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Identification
NameGallamine Triethiodide
Accession NumberDB00483  (APRD00712)
TypeSmall Molecule
GroupsApproved
DescriptionA synthetic nondepolarizing blocking drug. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. It should be used cautiously in patients at risk from increased heart rate but may be preferred for patients with bradycardia. (From AMA Drug Evaluations Annual, 1992, p198)
Structure
Thumb
Synonyms
Flaxedil
Gallamin triethiodid
Gallamini Triethiodidum
Triéthiodure de Gallamine
Trietioduro de galamina
External Identifiers
  • F 2559
  • HL 8583
  • RP 3697
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Flaxedil Inj 20mg/mlLiquid20 mgIntravenousAventis Pharma Inc1951-12-312003-07-22Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
FlaxedilSanofi-Aventis
MyraxanYoo Young
SincurarinaCarlo Erba
TricuranNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIQ3254X40X2
CAS number65-29-2
WeightAverage: 891.5291
Monoisotopic: 891.176873061
Chemical FormulaC30H60I3N3O3
InChI KeyREEUVFCVXKWOFE-UHFFFAOYSA-K
InChI
InChI=1S/C30H60N3O3.3HI/c1-10-31(11-2,12-3)22-25-34-28-20-19-21-29(35-26-23-32(13-4,14-5)15-6)30(28)36-27-24-33(16-7,17-8)18-9;;;/h19-21H,10-18,22-27H2,1-9H3;3*1H/q+3;;;/p-3
IUPAC Name
(2-{2,3-bis[2-(triethylazaniumyl)ethoxy]phenoxy}ethyl)triethylazanium triiodide
SMILES
[I-].[I-].[I-].CC[N+](CC)(CC)CCOC1=CC=CC(OCC[N+](CC)(CC)CC)=C1OCC[N+](CC)(CC)CC
Pharmacology
IndicationFor use as adjuncts to anesthesia to induce skeletal muscle relaxation and to facilitate the management of patients undergoing mechanical ventilation
Structured Indications Not Available
PharmacodynamicsGallamine Triethiodide is a nondepolarizing neuromuscular blocking drug (NDMRD) used as an adjunct to anesthesia to induce skeletal muscle relaxation. The actions of gallamine triethiodide are similar to those of tubocurarine, but this agent blocks the cardiac vagus and may cause sinus tachycardia and, occasionally, hypertension and increased cardiac output. Muscle groups differ in their sensitivity to these types of relaxants with ocular muscles (controlling eyelids) being most sensitive, followed by the muscles of the neck, jaw, limbs and then abdomen. The diaphragm is the least sensitive muscle to NDMRDs. Although the nondepolarizing neuromuscular blocking drugs do not have the same adverse effects as succinylcholine, their onset of action is slower. They also have a longer duration of action, making them more suitable for maintaining neuromuscular relaxation during major surgical procedures.
Mechanism of actionIt competes with acetylcholine (ACh) molecules and binds to muscarinic acetylcholine receptors on the post-synaptic membrane of the motor endplate. It acts by combining with the cholinergic receptor sites in muscle and competitively blocking the transmitter action of acetylcholine. It blocks the action of ACh and prevents activation of the muscle contraction process. It can also act on nicotinic presynaptic acetylcholine receptors which inhibits the release of ACh.
