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Azelastine

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Azelastine Basic information

Product Name:
Azelastine
Synonyms:
  • 1(2h)-phthalazinone,4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin
  • 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1-(2h)-phthalazinon
  • 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one hydrochloride
  • 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1-one
  • 4-[(4-chlorophenyl)methyl]-2-(1-methyl-4-azepanyl)-1-phthalazinone
  • 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one
  • Azelastinum [INN-Latin]
  • KBio3_002992
CAS:
58581-89-8
MF:
C22H24ClN3O
MW:
381.9
EINECS:
253-720-4
Product Categories:
  • TELAZOL
  • API
Mol File:
58581-89-8.mol
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Azelastine Chemical Properties

Melting point:
111 - 115°C
Boiling point:
533.9±60.0 °C(Predicted)
Density 
1.1505 (rough estimate)
refractive index 
1.5790 (estimate)
storage temp. 
2-8°C
solubility 
Chloroform (Slightly), DMSO (Slightly, Heated), Methanol (Slightly)
pka
pKa 9.82(H2O t=25 I=0.025) (Uncertain)
form 
Solid
color 
White to Off-White
BCS Class
1?
Stability:
Stable under recommended storage conditions., Stable Under Recommended Storage C
CAS DataBase Reference
58581-89-8(CAS DataBase Reference)
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Safety Information

Hazardous Substances Data
58581-89-8(Hazardous Substances Data)
Toxicity
LD50 orl-rat: 310 mg/kg ARZNAD 31,1184,81
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Azelastine Usage And Synthesis

Description

Azelastine has potent, long-lasting histamine H1-receptor blocking activity and several other interesting anti-inflammatory properties related to its antiallergic efficacy .

Uses

anesthetic, anticonvulsant

Definition

ChEBI: A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position.

brand name

Astelin (Medpointe); Optivar (Medpointe).

Clinical Use

Azelastine, although not a close structural analogue to the benzimidazoles, has some structural similarities to them. It is used as a nasal spray for allergic rhinitis and as eye drops for allergic conjunctivitis.Like olopatadine, azelastine also stabilizes mast cells, preventing degranulation and subsequent release of histamine, leukotrienes, and PGD2. It is available in Europe for systemic use in the treatment of asthma and seasonal allergies. Besides antihistaminic effects, it also may block release of histamine and other inflammatory mediators from mast cells. When administered orally, the N-dealkylated metabolite appears to contribute significantly to its pharmacological effects.

Safety Profile

Poison by ingestion,subcutaneous, intravenous, and intraperitoneal routes.Experimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and Cl- .

AzelastineSupplier

Wuhan Fortuna Chemical Co., Ltd Gold
Tel
027-027-59207852 13308628970
Email
buy@fortunachem.com
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Email
3bsc@sina.com
LGM Pharma
Tel
1-(800)-881-8210
Email
inquiries@lgmpharma.com
China Langchem Inc.
Tel
0086-21-58956006
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-83725681-603