Identification

Name
Moricizine
Accession Number
DB00680  (APRD01124)
Type
Small Molecule
Groups
Approved, Withdrawn
Description

An antiarrhythmia agent used primarily for ventricular rhythm disturbances. [PubChem]

Structure
Thumb
Synonyms
  • [10-(3-Morpholin-4-yl-propionyl)-10H-phenothiazin-2-yl]-carbamic acid ethyl ester
  • EN-313
  • Ethmozin
  • Ethyl 10-(3-morpholinopropionyl)phenothiazine-2-carbamate
  • Ethyl 10-(beta-N-morpholinylpropionyl)phenothiazine-2-carbamate
  • Etmozin
  • Moracizin
  • Moracizina
  • Moracizine
  • Moracizinum
  • Moricizine
External IDs
EN-313 / G 214
Product Ingredients
IngredientUNIICASInChI Key
moricizine hydrochloride71OK3Z1ESP 29560-58-5GAQAKFHSULJNAK-UHFFFAOYSA-N
International/Other Brands
Ethmozine / Etmozins (Olainfarm)
Categories
UNII
2GT1D0TMX1
CAS number
31883-05-3
Weight
Average: 427.517
Monoisotopic: 427.156576993
Chemical Formula
C22H25N3O4S
InChI Key
FUBVWMNBEHXPSU-UHFFFAOYSA-N
InChI
InChI=1S/C22H25N3O4S/c1-2-29-22(27)23-16-7-8-20-18(15-16)25(17-5-3-4-6-19(17)30-20)21(26)9-10-24-11-13-28-14-12-24/h3-8,15H,2,9-14H2,1H3,(H,23,27)
IUPAC Name
ethyl N-{10-[3-(morpholin-4-yl)propanoyl]-10H-phenothiazin-2-yl}carbamate
SMILES
CCOC(=O)NC1=CC2=C(SC3=CC=CC=C3N2C(=O)CCN2CCOCC2)C=C1

Pharmacology

Indication

Used to treat irregular heartbeats (arrhythmias) and maintain a normal heart rate.

Structured Indications
Not Available
Pharmacodynamics

Moricizine is used to treat irregular heartbeats (arrhythmias) and to maintain a normal heart rate. It acts on the heart muscle to improve the heart's rhythm. Moricizine has potent local anesthetic activity and membrane stabilizing effect. Decreases excitability, conduction velocity, and automaticity as a result of slowed atrioventricular (AV) nodal and His-Purkinje conduction. Decreases the action potential duration (APD) in Purkinje fibers; also decreases the effective refractory period (ERP) but to a lesser extent than the APD, so the ERP/APD ratio is increased. Decreases the maxiumum rate of Phase 0 depolarization (V max ), but does not affect action potential amplitude or maximum diastolic potential. Does not affect atrial, AV nodal, or left ventricular refractory periods and has minimal effect on ventricular repolarization (evidenced by the overall decrease in JT interval). Has no effect on sinoatrial (SA) nodal or intra-atrial conduction and only minimal effect on sinus cycle length and sinus node recovery time. In the Vaughan Williams classification of antiarrhythmics, moricizine is considered to be a class I agent. It has properties of class IA, IB, and IC agents but does not clearly belong to any of the three subclasses. It has less effect on the slope of phase 0 and a greater effect on action potential duration and effective refractory period than class IC agents.

Mechanism of action

Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes.

TargetActionsOrganism
ASodium channel protein type 5 subunit alpha
inhibitor
Human
Absorption

Well absorbed, absorption is complete within 2 to 3 hours. Significant first-pass metabolism results in an absolute bioavailability of approximately 38%. Administration within 30 minutes after a meal slows the rate, but does not affect the extent of absorption, although peak plasma concentrations are reduced.

Volume of distribution
  • 300 L
Protein binding

Approximately 95%.

Metabolism

Hepatic and extensive, to at least 26 metabolites, none accounting for as much as 1% of the administered dose. Two metabolites may be pharmacologically active but are present in extremely small quantities. Moricizine induces its own metabolism (it induces hepatic cytochrome P-450 activity).

Route of elimination

Less than 1% of orally administered Ethmozine® is excreted unchanged in the urine. Approximately 56% of the administered dose is excreted in the feces and 39% is excreted in the urine.

