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Identification
NameAzimilide
Accession NumberDB04957
TypeSmall Molecule
GroupsInvestigational
DescriptionAzimilide is an investigational class III anti-arrhythmic drug that blocks fast and slow components of the delayed rectifier cardiac potassium channels. It is not approved for use in any country, but is currently in clinical trials in the United States.
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
StedicorNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII74QU6P2934
CAS number149908-53-2
WeightAverage: 457.96
Monoisotopic: 457.1880675
Chemical FormulaC23H28ClN5O3
InChI KeyMREBEPTUUMTTIA-UHFFFAOYSA-N
InChI
InChI=1S/C23H28ClN5O3/c1-26-12-14-27(15-13-26)10-2-3-11-28-22(30)17-29(23(28)31)25-16-20-8-9-21(32-20)18-4-6-19(24)7-5-18/h4-9,16H,2-3,10-15,17H2,1H3
IUPAC Name
1-({[5-(4-chlorophenyl)furan-2-yl]methylidene}amino)-3-[4-(4-methylpiperazin-1-yl)butyl]imidazolidine-2,4-dione
SMILES
CN1CCN(CCCCN2C(=O)CN(N=CC3=CC=C(O3)C3=CC=C(Cl)C=C3)C2=O)CC1
Pharmacology
IndicationInvestigated for use/treatment in arrhythmia and atrial fibrillation.
Structured Indications Not Available
PharmacodynamicsAzimilide is a new class III anti-arrhythmic agent. It is distinguished by a relative lack of reverse use-dependence, excellent oral absorption, no need for dose titration, an option for out-patient initiation, no need for adjustment associated with renal or liver failure and a lack of interaction with warfarin or digoxin. It carries some risk of torsade de pointes and rarely, neutropoenia.
Mechanism of actionThe mechanism of action of azimilide is to block both the slowly conducting (I(Ks)) and rapidly conducting (I(Kr)) rectifier potassium currents in cardiac cells. This differs from other class III agents that block I(Kr) exclusively or in combination with sodium, calcium, or transient outward (I(to)) potassium current channels. It also has blocking effects on sodium (I(Na)) and calcium currents (I(CaL)). Its effects on reentrant circuits in infarct border zones causing ventricular tachyarrhythmias are unknown.
TargetKindPharmacological actionActionsOrganismUniProt ID
Potassium voltage-gated channel subfamily E member 1ProteinunknownNot AvailableHumanP15382 details
Potassium voltage-gated channel subfamily KQT member 1ProteinunknownNot AvailableHumanP51787 details
Potassium voltage-gated channel subfamily H member 2ProteinunknownNot AvailableHumanQ12809 details
Related Articles
AbsorptionExcellent oral absorption.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

The metabolic fate of azimilide in man is unusual as it undergoes a cleavage in vivo resulting in the formation of two classes of structurally distinct metabolites. One study has shown that a cleaved metabolite, 4-chloro-2-phenyl furoic acid was present at high concentration in plasma, while other plasma metabolites, azimilide N-oxide, and a cleaved hydantoin metabolite were present at lower concentrations than azimilide. In urine, the cleaved metabolites were the major metabolites, (> 35% of the dose) along with phenols (as conjugates, 7%-8%), azimilide N-oxide (4%-10%), a butanoic acid metabolite (2%-3%), and desmethyl azimilide (2%). A limited investigation of fecal metabolites indicated that azimilide (3%-5%), desmethyl azimilide (1%-3%), and the butanoic acid metabolite (< 1%) were present. Contributing pathways for metabolism of azimilide, identified through in vitro and in-vivo studies, were CYPs 1A1 (est. 28%), 3A4/5 (est. 20%), 2D6 (< 1%), FMO (est. 14%), and cleavage (35%). Enzyme(s) involved in the cleavage of azimilide were not identified.

