., 2004, Spontaneous occurrence of the disposition to malignant hyperthermia., Anesthesiology
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
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
Muniz VP et al., 2003, Screening for mutations in the RYR1 gene in families with malignant hyperthermia., J Mol Neurosci
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
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
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
Rüffert H et al., 2002, [Current aspects of the diagnosis of malignant hyperthermia]., Anaesthesist
Sei Y et al., 2002, Patients with malignant hyperthermia demonstrate an altered calcium control mechanism in B lymphocytes., Anesthesiology
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
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
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
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
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
McWilliams S et al., 2002, Novel skeletal muscle ryanodine receptor mutation in a large Brazilian family with malignant hyperthermia., Clin 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
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., 2001, Genotype-phenotype comparison of the Swiss malignant hyperthermia population., Hum Mutat
Sambuughin N et al., 2001, North American malignant hyperthermia population: screening of the ryanodine receptor gene and identification of novel mutations., Anesthesiology
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
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
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
Tobin JR et al., 2001, Malignant hyperthermia and apparent heat stroke., JAMA
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
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
Chamley D et al., 2000, Malignant hyperthermia in infancy and identification of novel RYR1 mutation., Br J Anaesth
Ichihara Y et al., 2000, [Preliminary report: first identification of known mutation in the ryanodine receptor gene in a Japanese malignant hyperthermia pedigree]., Masui
Brinkmeier H et al., 1999, Malignant hyperthermia causing Gly2435Arg mutation of the ryanodine receptor facilitates ryanodine-induced calcium release in myotubes., Br J Anaesth
Gencik M et al., 2000, Novel mutation in the RYR1 gene (R2454C) in a patient with malignant hyperthermia., Hum Mutat
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
Fortunato G et al., 1999, A case of discordance between genotype and phenotype in a malignant hyperthermia family., Eur J Hum Genet

HALOTHANE RYR1

Interaction Score: 14.02

Interaction Types & Directionality:

n/a

Interaction Info:

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

Sources:
PharmGKB
HALOTHANE KCNK13

Interaction Score: 2.06

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: 2.06

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 ATP5F1D

Interaction Score: 1.65

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17139284 17016423

Sources:
TdgClinicalTrial TEND
HALOTHANE KCNK9

Interaction Score: 1.18

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:
ChemblInteractions GuideToPharmacology
HALOTHANE KCNK5

Interaction Score: 1.03

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
HALOTHANE KCNK3

Interaction Score: 1.03

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:
ChemblInteractions GuideToPharmacology
HALOTHANE KCNK10

Interaction Score: 0.69

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:
ChemblInteractions GuideToPharmacology
HALOTHANE CYP2A6

Interaction Score: 0.6

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
11038165 8886611 19702528 19442086 14704462 12386121

Sources:
PharmGKB
HALOTHANE KCNK2

Interaction Score: 0.41

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:
ChemblInteractions GuideToPharmacology
HALOTHANE KCNK18

Interaction Score: 0.41

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 GLRA1

Interaction Score: 0.39

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

PMIDs:
15287733 17016423 17139284

Sources:
ChemblInteractions
HALOTHANE CACNA1S

Interaction Score: 0.32

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16163667 15201141 12411788 11260227

Sources:
PharmGKB
HALOTHANE GLRB

Interaction Score: 0.15

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 GABRA1

Interaction Score: 0.11

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:
17016423 17139284 11897112 12960553

Sources:
ChemblInteractions
HALOTHANE GABRQ

Interaction Score: 0.04

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: 0.03

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: 0.03

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: 0.03

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: 0.03

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 GABRB3

Interaction Score: 0.03

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: 0.03

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 GABRG2

Interaction Score: 0.03

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: 0.03

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: 0.03

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: 0.03

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: 0.03

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: 0.03

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: 0.02

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: 0.02

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 HSD17B10

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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 2 opener
Direct Interaction	yes
Specific Action of the Ligand	None

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

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

Trial Name	-
Novel drug target	Established target

activator (activating)
binder

activator (activating)
binder

positive modulator (activating)
other/unknown

HALOTHANE Drug Record

HALOTHANE chembl:CHEMBL931 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Sources: PharmGKB

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: TdgClinicalTrial TEND

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: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: activator (activating)

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

PMIDs: None found

Sources: GuideToPharmacology

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: ChemblInteractions GuideToPharmacology

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: ChemblInteractions GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 11038165 8886611 19702528 19442086 14704462 12386121

Sources: PharmGKB

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: ChemblInteractions GuideToPharmacology

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: allosteric modulator

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

PMIDs: 15287733 17016423 17139284

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16163667 15201141 12411788 11260227

Sources: PharmGKB

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: positive modulator (activating) other/unknown

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

PMIDs: 17016423 17139284 11897112 12960553

Sources: ChemblInteractions

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

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

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

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

Interaction Types & Directionality:

n/a

Sources:
PharmGKB

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:
TdgClinicalTrial TEND

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:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

activator (activating)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology

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:
ChemblInteractions GuideToPharmacology

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:
ChemblInteractions GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
11038165 8886611 19702528 19442086 14704462 12386121

Sources:
PharmGKB

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:
ChemblInteractions GuideToPharmacology

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:

allosteric modulator

Interaction Info:

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

Direct Interaction yes

PMIDs:
15287733 17016423 17139284

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
16163667 15201141 12411788 11260227

Sources:
PharmGKB

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:

positive modulator (activating)

other/unknown

Interaction Info:

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

Direct Interaction yes

PMIDs:
17016423 17139284 11897112 12960553

Sources:
ChemblInteractions

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

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

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

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

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

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