Half life

2 hours (range 1.5-3.5 hours).

Clearance
Not Available
Toxicity

Symptoms of overdose include vomiting, unconsciousness, and severe low blood pressure.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
5'-Deoxy-5'-MethylthioadenosineThe serum concentration of Moricizine can be increased when it is combined with 5'-Deoxy-5'-Methylthioadenosine.Experimental
AcebutololMoricizine may increase the hypotensive activities of Acebutolol.Approved
AlaproclateThe risk or severity of adverse effects can be increased when Moricizine is combined with Alaproclate.Experimental
AlfentanilMoricizine may increase the hypotensive activities of Alfentanil.Approved, Illicit
AlgeldrateAlgeldrate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AlmagateAlmagate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AlmasilateAlmasilate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AloglutamolAloglutamol can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AlphacetylmethadolMoricizine may increase the hypotensive activities of Alphacetylmethadol.Experimental, Illicit
AlphaprodineMoricizine may increase the hypotensive activities of Alphaprodine.Illicit
AlprenololMoricizine may increase the hypotensive activities of Alprenolol.Approved, Withdrawn
AluminiumAluminium can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminium acetoacetateAluminium acetoacetate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminium glycinateAluminium glycinate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AmodiaquineThe serum concentration of Moricizine can be increased when it is combined with Amodiaquine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Moricizine is combined with Amoxapine.Approved
ArotinololMoricizine may increase the hypotensive activities of Arotinolol.Approved
ArtemetherThe serum concentration of Moricizine can be increased when it is combined with Artemether.Approved
ArtemisininThe serum concentration of Moricizine can be increased when it is combined with Artemisinin.Investigational
ArtemotilThe serum concentration of Moricizine can be increased when it is combined with Artemotil.Experimental
ArtenimolThe serum concentration of Moricizine can be increased when it is combined with Artenimol.Approved
ArtesunateThe serum concentration of Moricizine can be increased when it is combined with Artesunate.Approved
AtenololMoricizine may increase the hypotensive activities of Atenolol.Approved
AtovaquoneThe serum concentration of Moricizine can be increased when it is combined with Atovaquone.Approved
BefunololMoricizine may increase the hypotensive activities of Befunolol.Experimental
BetaxololMoricizine may increase the hypotensive activities of Betaxolol.Approved
BevantololMoricizine may increase the hypotensive activities of Bevantolol.Approved
BezitramideMoricizine may increase the hypotensive activities of Bezitramide.Experimental, Illicit, Withdrawn
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Bismuth subnitrateBismuth subnitrate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
BisoprololMoricizine may increase the hypotensive activities of Bisoprolol.Approved
BopindololMoricizine may increase the hypotensive activities of Bopindolol.Approved
BucindololMoricizine may increase the hypotensive activities of Bucindolol.Investigational
BufuralolMoricizine may increase the hypotensive activities of Bufuralol.Experimental, Investigational
BupranololMoricizine may increase the hypotensive activities of Bupranolol.Approved
BuprenorphineMoricizine may increase the hypotensive activities of Buprenorphine.Approved, Illicit, Investigational, Vet Approved
ButorphanolMoricizine may increase the hypotensive activities of Butorphanol.Approved, Illicit, Vet Approved
Calcium CarbonateCalcium Carbonate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium silicateCalcium silicate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
CarfentanilMoricizine may increase the hypotensive activities of Carfentanil.Illicit, Vet Approved
CarteololMoricizine may increase the hypotensive activities of Carteolol.Approved
CarvedilolMoricizine may increase the hypotensive activities of Carvedilol.Approved, Investigational
CeliprololMoricizine may increase the hypotensive activities of Celiprolol.Approved, Investigational
ChloroquineThe serum concentration of Moricizine can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorproguanilThe serum concentration of Moricizine can be increased when it is combined with Chlorproguanil.Investigational
CitalopramThe risk or severity of adverse effects can be increased when Moricizine is combined with Citalopram.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Moricizine is combined with Clomipramine.Approved, Vet Approved
CloranololMoricizine may increase the hypotensive activities of Cloranolol.Experimental
CodeineMoricizine may increase the hypotensive activities of Codeine.Approved, Illicit