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
2-HYDROXY-1,4-NAPHTHOQUINONEThe risk or severity of adverse effects can be increased when 2-HYDROXY-1,4-NAPHTHOQUINONE is combined with Azimilide.Experimental
2-mercaptobenzothiazoleThe risk or severity of adverse effects can be increased when 2-mercaptobenzothiazole is combined with Azimilide.Vet Approved
AlfuzosinAlfuzosin may increase the hypotensive activities of Azimilide.Approved, Investigational
AmobarbitalThe metabolism of Azimilide can be increased when combined with Amobarbital.Approved, Illicit
AmorolfineThe risk or severity of adverse effects can be increased when Amorolfine is combined with Azimilide.Approved
Amphotericin BThe risk or severity of adverse effects can be increased when Amphotericin B is combined with Azimilide.Approved, Investigational
AN2690The risk or severity of adverse effects can be increased when AN2690 is combined with Azimilide.Investigational
AnidulafunginThe risk or severity of adverse effects can be increased when Anidulafungin is combined with Azimilide.Approved, Investigational
ArtemetherThe risk or severity of adverse effects can be increased when Artemether is combined with Azimilide.Approved
AtosibanThe risk or severity of adverse effects can be increased when Azimilide is combined with Atosiban.Approved
Atracurium besylateAzimilide may increase the neuromuscular blocking activities of Atracurium besylate.Approved
Bafilomycin A1The risk or severity of adverse effects can be increased when Bafilomycin A1 is combined with Azimilide.Experimental
BarbexacloneThe metabolism of Azimilide can be increased when combined with Barbexaclone.Experimental
BarbitalThe metabolism of Azimilide can be increased when combined with Barbital.Illicit
Benzoic AcidThe risk or severity of adverse effects can be increased when Benzoic Acid is combined with Azimilide.Approved
BifonazoleThe risk or severity of adverse effects can be increased when Bifonazole is combined with Azimilide.Approved
BucindololBucindolol may increase the hypotensive activities of Azimilide.Investigational
ButenafineThe risk or severity of adverse effects can be increased when Butenafine is combined with Azimilide.Approved
ButoconazoleThe risk or severity of adverse effects can be increased when Butoconazole is combined with Azimilide.Approved
CalciumThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium.Nutraceutical
Calcium AcetateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium Acetate.Approved
Calcium carbonateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium carbonate.Approved
Calcium ChlorideThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium Chloride.Approved
Calcium citrateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium citrate.Approved
Calcium glubionateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium glubionate.Approved
Calcium GluceptateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium Gluceptate.Approved
Calcium gluconateThe therapeutic efficacy of Azimilide can be decreased when used in combination with Calcium gluconate.Approved, Vet Approved
CandicidinThe risk or severity of adverse effects can be increased when Candicidin is combined with Azimilide.Withdrawn
CarbomycinThe metabolism of Azimilide can be decreased when combined with Carbomycin.Vet Approved
CarvedilolCarvedilol may increase the hypotensive activities of Azimilide.Approved, Investigational
CaspofunginThe risk or severity of adverse effects can be increased when Caspofungin is combined with Azimilide.Approved
CeruleninThe risk or severity of adverse effects can be increased when Cerulenin is combined with Azimilide.Approved
ChloroxineThe risk or severity of adverse effects can be increased when Chloroxine is combined with Azimilide.Approved
CiclopiroxThe risk or severity of adverse effects can be increased when Ciclopirox is combined with Azimilide.Approved, Investigational
CimetidineThe serum concentration of Azimilide can be increased when it is combined with Cimetidine.Approved
ClarithromycinThe metabolism of Azimilide can be decreased when combined with Clarithromycin.Approved
ClopidogrelThe therapeutic efficacy of Clopidogrel can be decreased when used in combination with Azimilide.Approved, Nutraceutical
ClotrimazoleThe risk or severity of adverse effects can be increased when Clotrimazole is combined with Azimilide.Approved, Vet Approved