TargetKindPharmacological actionActionsOrganismUniProt ID
Muscarinic acetylcholine receptor M2Proteinyes
antagonist
HumanP08172 details
AcetylcholinesteraseProteinyes
inhibitor
HumanP22303 details
Neuronal acetylcholine receptor subunit alpha-2Proteinunknown
antagonist
HumanQ15822 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
1,10-PhenanthrolineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with 1,10-Phenanthroline.Experimental
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Gallamine Triethiodide.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Gallamine Triethiodide.Experimental, Illicit
4-AndrostenedioneThe risk or severity of adverse effects can be increased when 4-Androstenedione is combined with Gallamine Triethiodide.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Gallamine Triethiodide.Experimental, Illicit
AcebutololGallamine Triethiodide may increase the bradycardic activities of Acebutolol.Approved
AcetylcholineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Acetylcholine.Approved
AcetyldigitoxinGallamine Triethiodide may increase the arrhythmogenic activities of Acetyldigitoxin.Approved
AclarubicinAclarubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
AclidiniumAclidinium may increase the anticholinergic activities of Gallamine Triethiodide.Approved
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Gallamine Triethiodide.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Gallamine Triethiodide.Experimental
AlfentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Alfentanil.Approved, Illicit
AlphacetylmethadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Alphacetylmethadol.Experimental, Illicit
AlprenololGallamine Triethiodide may increase the bradycardic activities of Alprenolol.Approved, Withdrawn
AmbenoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Ambenonium.Approved
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Gallamine Triethiodide.Approved
AmikacinAmikacin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
AmrubicinAmrubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Investigational
AnecortaveThe risk or severity of adverse effects can be increased when Anecortave is combined with Gallamine Triethiodide.Investigational
Anisotropine MethylbromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Anisotropine Methylbromide.Approved
annamycinannamycin may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
AnvirzelGallamine Triethiodide may increase the arrhythmogenic activities of Anvirzel.Investigational
Aop200704Gallamine Triethiodide may increase the bradycardic activities of Aop200704.Investigational
ApramycinApramycin may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental, Vet Approved
ArbekacinArbekacin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
ArecolineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Arecoline.Experimental
ArotinololGallamine Triethiodide may increase the bradycardic activities of Arotinolol.Approved
AtenololGallamine Triethiodide may increase the bradycardic activities of Atenolol.Approved
Atracurium besylateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Atracurium besylate.Approved
AtropineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Atropine.Approved, Vet Approved
BeclomethasoneThe risk or severity of adverse effects can be increased when Beclomethasone is combined with Gallamine Triethiodide.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Gallamine Triethiodide.Approved, Investigational
BefunololGallamine Triethiodide may increase the bradycardic activities of Befunolol.Experimental
BenactyzineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Benactyzine.Withdrawn
BendroflumethiazideThe serum concentration of Bendroflumethiazide can be increased when it is combined with Gallamine Triethiodide.Approved
BenzatropineThe risk or severity of adverse effects can be increased when Benzatropine is combined with Gallamine Triethiodide.Approved
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Gallamine Triethiodide.Approved, Vet Approved
BetaxololGallamine Triethiodide may increase the bradycardic activities of Betaxolol.Approved
BethanecholThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Bethanechol.Approved
BevantololGallamine Triethiodide may increase the bradycardic activities of Bevantolol.Approved
BezitramideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Bezitramide.Experimental, Illicit, Withdrawn
BiperidenThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Biperiden.Approved
BisoprololGallamine Triethiodide may increase the bradycardic activities of Bisoprolol.Approved
BopindololGallamine Triethiodide may increase the bradycardic activities of Bopindolol.Approved
Botulinum Toxin Type ABotulinum Toxin Type A may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Investigational
Botulinum Toxin Type BGallamine Triethiodide may increase the neuromuscular blocking activities of Botulinum Toxin Type B.Approved
BucindololGallamine Triethiodide may increase the bradycardic activities of Bucindolol.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Gallamine Triethiodide.Approved
BufuralolGallamine Triethiodide may increase the bradycardic activities of Bufuralol.Experimental, Investigational
BumetanideBumetanide may decrease the neuromuscular blocking activities of Gallamine Triethiodide.Approved
BupranololGallamine Triethiodide may increase the bradycardic activities of Bupranolol.Approved
BuprenorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Butorphanol.Approved, Illicit, Vet Approved
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
CarbacholThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Carbachol.Approved
CarfentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Carfentanil.Illicit, Vet Approved
CarteololGallamine Triethiodide may increase the bradycardic activities of Carteolol.Approved
CarvedilolGallamine Triethiodide may increase the bradycardic activities of Carvedilol.Approved, Investigational
CeliprololGallamine Triethiodide may increase the bradycardic activities of Celiprolol.Approved, Investigational
CevimelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Cevimeline.Approved
ChlorothiazideThe serum concentration of Chlorothiazide can be increased when it is combined with Gallamine Triethiodide.Approved, Vet Approved
ChlorphenoxamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Chlorphenoxamine.Withdrawn
ChlortetracyclineChlortetracycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
ChlorthalidoneThe serum concentration of Chlorthalidone can be increased when it is combined with Gallamine Triethiodide.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Gallamine Triethiodide.Approved, Investigational
CimetropiumGallamine Triethiodide may increase the anticholinergic activities of Cimetropium.Experimental
ClindamycinClindamycin may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
ClobetasolThe risk or severity of adverse effects can be increased when Clobetasol is combined with Gallamine Triethiodide.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Gallamine Triethiodide.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Gallamine Triethiodide.Approved
CodeineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Codeine.Approved, Illicit
ColistimethateColistimethate may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Gallamine Triethiodide.Approved
CoumaphosThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Coumaphos.Vet Approved
CyclopentolateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Cyclopentolate.Approved
CyclosporineCyclosporine may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Investigational, Vet Approved
DarifenacinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Darifenacin.Approved, Investigational
DaunorubicinDaunorubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
DecamethoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Decamethonium.Approved
dehydroepiandrosterone sulfateThe risk or severity of adverse effects can be increased when dehydroepiandrosterone sulfate is combined with Gallamine Triethiodide.Investigational
DemecariumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Demecarium.Approved
DemeclocyclineDemeclocycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
DeslanosideGallamine Triethiodide may increase the arrhythmogenic activities of Deslanoside.Approved
DesloratadineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Desloratadine.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Gallamine Triethiodide.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Gallamine Triethiodide.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Desoxycorticosterone Pivalate is combined with Gallamine Triethiodide.Experimental, Vet Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Gallamine Triethiodide.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Gallamine Triethiodide.Vet Approved
DexetimideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dexetimide.Withdrawn
DextromoramideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dextromoramide.Experimental, Illicit
DextropropoxypheneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dezocine.Approved
DichlorvosThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Dichlorvos.Vet Approved
DicyclomineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dicyclomine.Approved
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Gallamine Triethiodide.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Gallamine Triethiodide.Approved
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Gallamine Triethiodide.Approved
DigitoxinGallamine Triethiodide may increase the arrhythmogenic activities of Digitoxin.Approved
DigoxinGallamine Triethiodide may increase the arrhythmogenic activities of Digoxin.Approved
DihydrocodeineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydrocodeine.Approved, Illicit
DihydroetorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydroetorphine.Experimental, Illicit
DihydromorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Dihydromorphine.Experimental, Illicit
DihydrostreptomycinDihydrostreptomycin may increase the respiratory depressant activities of Gallamine Triethiodide.Vet Approved
DiphenoxylateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Diphenoxylate.Approved, Illicit
DipyridamoleThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Dipyridamole.Approved
DonepezilThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Donepezil.Approved
DoxorubicinDoxorubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Investigational
DoxycyclineDoxycycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Investigational, Vet Approved
DPDPEThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with DPDPE.Investigational
DronabinolGallamine Triethiodide may increase the tachycardic activities of Dronabinol.Approved, Illicit
EchothiophateThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Echothiophate.Approved
EdrophoniumThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Edrophonium.Approved
EluxadolineGallamine Triethiodide may increase the constipating activities of Eluxadoline.Approved
EPIBATIDINEThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with EPIBATIDINE.Experimental
EpirubicinEpirubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Gallamine Triethiodide.Experimental
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Gallamine Triethiodide.Approved
EsmololGallamine Triethiodide may increase the bradycardic activities of Esmolol.Approved
EstroneThe risk or severity of adverse effects can be increased when Estrone is combined with Gallamine Triethiodide.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Estrone sulfate is combined with Gallamine Triethiodide.Approved
Etacrynic acidEtacrynic acid may decrease the neuromuscular blocking activities of Gallamine Triethiodide.Approved
EthopropazineThe risk or severity of adverse effects can be increased when Ethopropazine is combined with Gallamine Triethiodide.Approved
EthylmorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Ethylmorphine.Approved, Illicit
EtorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Etorphine.Illicit, Vet Approved
FentanylThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FenthionThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Fenthion.Vet Approved
FesoterodineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Fesoterodine.Approved
fluasteroneThe risk or severity of adverse effects can be increased when fluasterone is combined with Gallamine Triethiodide.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Gallamine Triethiodide.Approved
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Gallamine Triethiodide.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Flunisolide is combined with Gallamine Triethiodide.Approved, Investigational
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Gallamine Triethiodide.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Gallamine Triethiodide.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Gallamine Triethiodide.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Gallamine Triethiodide.Approved
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Gallamine Triethiodide.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Gallamine Triethiodide.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Gallamine Triethiodide.Approved
Fluticasone furoateThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Gallamine Triethiodide.Approved
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Fluticasone Propionate is combined with Gallamine Triethiodide.Approved
FormestaneThe risk or severity of adverse effects can be increased when Formestane is combined with Gallamine Triethiodide.Approved, Investigational, Withdrawn
FramycetinFramycetin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
FurosemideFurosemide may decrease the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
GalantamineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Galantamine.Approved
GeneticinGeneticin may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental
GentamicinGentamicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
GENTAMICIN C1AGENTAMICIN C1A may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental
Ginkgo bilobaThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Ginkgo biloba.Approved, Nutraceutical
Glucagon recombinantThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Glucagon recombinant.Approved
GlycopyrroniumGallamine Triethiodide may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GTS-21The risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with GTS-21.Investigational
HE3286The risk or severity of adverse effects can be increased when HE3286 is combined with Gallamine Triethiodide.Investigational
HeroinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Heroin.Approved, Illicit
HexamethoniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hexamethonium.Experimental
HomatropineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Homatropine.Approved
Huperzine AThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Huperzine A.Investigational
HydrochlorothiazideThe serum concentration of Hydrochlorothiazide can be increased when it is combined with Gallamine Triethiodide.Approved, Vet Approved
HydrocodoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hydrocodone.Approved, Illicit
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Gallamine Triethiodide.Approved, Vet Approved
HydroflumethiazideThe serum concentration of Hydroflumethiazide can be increased when it is combined with Gallamine Triethiodide.Approved
HydromorphoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Hydromorphone.Approved, Illicit
Hygromycin BHygromycin B may increase the respiratory depressant activities of Gallamine Triethiodide.Vet Approved
HyoscyamineThe risk or severity of adverse effects can be increased when Hyoscyamine is combined with Gallamine Triethiodide.Approved
IdarubicinIdarubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
IndapamideThe serum concentration of Indapamide can be increased when it is combined with Gallamine Triethiodide.Approved
IndenololGallamine Triethiodide may increase the bradycardic activities of Indenolol.Withdrawn
INNO-206INNO-206 may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
Ipratropium bromideThe risk or severity of adverse effects can be increased when Ipratropium bromide is combined with Gallamine Triethiodide.Approved
IsoflurophateThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Isoflurophate.Approved, Withdrawn
IstaroximeThe risk or severity of adverse effects can be increased when Istaroxime is combined with Gallamine Triethiodide.Investigational
ItoprideThe therapeutic efficacy of Itopride can be decreased when used in combination with Gallamine Triethiodide.Investigational
KanamycinKanamycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
KetobemidoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Ketobemidone.Approved
LabetalolGallamine Triethiodide may increase the bradycardic activities of Labetalol.Approved
LevobunololGallamine Triethiodide may increase the bradycardic activities of Levobunolol.Approved
Levomethadyl AcetateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Levomethadyl Acetate.Approved
LevorphanolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Levorphanol.Approved
LithiumLithium may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
LobelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Lobeline.Investigational
LofentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Lofentanil.Illicit
Magnesium hydroxideMagnesium hydroxide may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
Magnesium oxideMagnesium oxide may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
Magnesium salicylateMagnesium salicylate may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
Magnesium SulfateMagnesium Sulfate may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
MalathionThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Malathion.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when ME-609 is combined with Gallamine Triethiodide.Investigational
MecamylamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Mecamylamine.Approved
