EFONIDIPINE

EFONIDIPINE Basic information
Product Name:EFONIDIPINE
Synonyms:Efonidipine hydrochloride monoethanolate;Efonidipine Hydrochloride ethanol (1:1:1);2-(phenyl(phenylmethyl)amino)ethyleste;3-pyridinecarboxylicacid,1,4-dihydro-2,6-dimethyl-5-(5,5-dimethyl-1,3,2-dioxa;efonidipinehydrochlorideethanolate;nz-105;nz105ethanolate;r,p-oxide,monohydrochloride
CAS:111011-76-8
MF:C34H38N3O7P
MW:631.66
EINECS:
Product Categories:
Mol File:111011-76-8.mol
EFONIDIPINE Structure
EFONIDIPINE Chemical Properties
Melting point 151° (dec)
storage temp. Inert atmosphere,2-8°C
solubility DMSO : 25 mg/mL (35.01 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)
form Powder
Safety Information
MSDS Information
EFONIDIPINE Usage And Synthesis
DescriptionEfonidipine hydrochloride ethanol was first launched in Japan for the treatment of essential severe and renal hypertension. As the fourteenth dihydropyridine (DHP) calcium channel blocker to reach the market, it functions by binding to the DHP receptors on voltage-dependent calcium channels to cause diuretic and natriuretic actions in patients with essential hypertension. Its vasodilating and calcium antagonist effects are very slow in onset and long-lasting in all types of experimentally hypertensive models and the agent is reported to exhibit an improved side effect profile compared with other drugs of the same class. This may be explained by the slow and long-lasting inhibition of transmembrane Ca+2 uptake, which is accompanied by its very slow binding to and dissociation from the DHP receptors. A recent study in cholesterol-fed rabbits suggested that efonidipine may suppress the development of atherosclerosis without affecting the plasma lipids. Clinical trials for angina, peetoris, and for cerebrovasodilatory disorders have been reported.
OriginatorNissan Chemical (Japan)
UsesEfonidipine Hydrochloride Monoethanolate is a potent inhibitor of the L-type calcium channel.
DefinitionChEBI: Efonidipine hydrochloride is a dihydropyridine.
Brand nameLandel
Biological ActivitySelective blocker of L-type and T-type Ca 2+ channels. Displays minimal inhibition of N- and P/Q-type channels and no inhibition of R-type channels. R (-) and S (+)-enantiomers displays different channel selectivity; S (+)-Efonidipine blocks L-type and T-type channels whereas R (-)-Efonidipine displays selectivity for T-type channels. Exhibits antihypertensive activity.
EFONIDIPINE Preparation Products And Raw materials
Isosorbide dinitrate

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