Cycloguanil embonateThe serum concentration of Moricizine can be increased when it is combined with Cycloguanil embonate.Experimental
DapoxetineThe risk or severity of adverse effects can be increased when Moricizine is combined with Dapoxetine.Investigational
DapsoneThe serum concentration of Moricizine can be increased when it is combined with Dapsone.Approved, Investigational
DextromoramideMoricizine may increase the hypotensive activities of Dextromoramide.Experimental, Illicit
DextropropoxypheneMoricizine may increase the hypotensive activities of Dextropropoxyphene.Approved, Illicit, Withdrawn
DezocineMoricizine may increase the hypotensive activities of Dezocine.Approved
DihydrocodeineMoricizine may increase the hypotensive activities of Dihydrocodeine.Approved, Illicit
DihydroetorphineMoricizine may increase the hypotensive activities of Dihydroetorphine.Experimental, Illicit
DihydromorphineMoricizine may increase the hypotensive activities of Dihydromorphine.Experimental, Illicit
DiphenoxylateMoricizine may increase the hypotensive activities of Diphenoxylate.Approved, Illicit
DoxycyclineThe serum concentration of Moricizine can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DPDPEMoricizine may increase the hypotensive activities of DPDPE.Investigational
EpanololMoricizine may increase the hypotensive activities of Epanolol.Experimental
EscitalopramThe risk or severity of adverse effects can be increased when Moricizine is combined with Escitalopram.Approved, Investigational
EsmololMoricizine may increase the hypotensive activities of Esmolol.Approved
EthylmorphineMoricizine may increase the hypotensive activities of Ethylmorphine.Approved, Illicit
EtorphineMoricizine may increase the hypotensive activities of Etorphine.Illicit, Vet Approved
FenfluramineThe risk or severity of adverse effects can be increased when Moricizine is combined with Fenfluramine.Illicit, Withdrawn
FentanylMoricizine may increase the hypotensive activities of Fentanyl.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when Moricizine is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Moricizine is combined with Fluvoxamine.Approved, Investigational
HalofantrineThe serum concentration of Moricizine can be increased when it is combined with Halofantrine.Approved
HeroinMoricizine may increase the hypotensive activities of Heroin.Approved, Illicit
HydrocodoneMoricizine may increase the hypotensive activities of Hydrocodone.Approved, Illicit
HydromorphoneMoricizine may increase the hypotensive activities of Hydromorphone.Approved, Illicit
HydrotalciteHydrotalcite can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
HydroxychloroquineThe serum concentration of Moricizine can be increased when it is combined with Hydroxychloroquine.Approved
IndalpineThe risk or severity of adverse effects can be increased when Moricizine is combined with Indalpine.Investigational, Withdrawn
IndenololMoricizine may increase the hypotensive activities of Indenolol.Withdrawn
KetobemidoneMoricizine may increase the hypotensive activities of Ketobemidone.Approved
LabetalolMoricizine may increase the hypotensive activities of Labetalol.Approved
LandiololMoricizine may increase the hypotensive activities of Landiolol.Investigational
LevobunololMoricizine may increase the hypotensive activities of Levobunolol.Approved
Levomethadyl AcetateMoricizine may increase the hypotensive activities of Levomethadyl Acetate.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Moricizine is combined with Levomilnacipran.Approved
LevorphanolMoricizine may increase the hypotensive activities of Levorphanol.Approved
LofentanilMoricizine may increase the hypotensive activities of Lofentanil.Illicit
LumefantrineThe serum concentration of Moricizine can be increased when it is combined with Lumefantrine.Approved
MagaldrateMagaldrate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Withdrawn
Magnesium HydroxideMagnesium Hydroxide can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium peroxideMagnesium peroxide can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium silicateMagnesium silicate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Moricizine resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MefloquineThe serum concentration of Moricizine can be increased when it is combined with Mefloquine.Approved
MepindololMoricizine may increase the hypotensive activities of Mepindolol.Experimental
MeptazinolMoricizine may increase the hypotensive activities of Meptazinol.Experimental
MethadoneMoricizine may increase the hypotensive activities of Methadone.Approved
Methadyl AcetateMoricizine may increase the hypotensive activities of Methadyl Acetate.Approved, Illicit
MetipranololMoricizine may increase the hypotensive activities of Metipranolol.Approved
MetoprololMoricizine may increase the hypotensive activities of Metoprolol.Approved, Investigational
MilnacipranThe risk or severity of adverse effects can be increased when Moricizine is combined with Milnacipran.Approved