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Gallamine Triethiodide.Approved
MefloquineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Mefloquine.Approved
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Gallamine Triethiodide.Vet Approved
MemantineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Memantine.Approved, Investigational
MethacholineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methacholine.Approved
MethadoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methadone.Approved
Methadyl AcetateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methadyl Acetate.Approved, Illicit
Methanesulfonyl FluorideThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Methanesulfonyl Fluoride.Investigational
MethanthelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Methantheline.Approved
MethyclothiazideThe serum concentration of Methyclothiazide can be increased when it is combined with Gallamine Triethiodide.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Gallamine Triethiodide.Approved, Vet Approved
MetipranololGallamine Triethiodide may increase the bradycardic activities of Metipranolol.Approved
MetixeneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Metixene.Approved
MetolazoneThe serum concentration of Metolazone can be increased when it is combined with Gallamine Triethiodide.Approved
MetoprololGallamine Triethiodide may increase the bradycardic activities of Metoprolol.Approved, Investigational
MetrizamideMetrizamide may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
MianserinMianserin may increase the anticholinergic activities of Gallamine Triethiodide.Approved
MinaprineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Minaprine.Approved
MinocyclineMinocycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Investigational
MirabegronThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Mirabegron.Approved
MivacuriumGallamine Triethiodide may decrease the neuromuscular blocking activities of Mivacurium.Approved
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Gallamine Triethiodide.Approved, Vet Approved
MorphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Morphine.Approved, Investigational
N-butylscopolammonium bromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with N-butylscopolammonium bromide.Vet Approved
NabiloneGallamine Triethiodide may increase the tachycardic activities of Nabilone.Approved, Investigational
NadololGallamine Triethiodide may increase the bradycardic activities of Nadolol.Approved
NalbuphineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nalbuphine.Approved
NCX 1022The risk or severity of adverse effects can be increased when NCX 1022 is combined with Gallamine Triethiodide.Investigational
NeamineNeamine may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental
NeomycinNeomycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
NeostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Neostigmine.Approved, Vet Approved
NetilmicinNetilmicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
NicotineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nicotine.Approved
Nicotine bitartrateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Nicotine bitartrate.Approved
NormethadoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Normethadone.Approved, Illicit
NVA237The risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with NVA237.Investigational
Oleoyl estroneThe risk or severity of adverse effects can be increased when Oleoyl estrone is combined with Gallamine Triethiodide.Investigational
OpiumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Opium.Approved, Illicit
OrphenadrineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Orphenadrine.Approved
OuabainGallamine Triethiodide may increase the arrhythmogenic activities of Ouabain.Approved
OxprenololGallamine Triethiodide may increase the bradycardic activities of Oxprenolol.Approved
OxybutyninThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxybutynin.Approved, Investigational
OxycodoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxycodone.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Oxymorphone.Approved, Investigational, Vet Approved
OxyphenoniumThe risk or severity of adverse effects can be increased when Oxyphenonium is combined with Gallamine Triethiodide.Approved
OxytetracyclineOxytetracycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
PancuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pancuronium.Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Gallamine Triethiodide.Approved
ParomomycinParomomycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Investigational
PenbutololGallamine Triethiodide may increase the bradycardic activities of Penbutolol.Approved, Investigational
PentazocineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pentazocine.Approved, Vet Approved
PentoliniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pentolinium.Approved
PethidineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pethidine.Approved
PhysostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Physostigmine.Approved
PilocarpineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pilocarpine.Approved
PindololGallamine Triethiodide may increase the bradycardic activities of Pindolol.Approved
PipecuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pipecuronium.Approved
PirarubicinPirarubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
PirenzepineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Pirenzepine.Approved
PiretanidePiretanide may decrease the neuromuscular blocking activities of Gallamine Triethiodide.Experimental
PiritramideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Piritramide.Investigational
PlicamycinPlicamycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Withdrawn
Polymyxin B SulfatePolymyxin B Sulfate may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
PolythiazideThe serum concentration of Polythiazide can be increased when it is combined with Gallamine Triethiodide.Approved
