Moricizine

Names

[ Name ]:
Moricizine

[Synonym ]:
Moracizin
Moracizina [INN-Spanish]
Moracizinum
ethyl N-[10-(3-morpholin-4-ylpropanoyl)phenothiazin-2-yl]carbamate
Moracizine
Moracizina
Ethmozin
[10-(3-morpholin-4-yl-propionyl)-10H-phenothiazin-2-yl]-carbamic acid ethyl ester
Ethmozine
Etmozin
MORICIZINE
Moracizinum [INN-Latin]
EINECS 250-854-5

Biological Activity

[Description]:

Moricizine is an antiarrhythmia agent used primarily for ventricular rhythm disturbances.Target: Sodium ChannelMoricizine is an antiarrhythmia agent used primarily for ventricular rhythm disturbances. Moricizine works by inhibiting the rapid inward sodium current across myocardial cell membranes. Moricizine induced the tonic block of INa with the apparent dissociation constant (Kd,app) of 6.3 microM at -100 mV and 99.3 microM at -140 mV. Moricizine at 30 microM shifted the h infinity curve to the hyperpolarizing direction by 8.6 +/- 2.4 mV. Moricizine also produced the phasic block of INa, which was enhanced with the increase in the duration of train pulses, and was more prominent with a holding potential (HP) of -100 mV than with an HP of -140 mV. Moricizine would exert an antiarrhythmic action on atrial myocytes, as well as on ventricular myocytes, by blocking Na+ channels with a high affinity to the inactivated state and a slow dissociation kinetics [1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Cardiovascular Disease

[References]

[1]. Ahmmed, G.U., et al., Analysis of moricizine block of sodium current in isolated guinea-pig atrial myocytes. Atrioventricular difference of moricizine block. Vascul Pharmacol, 2002. 38(3): p. 131-41.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.315g/cm3

[ Boiling Point ]:
625ºC at 760 mmHg

[ Molecular Formula ]:
C₂₂H₂₅N₃O₄S

[ Molecular Weight ]:
427.51700

[ Flash Point ]:
331.8ºC

[ Exact Mass ]:
427.15700

[ PSA ]:
96.41000

[ LogP ]:
4.18250

[ Index of Refraction ]:
1.639

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: FC9045000

CHEMICAL NAME :: Carbamic acid, (10-(3-(4-morpholinyl)-1-oxopropyl)-10H-phenothiazin- 2-yl)-, ethyl ester

CAS REGISTRY NUMBER :: 31883-05-3

LAST UPDATED :: 199703

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C22-H25-N3-O4-S

MOLECULAR WEIGHT :: 427.56

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 11 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #5116974

Safety Information

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%