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Merck
CN

A7611

Azelastine hydrochloride

≥98% (HPLC)

Synonym(s):

4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one hydrochloride, Astelin, Optivar

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About This Item

Empirical Formula (Hill Notation):
C22H24ClN3O · HCl
CAS Number:
79307-93-0
Molecular Weight:
418.36
MDL number:
MFCD00242783
UNSPSC Code:
12352200
PubChem Substance ID:
329770938
NACRES:
NA.77

Key Documents

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Quality Level

100

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to off-white

solubility

DMSO: >10 mg/mL

originator

Wallace

storage temp.

−20°C

SMILES string

Cl.CN1CCCC(CC1)N2N=C(Cc3ccc(Cl)cc3)c4ccccc4C2=O

InChI

1S/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H

InChI key

YEJAJYAHJQIWNU-UHFFFAOYSA-N

Gene Information

human ... HRH1(3269)

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Application

Azelastine hydrochloride is a H1 histamine receptor antagonist and NF-kB activator. Azelastine hydrochloride has been used in a study to investigate the potential of polymeric microspheres for treatment of allergic conjunctivitis.

Biochem/physiol Actions

H1 histamine receptor antagonist; NF-kB activator.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Wallace. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Pictograms

Exclamation mark
GHS07

Signal Word

Warning

Hazard Statements

H302

Precautionary Statements

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000247045
0000247045
030M4702V
0000136710
0000126491

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Alisa Rudnitskaya et al.
Analytica chimica acta, 770, 45-52 (2013-03-19)
The application of the potentiometric multisensor system (electronic tongue, ET) for quantification of the bitter taste of structurally diverse active pharmaceutical ingredients (API) is reported. The measurements were performed using a set of bitter substances that had been assessed by
Hartmut Derendorf et al.
British journal of clinical pharmacology, 74(1), 125-133 (2012-02-24)
• The topical second generation anti-histamine azelastine hydrochloride (AZE) and the potent corticosteroid fluticasone propionate (FP) are well established first-line treatments in allergic rhinitis (AR). • MP29-02, a novel intranasal AZE and FP formulation, has been shown to control AR
Jonathan A Bernstein
Current medical research and opinion, 23(10), 2441-2452 (2007-08-29)
Azelastine hydrochloride (Astelin) nasal spray 0.1% solution is a second-generation intranasal antihistamine available in the US for treatment of both seasonal allergic rhinitis (SAR) and nonallergic vasomotor rhinitis (VMR). Searches of journal articles including the title word 'azelastine' from 1979
Daniel Baumann et al.
European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 80(1), 156-163 (2011-09-29)
For locally acting drugs, an extended residence time in the nasal cavity is desirable and related to a prolonged effect. We sought to develop a model for comparative determination of intranasal pharmacokinetics. We embedded human respiratory tissue into a solid
Carsten Gründemann et al.
Journal of ethnopharmacology, 145(1), 118-126 (2012-11-13)
Extracts from Veronica officinalis L. are traditionally used for the treatment of lung diseases; however, the effective compounds and the mode of action are still unknown. Here we analyzed the effects of a standardized Veronica extract on genes expression and
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Articles

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