Potassium ChlorideGallamine Triethiodide may increase the ulcerogenic activities of Potassium Chloride.Approved, Withdrawn
PractololGallamine Triethiodide may increase the bradycardic activities of Practolol.Approved
PramlintidePramlintide may increase the anticholinergic activities of Gallamine Triethiodide.Approved, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Gallamine Triethiodide.Approved, Nutraceutical
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Gallamine Triethiodide.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Gallamine Triethiodide.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Gallamine Triethiodide.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Gallamine Triethiodide.Experimental
ProcainamideProcainamide may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
ProcyclidineThe risk or severity of adverse effects can be increased when Procyclidine is combined with Gallamine Triethiodide.Approved
PropanthelineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Propantheline.Approved
PropiverineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Propiverine.Investigational
PropranololGallamine Triethiodide may increase the bradycardic activities of Propranolol.Approved, Investigational
PuromycinPuromycin may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental
PyridostigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Pyridostigmine.Approved
QuinethazoneThe serum concentration of Quinethazone can be increased when it is combined with Gallamine Triethiodide.Approved
QuinidineQuinidine may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
QuinineQuinine may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
RamosetronGallamine Triethiodide may increase the constipating activities of Ramosetron.Approved
RapacuroniumGallamine Triethiodide may decrease the neuromuscular blocking activities of Rapacuronium.Withdrawn
RemifentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Remifentanil.Approved
RibostamycinRibostamycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Gallamine Triethiodide.Approved
RivastigmineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Rivastigmine.Approved, Investigational
ScopolamineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Scopolamine.Approved
Scopolamine butylbromideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Scopolamine butylbromide.Approved
SecretinThe therapeutic efficacy of Secretin can be decreased when used in combination with Gallamine Triethiodide.Approved, Investigational
SisomicinSisomicin may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
SolifenacinThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Solifenacin.Approved
SotalolGallamine Triethiodide may increase the bradycardic activities of Sotalol.Approved
SP1049CSP1049C may increase the respiratory depressant activities of Gallamine Triethiodide.Investigational
SpectinomycinSpectinomycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
StreptomycinStreptomycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Vet Approved
StreptozocinStreptozocin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
SuccinylcholineThe serum concentration of Succinylcholine can be increased when it is combined with Gallamine Triethiodide.Approved
SufentanilThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Sufentanil.Approved, Investigational
SulpirideThe therapeutic efficacy of Sulpiride can be decreased when used in combination with Gallamine Triethiodide.Approved
TacrineThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Tacrine.Withdrawn
TapentadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tapentadol.Approved
TetracyclineTetracycline may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved, Vet Approved
TimololGallamine Triethiodide may increase the bradycardic activities of Timolol.Approved
TiotropiumGallamine Triethiodide may increase the anticholinergic activities of Tiotropium.Approved
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Gallamine Triethiodide.Approved
TobramycinTobramycin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved, Investigational
TolterodineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tolterodine.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Topiramate.Approved
TorasemideTorasemide may decrease the neuromuscular blocking activities of Gallamine Triethiodide.Approved
TramadolThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tramadol.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Gallamine Triethiodide.Approved, Vet Approved
TrichlorfonThe therapeutic efficacy of Gallamine Triethiodide can be decreased when used in combination with Trichlorfon.Vet Approved
TrichlormethiazideThe serum concentration of Trichlormethiazide can be increased when it is combined with Gallamine Triethiodide.Approved, Vet Approved
TrihexyphenidylThe risk or severity of adverse effects can be increased when Trihexyphenidyl is combined with Gallamine Triethiodide.Approved
TrimethaphanThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Trimethaphan.Approved
TropicamideThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tropicamide.Approved
TrospiumThe risk or severity of adverse effects can be increased when Trospium is combined with Gallamine Triethiodide.Approved
TubocurarineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Tubocurarine.Approved
UmeclidiniumUmeclidinium may increase the anticholinergic activities of Gallamine Triethiodide.Approved
ValrubicinValrubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
VancomycinVancomycin may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
VareniclineThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Varenicline.Approved, Investigational
VecuroniumThe risk or severity of adverse effects can be increased when Gallamine Triethiodide is combined with Vecuronium.Approved
ZorubicinZorubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Experimental
Food InteractionsNot Available
References
Synthesis Reference

Fourneau, E.; U.S.Patent 2,544,076; March 6, 1951; assigned to Societe des Usines Chimiques Rhone-Poulenc, France.

