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EFONIDIPINE

EFONIDIPINE structure

EFONIDIPINE 

structure
  • CAS No:

    111011-76-8

  • Formula:

    C34H38N3O7P

  • Chemical 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

  • Categories:

    Active Pharmaceutical Ingredients  >  Circulatory System Drugs

Description

Efonidipine 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


Efonidipine hydrochloride is a dihydropyridine.

EFONIDIPINE Basic Attributes

631.66

631.244751

DTXSID5020150

Characteristics

143

1.3±0.1 g/cm3

151° (dec)

405.5±32.9 °C

1.625

Desiccate at +4°C

Safety Information

P201, P202, P281, P308+P313, P405, P501

H361

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.

Drug Information

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|Agents that promote the excretion of urine through their effects on kidney function. (See all compounds classified as Diuretics.)|A class of drugs that act by selective inhibition of calcium influx through cellular membranes. (See all compounds classified as Calcium Channel Blockers.)

5-(5,5-dimethyl-1,3,2-dioxaphosphorinan-2-yl)-1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3-pyridinecarboxylic acid, 2-(phenyl(phenylmethyl)amino) ethyl ester, P-oxide, hydrochloride

EFONIDIPINE Use and Manufacturing

Selective 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.

Computed Properties

Molecular Weight:714.2
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:10
Rotatable Bond Count:10
Exact Mass:713.2632801
Monoisotopic Mass:713.2632801
Topological Polar Surface Area:143
Heavy Atom Count:49
Complexity:1170
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:3
Compound Is Canonicalized:Yes

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