Home Neuronal Signaling Histamine Receptor antagonist Azelastine HCl For research use only.

Azelastine HCl

Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.

Azelastine HCl Chemical Structure

Azelastine HCl Chemical Structure

CAS No. 79307-93-0

Purity & Quality Control

Azelastine HCl Related Products

Signaling Pathway

Histamine Receptor Signaling Pathways

Histamine Receptor Signaling Pathway

Biological Activity

Description Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Targets
Histamine receptor [1]
In vitro
In vitro Azelastine inhibits Ag- and ionomycin-induced TNF-alpha release with IC50 values of 25.7 mM and 1.66 mM, respectively, in a rat mast RBL-2H3 cell line. Azelastine also inhibits TNF-alpha mRNA expression, TNF-alpha protein synthesis and release, and, possibly related to these effects, Ca2+ influx, in Ag-stimulated cells. Azelastine inhibits TNF-alpha release to a greater extent than mRNA expression/protein synthesis and Ca2+ influx in ionomycin-stimulated cells, suggesting that Azelastine inhibits the release process more potently than transcription or production of TNF-alpha by interfering with a signal other than Ca2+. Azelastine added 1 hour after ionomycin stimulation also immediately blocks subsequent release of TNF-alpha, which has been produced in the cells, without affecting Ca2+ influx. Azelastine inhibits ionomycin-induced, but not Ag-induced, protein kinase C translocation to the membranes. [1] Azelastine hydrochloride (Azeptin) dose-dependently suppresses both DNA and protein synthesis in human gingival fibroblasts (HF) and also suppresses blastogenesis of human peripheral blood lymphocytes (PBL). Azelastine hydrochloride (Azeptin) suppresses both inducible nitric oxide synthase-mRNA level and NO generation in mouse peritoneal macrophages. [2] Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells. [3]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00612118 Completed
Allergic Rhinitis|Rhinitis Allergic Seasonal
GlaxoSmithKline
 February 2008 Phase 2

Chemical Information & Solubility

Molecular Weight 418.36 Formula

C22H24ClN3O.HCl
CAS No. 79307-93-0 SDF Download Azelastine HCl SDF
Smiles CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 84 mg/mL ( (200.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : 35 mg/mL


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In vivo
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