CordycepinThe risk or severity of adverse effects can be increased when Cordycepin is combined with Azimilide.Investigational
CyclosporineThe risk or severity of adverse effects can be increased when Cyclosporine is combined with Azimilide.Approved, Investigational, Vet Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Azimilide.Investigational
Decanoic AcidThe risk or severity of adverse effects can be increased when Decanoic Acid is combined with Azimilide.Experimental
DoxazosinDoxazosin may increase the hypotensive activities of Azimilide.Approved
EconazoleThe risk or severity of adverse effects can be increased when Econazole is combined with Azimilide.Approved
EfavirenzThe serum concentration of Azimilide can be decreased when it is combined with Efavirenz.Approved, Investigational
EfinaconazoleThe risk or severity of adverse effects can be increased when Efinaconazole is combined with Azimilide.Approved
ErythromycinThe metabolism of Azimilide can be decreased when combined with Erythromycin.Approved, Vet Approved
FluconazoleThe serum concentration of Azimilide can be increased when it is combined with Fluconazole.Approved
FlucytosineThe risk or severity of adverse effects can be increased when Flucytosine is combined with Azimilide.Approved
FosphenytoinThe serum concentration of Fosphenytoin can be increased when it is combined with Azimilide.Approved
GlyphosateThe risk or severity of adverse effects can be increased when Glyphosate is combined with Azimilide.Experimental
GriseofulvinThe risk or severity of adverse effects can be increased when Griseofulvin is combined with Azimilide.Approved, Vet Approved
HaloproginThe risk or severity of adverse effects can be increased when Haloprogin is combined with Azimilide.Approved, Withdrawn
HexetidineThe risk or severity of adverse effects can be increased when Hexetidine is combined with Azimilide.Approved
HexobarbitalThe metabolism of Azimilide can be increased when combined with Hexobarbital.Approved
IndoraminIndoramin may increase the hypotensive activities of Azimilide.Withdrawn
IsoconazoleThe risk or severity of adverse effects can be increased when Isoconazole is combined with Azimilide.Approved
ItraconazoleThe risk or severity of adverse effects can be increased when Itraconazole is combined with Azimilide.Approved, Investigational
JosamycinThe metabolism of Azimilide can be decreased when combined with Josamycin.Approved
KetoconazoleThe risk or severity of adverse effects can be increased when Ketoconazole is combined with Azimilide.Approved, Investigational
KitasamycinThe metabolism of Azimilide can be decreased when combined with Kitasamycin.Experimental
LabetalolLabetalol may increase the hypotensive activities of Azimilide.Approved
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Azimilide is combined with Magnesium hydroxide.Approved
Magnesium oxideThe risk or severity of adverse effects can be increased when Azimilide is combined with Magnesium oxide.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Azimilide is combined with Magnesium salicylate.Approved
Magnesium SulfateThe risk or severity of adverse effects can be increased when Azimilide is combined with Magnesium Sulfate.Approved, Vet Approved
MethohexitalThe metabolism of Azimilide can be increased when combined with Methohexital.Approved
MethylphenobarbitalThe metabolism of Azimilide can be increased when combined with Methylphenobarbital.Approved
MevastatinThe risk or severity of adverse effects can be increased when Mevastatin is combined with Azimilide.Experimental
MicafunginThe risk or severity of adverse effects can be increased when Micafungin is combined with Azimilide.Approved, Investigational
MiconazoleThe risk or severity of adverse effects can be increased when Miconazole is combined with Azimilide.Approved, Investigational, Vet Approved
MiltefosineThe risk or severity of adverse effects can be increased when Miltefosine is combined with Azimilide.Approved
MivacuriumAzimilide may increase the neuromuscular blocking activities of Mivacurium.Approved
MonensinThe risk or severity of adverse effects can be increased when Monensin is combined with Azimilide.Vet Approved
MyxothiazolThe risk or severity of adverse effects can be increased when Myxothiazol is combined with Azimilide.Experimental
NafcillinThe metabolism of Azimilide can be increased when combined with Nafcillin.Approved
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Azimilide.Approved
