EMEDASTINE FUMARATE

ChemicalBook > CAS DataBase List > EMEDASTINE FUMARATE

Product Name: EMEDASTINE FUMARATE
CAS No.: 87233-62-3
Chemical Name: EMEDASTINE FUMARATE
Synonyms: Emadine;1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazoledifumarate;Daren;kb2413;Remicut;kb-2413;kg-2413;Rapimine;AL 3432A;ly188695
CBNumber: CB6714475
Molecular Formula: C25H34N4O9
Formula Weight: 534.56
MOL File: 87233-62-3.mol

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EMEDASTINE FUMARATE Property

Melting point:: 148-151°
storage temp.: 2-8°C
solubility: Soluble in water, sparingly soluble in anhydrous ethanol, very slightly soluble in acetone.
Merck: 14,3557

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Safety

RTECS: DD8870000
HS Code: 2933992600
Toxicity: LD50 orally in guinea pigs: 744 mg/kg (Fukuda)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: Y0000537
Product name: Emedastine difumarate
Purity: European Pharmacopoeia (EP) Reference Standard
Packaging: y0000537
Price: $150
Updated: 2024/03/01

Sigma-Aldrich

Product number: 1234806
Product name: Emedastine difumarate
Packaging: 100mg
Price: $406
Updated: 2024/03/01

TCI Chemical

Product number: E0936
Product name: Emedastine Difumarate
Purity: >98.0%(HPLC)(T)
Packaging: 200mg
Price: $244
Updated: 2021/12/16

Cayman Chemical

Product number: 23946
Product name: Emedastine (fumarate)
Purity: ≥98%
Packaging: 5mg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 23946
Product name: Emedastine (fumarate)
Purity: ≥98%
Packaging: 10mg
Price: $61
Updated: 2024/03/01

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EMEDASTINE FUMARATE Chemical Properties,Usage,Production

Description

Emedastine difumarate, a potent H₁-receptor antagonist, was launched in Japan for the treatment of allergic rhinitis and urticaria. Emedastine exerts its antiallergic effect via inhibition of substance P-induced histamine release. It has been demonstrated both in vitro and in vivo that this effect is mediated by the inhibition of Ca²⁺release from extracellular stores and of Ca²⁺ influx into mast cells. In a clinical trial with bronchial asthma, emedastine improved asthmatic symptoms in 55.3% of patients.

Description

Emedastine is a histamine H₁ receptor antagonist (K_i = 1.3 nM). It is selective for histamine H₁ over H₂ and H₃ receptors (K_is = 49 and 12.43 μM, respectively), as well as α₁-, α₂-, and β₁-adrenergic and dopamine D₁ and D₂ receptors, and the serotonin (5-HT) receptor subtypes 5-HT₁ and 5-HT₂ at 10 μM. Emedastine inhibits histamine-induced phosphoinositide turnover and intracellular calcium mobilization in primary human conjunctival epithelial cells (HCECs; IC₅₀s = 1.6 and 2.9 nM, respectively). It also inhibits histamine-stimulated secretion of IL-6, IL-8, and GM-CSF by primary HCECs (IC₅₀s = 2.23, 3.42, and 1.50 nM, respectively). Ocular application of emedastine prior to histamine challenge inhibits vascular permeability in guinea pigs. Formulations containing emedastine have been used in the treatment of allergic conjunctivitis.

Chemical Properties

White or yellowish powder

Originator

Kanebo (Japan)

Uses

Antihistaminic, H1-receptor; asthma prophylactic; anti-allergic.

Definition

ChEBI: The fumaric acid salt of emedastine containing two molecules of fumaric acid for each molecule of emedastine. A relatively selective histamine H1 antagonist, it is used for allergic rhinitis, urticaria, and pruritic skin disorders, and in eyedrops for the symptomatic relief of allergic conjuntivitis.