General ReferencesNot Available
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (28.5 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8901
Blood Brain Barrier+0.8616
Caco-2 permeable+0.6256
P-glycoprotein substrateSubstrate0.6912
P-glycoprotein inhibitor INon-inhibitor0.8173
P-glycoprotein inhibitor IINon-inhibitor0.8176
Renal organic cation transporterNon-inhibitor0.6818
CYP450 2C9 substrateNon-substrate0.8147
CYP450 2D6 substrateNon-substrate0.6511
CYP450 3A4 substrateSubstrate0.5708
CYP450 1A2 substrateNon-inhibitor0.8002
CYP450 2C9 inhibitorNon-inhibitor0.8613
CYP450 2D6 inhibitorNon-inhibitor0.8874
CYP450 2C19 inhibitorNon-inhibitor0.8815
CYP450 3A4 inhibitorNon-inhibitor0.9296
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6622
Ames testNon AMES toxic0.6156
CarcinogenicityNon-carcinogens0.5724
BiodegradationNot ready biodegradable0.9841
Rat acute toxicity2.8202 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7691
hERG inhibition (predictor II)Inhibitor0.666
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Davis and geck div american cyanamid co
PackagersNot Available
Dosage forms
FormRouteStrength
LiquidIntravenous20 mg
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point152-153Fourneau, E.; U.S.Patent 2,544,076; March 6, 1951; assigned to Societe des Usines Chimiques Rhone-Poulenc, France.
water solubilitySolubleNot Available
logP3.5Not Available
Predicted Properties
PropertyValueSource
Water Solubility4.65e-06 mg/mLALOGPS
logP-0.38ALOGPS
logP-7.7ChemAxon
logS-8.3ALOGPS
pKa (Strongest Basic)-4.5ChemAxon
Physiological Charge3ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area27.69 Å2ChemAxon
Rotatable Bond Count21ChemAxon
Refractivity189.98 m3·mol-1ChemAxon
Polarizability63.43 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenol ethers
Direct ParentPhenol ethers
Alternative Parents
Substituents
  • Phenol ether
  • Choline
  • Alkyl aryl ether
  • Quaternary ammonium salt
  • Ether
  • Hydrocarbon derivative
  • Organic iodide salt
  • Organic salt
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Organic zwitterion
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
G-protein coupled acetylcholine receptor activity
Specific Function:
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then trigge...