NatamycinThe risk or severity of adverse effects can be increased when Natamycin is combined with Azimilide.Approved
NitroprussideAzimilide may increase the hypotensive activities of Nitroprusside.Approved
NitroxolineThe risk or severity of adverse effects can be increased when Nitroxoline is combined with Azimilide.Approved
NystatinThe risk or severity of adverse effects can be increased when Nystatin is combined with Azimilide.Approved, Vet Approved
OleandomycinThe metabolism of Azimilide can be decreased when combined with Oleandomycin.Vet Approved
OxiconazoleThe risk or severity of adverse effects can be increased when Oxiconazole is combined with Azimilide.Approved
pafuramidineThe risk or severity of adverse effects can be increased when pafuramidine is combined with Azimilide.Investigational
PentamidineThe risk or severity of adverse effects can be increased when Pentamidine is combined with Azimilide.Approved
PentobarbitalThe metabolism of Azimilide can be increased when combined with Pentobarbital.Approved, Vet Approved
PhenobarbitalThe metabolism of Azimilide can be increased when combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Azimilide.Approved, Vet Approved
PosaconazoleThe risk or severity of adverse effects can be increased when Posaconazole is combined with Azimilide.Approved, Investigational, Vet Approved
PrazosinPrazosin may increase the hypotensive activities of Azimilide.Approved
PrimidoneThe metabolism of Azimilide can be increased when combined with Primidone.Approved, Vet Approved
RadicicolThe risk or severity of adverse effects can be increased when Radicicol is combined with Azimilide.Experimental
RapacuroniumAzimilide may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RifabutinThe serum concentration of Azimilide can be decreased when it is combined with Rifabutin.Approved
RifampicinThe serum concentration of Azimilide can be decreased when it is combined with Rifampicin.Approved
RifapentineThe serum concentration of Azimilide can be decreased when it is combined with Rifapentine.Approved
Salicylhydroxamic AcidThe risk or severity of adverse effects can be increased when Salicylhydroxamic Acid is combined with Azimilide.Experimental
Salicylic acidThe risk or severity of adverse effects can be increased when Salicylic acid is combined with Azimilide.Approved, Vet Approved
SecobarbitalThe metabolism of Azimilide can be increased when combined with Secobarbital.Approved, Vet Approved
SertaconazoleThe risk or severity of adverse effects can be increased when Sertaconazole is combined with Azimilide.Approved
SilodosinSilodosin may increase the hypotensive activities of Azimilide.Approved
SinefunginThe risk or severity of adverse effects can be increased when Sinefungin is combined with Azimilide.Experimental
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Azimilide.Approved, Investigational
SolithromycinThe metabolism of Azimilide can be decreased when combined with Solithromycin.Investigational
SulconazoleThe risk or severity of adverse effects can be increased when Sulconazole is combined with Azimilide.Approved
TamsulosinTamsulosin may increase the hypotensive activities of Azimilide.Approved, Investigational
TavaboroleThe risk or severity of adverse effects can be increased when Tavaborole is combined with Azimilide.Approved
TelithromycinThe metabolism of Azimilide can be decreased when combined with Telithromycin.Approved
TerazosinTerazosin may increase the hypotensive activities of Azimilide.Approved
TerbinafineThe risk or severity of adverse effects can be increased when Terbinafine is combined with Azimilide.Approved, Investigational, Vet Approved
TerconazoleThe risk or severity of adverse effects can be increased when Terconazole is combined with Azimilide.Approved
ThiamylalThe metabolism of Azimilide can be increased when combined with Thiamylal.Approved, Vet Approved
ThiopentalThe metabolism of Azimilide can be increased when combined with Thiopental.Approved, Vet Approved
ThymolThe risk or severity of adverse effects can be increased when Thymol is combined with Azimilide.Approved
TioconazoleThe risk or severity of adverse effects can be increased when Tioconazole is combined with Azimilide.Approved
TolnaftateThe risk or severity of adverse effects can be increased when Tolnaftate is combined with Azimilide.Approved, Vet Approved
TrimazosinTrimazosin may increase the hypotensive activities of Azimilide.Experimental