MizoribineThe serum concentration of Moricizine can be increased when it is combined with Mizoribine.Investigational
MorphineMoricizine may increase the hypotensive activities of Morphine.Approved, Investigational
NadololMoricizine may increase the hypotensive activities of Nadolol.Approved
NalbuphineMoricizine may increase the hypotensive activities of Nalbuphine.Approved
NicomorphineMoricizine may increase the hypotensive activities of Nicomorphine.Experimental
NormethadoneMoricizine may increase the hypotensive activities of Normethadone.Approved, Illicit
OlanzapineThe risk or severity of adverse effects can be increased when Moricizine is combined with Olanzapine.Approved, Investigational
OpiumMoricizine may increase the hypotensive activities of Opium.Approved, Illicit
OxprenololMoricizine may increase the hypotensive activities of Oxprenolol.Approved
OxycodoneMoricizine may increase the hypotensive activities of Oxycodone.Approved, Illicit, Investigational
OxymorphoneMoricizine may increase the hypotensive activities of Oxymorphone.Approved, Investigational, Vet Approved
ParoxetineThe risk or severity of adverse effects can be increased when Moricizine is combined with Paroxetine.Approved, Investigational
PenbutololMoricizine may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentazocineMoricizine may increase the hypotensive activities of Pentazocine.Approved, Vet Approved
PethidineMoricizine may increase the hypotensive activities of Pethidine.Approved
PhenazocineMoricizine may increase the hypotensive activities of Phenazocine.Experimental
PhenoperidineMoricizine may increase the hypotensive activities of Phenoperidine.Experimental
PindololMoricizine may increase the hypotensive activities of Pindolol.Approved
PiritramideMoricizine may increase the hypotensive activities of Piritramide.Investigational
PractololMoricizine may increase the hypotensive activities of Practolol.Approved
PrimaquineThe serum concentration of Moricizine can be increased when it is combined with Primaquine.Approved
ProguanilThe serum concentration of Moricizine can be increased when it is combined with Proguanil.Approved
PropranololMoricizine may increase the hypotensive activities of Propranolol.Approved, Investigational
PyrimethamineThe serum concentration of Moricizine can be increased when it is combined with Pyrimethamine.Approved, Vet Approved
PyronaridineThe serum concentration of Moricizine can be increased when it is combined with Pyronaridine.Investigational
QuinacrineThe serum concentration of Moricizine can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Moricizine can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Moricizine can be increased when it is combined with Quinine.Approved
RadicicolThe serum concentration of Moricizine can be increased when it is combined with Radicicol.Experimental
RemifentanilMoricizine may increase the hypotensive activities of Remifentanil.Approved
SertralineThe risk or severity of adverse effects can be increased when Moricizine is combined with Sertraline.Approved
SinefunginThe serum concentration of Moricizine can be increased when it is combined with Sinefungin.Experimental
SotalolMoricizine may increase the hypotensive activities of Sotalol.Approved
SufentanilMoricizine may increase the hypotensive activities of Sufentanil.Approved, Investigational
SulfadoxineThe serum concentration of Moricizine can be increased when it is combined with Sulfadoxine.Approved
SulfametopyrazineThe serum concentration of Moricizine can be increased when it is combined with Sulfametopyrazine.Approved, Withdrawn
tafenoquineThe serum concentration of Moricizine can be increased when it is combined with tafenoquine.Investigational
TalinololMoricizine may increase the hypotensive activities of Talinolol.Investigational
TapentadolMoricizine may increase the hypotensive activities of Tapentadol.Approved
TertatololMoricizine may increase the hypotensive activities of Tertatolol.Experimental
ThiopentalThe risk or severity of adverse effects can be increased when Moricizine is combined with Thiopental.Approved, Vet Approved
TilidineMoricizine may increase the hypotensive activities of Tilidine.Experimental
TimololMoricizine may increase the hypotensive activities of Timolol.Approved
TramadolMoricizine may increase the hypotensive activities of Tramadol.Approved, Investigational
TrazodoneThe risk or severity of adverse effects can be increased when Moricizine is combined with Trazodone.Approved, Investigational
TrimethoprimThe serum concentration of Moricizine can be increased when it is combined with Trimethoprim.Approved, Vet Approved
VilazodoneThe risk or severity of adverse effects can be increased when Moricizine is combined with Vilazodone.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Moricizine is combined with Vortioxetine.Approved
ZimelidineThe risk or severity of adverse effects can be increased when Moricizine is combined with Zimelidine.Withdrawn
Food Interactions
Not Available