Gene Name:
CHRM2
Uniprot ID:
P08172
Molecular Weight:
51714.605 Da
References
  1. Huang XP, Prilla S, Mohr K, Ellis J: Critical amino acid residues of the common allosteric site on the M2 muscarinic acetylcholine receptor: more similarities than differences between the structurally divergent agents gallamine and bis(ammonio)alkane-type hexamethylene-bis-[dimethyl-(3-phthalimidopropyl)ammonium]dibromide. Mol Pharmacol. 2005 Sep;68(3):769-78. Epub 2005 Jun 3. [PubMed:15937215 ]
  2. De Vries B, Roffel AF, Kooistra JM, Meurs H, Zaagsma J: Effects of fenoterol on beta-adrenoceptor and muscarinic M2 receptor function in bovine tracheal smooth muscle. Eur J Pharmacol. 2001 May 11;419(2-3):253-9. [PubMed:11426849 ]
  3. Cembala TM, Forde SC, Appadu BL, Lambert DG: Allosteric interaction of the neuromuscular blockers vecuronium and pancuronium with recombinant human muscarinic M2 receptors. Eur J Pharmacol. 2007 Aug 13;569(1-2):37-40. Epub 2007 May 22. [PubMed:17588565 ]
  4. Ten Berge RE, Krikke M, Teisman AC, Roffel AF, Zaagsma J: Dysfunctional muscarinic M2 autoreceptors in vagally induced bronchoconstriction of conscious guinea pigs after the early allergic reaction. Eur J Pharmacol. 1996 Dec 27;318(1):131-9. [PubMed:9007524 ]
  5. Spina D, Minshall E, Goldie RG, Page CP: The effect of allosteric antagonists in modulating muscarinic M2-receptor function in guinea-pig isolated trachea. Br J Pharmacol. 1994 Jul;112(3):901-5. [PubMed:7522861 ]
  6. Redka DS, Pisterzi LF, Wells JW: Binding of orthosteric ligands to the allosteric site of the M(2) muscarinic cholinergic receptor. Mol Pharmacol. 2008 Sep;74(3):834-43. doi: 10.1124/mol.108.048074. Epub 2008 Jun 13. [PubMed:18552124 ]
  7. Maier-Peuschel M, Frolich N, Dees C, Hommers LG, Hoffmann C, Nikolaev VO, Lohse MJ: A fluorescence resonance energy transfer-based M2 muscarinic receptor sensor reveals rapid kinetics of allosteric modulation. J Biol Chem. 2010 Mar 19;285(12):8793-800. doi: 10.1074/jbc.M109.098517. Epub 2010 Jan 18. [PubMed:20083608 ]
  8. Ehlert FJ, Griffin MT: Two-state models and the analysis of the allosteric effect of gallamine at the M2 muscarinic receptor. J Pharmacol Exp Ther. 2008 Jun;325(3):1039-60. doi: 10.1124/jpet.108.136960. Epub 2008 Feb 27. [PubMed:18305010 ]
  9. Elsinghorst PW, Cieslik JS, Mohr K, Trankle C, Gutschow M: First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18. [PubMed:17944454 ]
  10. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serine hydrolase activity
Specific Function:
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name:
ACHE
Uniprot ID:
P22303
Molecular Weight:
67795.525 Da
References
  1. Radic Z, Taylor P: The influence of peripheral site ligands on the reaction of symmetric and chiral organophosphates with wildtype and mutant acetylcholinesterases. Chem Biol Interact. 1999 May 14;119-120:111-7. [PubMed:10421444 ]
  2. Radic Z, Taylor P: Peripheral site ligands accelerate inhibition of acetylcholinesterase by neutral organophosphates. J Appl Toxicol. 2001 Dec;21 Suppl 1:S13-4. [PubMed:11920914 ]
  3. Robaire B, Kato G: Effects of edrophonium, eserine, decamethonium, d-tubocurarine, and gallamine on the kinetics of membrane-bound and solubilized eel acetylcholinesterase. Mol Pharmacol. 1975 Nov;11(6):722-34. [PubMed:1207670 ]
  4. Seto Y, Shinohara T: Structure-activity relationship of reversible cholinesterase inhibitors including paraquat. Arch Toxicol. 1988 Aug;62(1):37-40. [PubMed:3190453 ]
  5. Bourgeois JP, Betz H, Changuex JP: [Effects of chronic paralysis of chick embryo by flaxedil on the development of the neuromuscular junction]. C R Acad Sci Hebd Seances Acad Sci D. 1978 Mar 13;286(10):773-6. [PubMed:417864 ]
  6. Elsinghorst PW, Cieslik JS, Mohr K, Trankle C, Gutschow M: First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor. J Med Chem. 2007 Nov 15;50(23):5685-95. Epub 2007 Oct 18. [PubMed:17944454 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Drug binding
Specific Function:
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name:
CHRNA2
Uniprot ID:
Q15822
Molecular Weight:
59764.82 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Aoshima H, Inoue Y, Hori K: Inhibition of ionotropic neurotransmitter receptors by antagonists: strategy to estimate the association and the dissociation rate constant of antagonists with very strong affinity to the receptors. J Biochem. 1992 Oct;112(4):495-502. [PubMed:1337082 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23