TrimetrexateThe risk or severity of adverse effects can be increased when Trimetrexate is combined with Azimilide.Approved, Investigational
TroleandomycinThe metabolism of Azimilide can be decreased when combined with Troleandomycin.Approved
TylosinThe metabolism of Azimilide can be decreased when combined with Tylosin.Vet Approved
VoriconazoleThe risk or severity of adverse effects can be increased when Voriconazole is combined with Azimilide.Approved, Investigational
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Schmitt H, Cabo C, Coromilas JC, Wit AL: Effects of azimilide, a new class III antiarrhythmic drug, on reentrant circuits causing ventricular tachycardia and fibrillation in a canine model of myocardial infarction. J Cardiovasc Electrophysiol. 2001 Sep;12(9):1025-33. [PubMed:11573692 ]
  2. Abrol R, Page RL: Azimilide dihydrochloride: a new class III anti-arrhythmic agent. Expert Opin Investig Drugs. 2000 Nov;9(11):2705-15. [PubMed:11060832 ]
  3. Tran HT: Azimilide dihydrochloride: a unique class III antiarrhythmic agent. Heart Dis. 1999 May-Jun;1(2):114-6. [PubMed:11720612 ]
  4. Toothaker RD, Corey AE, Valentine SN, Agnew JR, Parekh N, Moehrke W, Thompson GA, Powell JH: Influence of coadministration on the pharmacokinetics of azimilide dihydrochloride and digoxin. J Clin Pharmacol. 2005 Jul;45(7):773-80. [PubMed:15951467 ]
  5. Riley P, Figary PC, Entwisle JR, Roe AL, Thompson GA, Ohashi R, Ohashi N, Moorehead TJ: The metabolic profile of azimilide in man: in vivo and in vitro evaluations. J Pharm Sci. 2005 Sep;94(9):2084-95. [PubMed:16052551 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9013
Caco-2 permeable-0.5057
P-glycoprotein substrateSubstrate0.7072
P-glycoprotein inhibitor IInhibitor0.79
P-glycoprotein inhibitor IINon-inhibitor0.5948
Renal organic cation transporterInhibitor0.614
CYP450 2C9 substrateNon-substrate0.7463
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7085
CYP450 1A2 substrateNon-inhibitor0.8317
CYP450 2C9 inhibitorNon-inhibitor0.7377
CYP450 2D6 inhibitorNon-inhibitor0.8987
CYP450 2C19 inhibitorInhibitor0.5383
CYP450 3A4 inhibitorNon-inhibitor0.8177
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8234
Ames testAMES toxic0.5429
CarcinogenicityNon-carcinogens0.7114
BiodegradationNot ready biodegradable0.9967
Rat acute toxicity2.6412 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.8037
hERG inhibition (predictor II)Inhibitor0.5718
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0861 mg/mLALOGPS
logP2.91ALOGPS
logP2.59ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)11.95ChemAxon
pKa (Strongest Basic)8.7ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area72.6 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity124.83 m3·mol-1ChemAxon
Polarizability50.15 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
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 hydantoins. These are heterocyclic compounds containing an imidazolidine substituted by ketone group at positions 2 and 4.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassAzolidines
Sub ClassImidazolidines
Direct ParentHydantoins
Alternative Parents
Substituents
  • Hydantoin
  • Alpha-amino acid or derivatives
  • Halobenzene
  • Ureide
  • N-methylpiperazine
  • N-alkylpiperazine
  • Chlorobenzene
  • Aryl chloride
  • 1,4-diazinane
  • Piperazine
  • Semicarbazone
  • Aryl halide
  • Monocyclic benzene moiety
  • Benzenoid
  • Dicarboximide
  • Heteroaromatic compound
  • Furan
  • Semicarbazide
  • Tertiary amine
  • Tertiary aliphatic amine
  • Amino acid or derivatives
  • Oxacycle
  • Carboxylic acid derivative
  • Azacycle
  • Organooxygen compound
  • Organic oxygen compound
  • Amine
  • Carbonyl group
  • Organic nitrogen compound
  • Hydrocarbon derivative
  • Organic oxide
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Aromatic heteromonocyclic compound
Molecular FrameworkAromatic heteromonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Telethonin binding
Specific Function:
Ancillary protein that assembles as a beta subunit with a voltage-gated potassium channel complex of pore-forming alpha subunits. Modulates the gating kinetics and enhances stability of the channel complex. Assembled with KCNB1 modulates the gating characteristics of the delayed rectifier voltage-dependent potassium channel KCNB1 (PubMed:19219384). Assembled with KCNQ1/KVLQT1 is proposed to for...