Manufacturing Process

Preparation of 2-(4-methyl-1-piperazinyl)benzimidazole. A mixture of 2- chlorobenzimidazole (10.00 g) and N-mehylpiperazine (20.00 g) is stirred at 125°C for 5 hours. A 10% aqueous sodium hydroxide (100 ml) is added to the reaction mixture, and the precipitated crystals are separated by filtration. The filtrate is extracted with chloroform, and the chloroform extract is evaporated to dryness to give the same crystals. The crystals are combined and recrystallized from water-methanol to give 2-(4-methyl-1- piperazinyl)benzimidazole (7.02 g) as colorless needles, m.p. 225°-226°C.
2-(4-Methyl-1-piperazinyl)benzimididazole (5.00 g) prepared as above is dissolved in N,N-dimethylformamide (50 ml) and thereto is added sodium hydride (concentration: 50%) (1.50 g) at room temperature, and the mixture is stirred for 30 minutes. To the mixture is added 2-bromoethyl ethyl ether (4.00 g), and the mixture is stirred at 70°C for 10 hours. To the reaction mixture is added water (150 ml), and the mixture is extracted with ethyl acetate. The extract is washed with water, dried over anhydrous magnesium sulfate and then concentrated to give a brown oily substance (5.40 g). The brown oily substance is treated with fumaric acid (3.26 g) in hot ethanol. The crude crystals thus obtained are recrystallized from ethyl acetate-ethanol to give 1-[2-(ethoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole 3/2 fumarate (6.31 g) as colorless plates, melting point 167.5°-168.5°C. Elementary analysis for C22H30N4O7: Calcd. (%): C, 57.13; H, 6.54; N, 12.11; Found (%): C, 57.04; H, 6.44; N, 12.02.
1-[2-(Ethoxy)ethyl]-2-(4-methyl-1-piperazinyl)benzimidazole can be prepared using 2-chloro-(1-[2-(ethoxy)ethyl]benzimidazole), (last one can be produced from 2-bromoethyl ethyl ether 2-chlorobenzimidazole) and N-methylpiperazine and fumaric acid there are obtained crude crystals, which are recrystallized from ethanol to give 1-[2-(ethoxy)ethyl]-2-(4-methyl-1- piperazinyl)benzimidazole 3/2 fumarate. This product has the same physical properties as those of the product above described.

brand name

Emadine (Alcon);Daren;Remicut.

Therapeutic Function

Antiallergic, Antihistaminic

Hazard

A poison by ingestion.

EMEDASTINE FUMARATE Preparation Products And Raw materials

Raw materials

Preparation Products

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View Lastest Price from EMEDASTINE FUMARATE manufacturers

Henan Fengda Chemical Co., Ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $32.00-1.30/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: g-kg-tons, free sample is available
Release date: 2024-04-15

Baoji Guokang Healthchem co.,ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $150.00/g
Min. Order: 1g
Purity: 99%
Supply Ability: 100KG
Release date: 2021-06-03

Hebei Zhanyao Biotechnology Co. Ltd

Product: EMEDASTINE FUMARATE 87233-62-3
Price: US $10.00/Kg/Bag
Min. Order: 1Kg/Bag
Purity: 99%
Supply Ability: 20 Tons
Release date: 2021-11-22

87233-62-3, EMEDASTINE FUMARATERelated Search:

/ EmedastineN-Oxide Emedastine EP Impurity C HCl EMEDASTINE FUMARATE Emedastine

1-(2-ethoxyethyl)-2-(4-methyl-1-homopiperazinyl)benzimidazoledifumarate

1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)-benzimidazol

1-(2-ethoxyethyl)-2-(4-methylhexahydro-1h-1,4-diazepin-1-yl)benzimidazolefum

1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepine-1-yl)-1H-benzimidazole·bisfumaric acid

Daren

Emedastin difumarate

Emedastin fumarate

Remicut

Emedastine Difumarate (100 mg)

Rapimine

Emadine

AL 3432A

1-(2-Ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-1H-benzimidazole (2E)-2-butenedioate (1:2)

1-(2-ethoxyethyl)-2-(4-methyl-1,4-diazepan-1-yl)-1H-benzo[d]imidazole difumarate

1h-benzimidazole,1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1h-1,4-diazepin-1-yl)

arate(1:2)

emedastinedifumarate

kb2413

kb-2413

kg-2413

ly188695

EMEDASTINE FUMARATE

EmedastineDifumarate&gt

Emedastine difumarate CRS

1-(2-Ethoxyethyl)-2-(4-methylhexahydro-1H-1,4-diazepin-1- yl)-1H-benzimidazole bis[hydrogen (2E)-butenedioate

Emestine Fumarate

Emedastine Difumarate (1234806)

87233-62-3

C25H34N4O9

C17H26N4O2C4H4O4