References

Synthesis Reference
US3740395A
General References
Not Available
External Links
Human Metabolome Database
HMDB14818
KEGG Drug
D05077
KEGG Compound
C07743
PubChem Compound
34633
PubChem Substance
46509072
ChemSpider
31872
ChEBI
6997
ChEMBL
CHEMBL1075
Therapeutic Targets Database
DAP000510
PharmGKB
PA164747738
Drugs.com
Drugs.com Drug Page
Wikipedia
Moricizine
ATC Codes
C01BG01 — Moracizine
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2CompletedTreatmentArrythmias / Cardiovascular Disease (CVD) / Heart Diseases / Ventricular Arrythmias1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Death, Sudden,Cardiac / Heart Arrest / Heart Diseases / Myocardial Infarction (MI) / Myocardial Ischemia / Ventricular Arrythmias1
3CompletedTreatmentArrythmias / Cardiovascular Disease (CVD) / Heart Diseases / Nonvalvular Atrial Fibrillation1

Pharmacoeconomics

Manufacturers
  • Shire development inc
Packagers
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)156-157 °CPhysProp
water solubility0.457 mg/LNot Available
logP2.98SANGSTER (1994)
Predicted Properties
PropertyValueSource
Water Solubility0.0339 mg/mLALOGPS
logP3.04ALOGPS
logP3.07ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)12.9ChemAxon
pKa (Strongest Basic)6.73ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area71.11 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity118.88 m3·mol-1ChemAxon
Polarizability45.27 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9885
Blood Brain Barrier+0.9535
Caco-2 permeable-0.5796
P-glycoprotein substrateSubstrate0.6871
P-glycoprotein inhibitor IInhibitor0.9072
P-glycoprotein inhibitor IINon-inhibitor0.5751
Renal organic cation transporterNon-inhibitor0.8329
CYP450 2C9 substrateNon-substrate0.7472
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.5274
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.6367
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.7959
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.7638
Ames testNon AMES toxic0.6915
CarcinogenicityNon-carcinogens0.9153
BiodegradationNot ready biodegradable0.8412
Rat acute toxicity2.4731 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9229
hERG inhibition (predictor II)Inhibitor0.732
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of chemical entities known as phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
Kingdom
Chemical entities
Super Class
Organic compounds
Class
Organoheterocyclic compounds
Sub Class
Benzothiazines
Direct Parent
Phenothiazines
Alternative Parents
Diarylthioethers / Beta amino acids and derivatives / 1,4-thiazines / Morpholines / Benzenoids / Tertiary carboxylic acid amides / Trialkylamines / Propargyl-type 1,3-dipolar organic compounds / Oxacyclic compounds / Azacyclic compounds
show 6 more
Substituents
Phenothiazine / Beta amino acid or derivatives / Diarylthioether / Aryl thioether / Para-thiazine / Morpholine / Oxazinane / Benzenoid / Tertiary carboxylic acid amide / Amino acid or derivatives
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
phenothiazines, carbamate ester, morpholines (CHEBI:6997 )

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Voltage-gated sodium channel activity involved in sa node cell action potential
Specific Function
This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the pr...
Gene Name
SCN5A
Uniprot ID
Q14524
Uniprot Name
Sodium channel protein type 5 subunit alpha
Molecular Weight
226937.475 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. Ahmmed GU, Hisatome I, Kurata Y, Makita N, Tanaka Y, Tanaka H, Okamura T, Sonoyama K, Furuse Y, Kato M, Yamamoto Y, Ogura K, Shimoyama M, Miake J, Sasaki N, Ogino K, Igawa O, Yoshida A, Shigemasa C: Analysis of moricizine block of sodium current in isolated guinea-pig atrial myocytes. Atrioventricular difference of moricizine block. Vascul Pharmacol. 2002 Mar;38(3):131-41. [PubMed:12402511 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Drug created on June 13, 2005 07:24 / Updated on October 02, 2017 04:42