Gene Name:
KCNE1
Uniprot ID:
P15382
Molecular Weight:
14674.66 Da
References
  1. Schmitt H, Cabo C, Coromilas JC, Wit AL: Effects of azimilide, a new class III antiarrhythmic drug, on reentrant circuits causing ventricular tachycardia and fibrillation in a canine model of myocardial infarction. J Cardiovasc Electrophysiol. 2001 Sep;12(9):1025-33. [PubMed:11573692 ]
  2. Abrol R, Page RL: Azimilide dihydrochloride: a new class III anti-arrhythmic agent. Expert Opin Investig Drugs. 2000 Nov;9(11):2705-15. [PubMed:11060832 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Potassium channel that plays an important role in a number of tissues, including heart, inner ear, stomach and colon (By similarity) (PubMed:10646604). Associates with KCNE beta subunits that modulates current kinetics (By similarity) (PubMed:9312006, PubMed:9108097, PubMed:8900283, PubMed:10646604, PubMed:11101505, PubMed:19687231). Induces a voltage-dependent by rapidly activating and slowly ...
Gene Name:
KCNQ1
Uniprot ID:
P51787
Molecular Weight:
74697.925 Da
References
  1. Schmitt H, Cabo C, Coromilas JC, Wit AL: Effects of azimilide, a new class III antiarrhythmic drug, on reentrant circuits causing ventricular tachycardia and fibrillation in a canine model of myocardial infarction. J Cardiovasc Electrophysiol. 2001 Sep;12(9):1025-33. [PubMed:11573692 ]
  2. Abrol R, Page RL: Azimilide dihydrochloride: a new class III anti-arrhythmic agent. Expert Opin Investig Drugs. 2000 Nov;9(11):2705-15. [PubMed:11060832 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
References
  1. Schmitt H, Cabo C, Coromilas JC, Wit AL: Effects of azimilide, a new class III antiarrhythmic drug, on reentrant circuits causing ventricular tachycardia and fibrillation in a canine model of myocardial infarction. J Cardiovasc Electrophysiol. 2001 Sep;12(9):1025-33. [PubMed:11573692 ]
  2. Abrol R, Page RL: Azimilide dihydrochloride: a new class III anti-arrhythmic agent. Expert Opin Investig Drugs. 2000 Nov;9(11):2705-15. [PubMed:11060832 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Riley P, Figary PC, Entwisle JR, Roe AL, Thompson GA, Ohashi R, Ohashi N, Moorehead TJ: The metabolic profile of azimilide in man: in vivo and in vitro evaluations. J Pharm Sci. 2005 Sep;94(9):2084-95. [PubMed:16052551 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Riley P, Figary PC, Entwisle JR, Roe AL, Thompson GA, Ohashi R, Ohashi N, Moorehead TJ: The metabolic profile of azimilide in man: in vivo and in vitro evaluations. J Pharm Sci. 2005 Sep;94(9):2084-95. [PubMed:16052551 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Riley P, Figary PC, Entwisle JR, Roe AL, Thompson GA, Ohashi R, Ohashi N, Moorehead TJ: The metabolic profile of azimilide in man: in vivo and in vitro evaluations. J Pharm Sci. 2005 Sep;94(9):2084-95. [PubMed:16052551 ]
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Drug created on October 21, 2007 16:23 / Updated on August 17, 2016 12:24