Azelastine Hydrochloride

• CAT Number: A000915
• CAS Number: 79307-93-0
• Molecular Formula: C22H25Cl2N3O
• Molecular Weight: 418.4
• Purity: ≥95%
• Target: Histamine Receptor
• Solubility: Soluble in DMSO > 10 mM
• Storage: -20°C
• 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
• InChIKey: YEJAJYAHJQIWNU-UHFFFAOYSA-N
• SMILES: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl

Azelastine HCl is a potent and selective H1-receptor antagonist, with antiallergic effects related to histamine antagonism, and further antiallergic and anti-inflammatory effects unrelated to H1-receptor binding. Azelastine HCl is an activator of NF-kB activator. Azelastine hydrochloride has been used in a study to investigate the potential of polymeric microspheres for treatment of allergic conjunctivitis. Azelastine is shown to block secretion of IL-6, IL-8, and TNF alpha from mast cells by inhibiting NF-κB activation.

Reference

1: Karpishchenko SA, Kolesnikova OM. [The effectiveness of the combination of
azelastine hydrochloride and mometasone furoate for the intranasal application in
the patients presenting with seasonal allergic rhinitis]. Vestn Otorinolaringol.
2017;82(5):44-47. doi: 10.17116/otorino201782544-47. Russian. PubMed PMID:
29072663.

2: Scadding G, Price D, El-Shanawany T, Ahmed S, Ray J, Sargur R, Kumar N.
Multicentre, non-interventional study to assess the profile of patients with
uncontrolled rhinitis prescribed a novel formulation of azelastine hydrochloride
and fluticasone propionate in a single spray in routine clinical practice in the
UK. BMJ Open. 2017 Apr 24;7(4):e014777. doi: 10.1136/bmjopen-2016-014777. PubMed
PMID: 28442578.

3: Prenner BM. A review of the clinical efficacy and safety of MP-AzeFlu, a novel
intranasal formulation of azelastine hydrochloride and fluticasone propionate, in
clinical studies conducted during different allergy seasons in the US. J Asthma
Allergy. 2016 Jul 11;9:135-43. doi: 10.2147/JAA.S98172. eCollection 2016. Review.
PubMed PMID: 27468241; PubMed Central PMCID: PMC4946862.

4: Merey HA, El-Mosallamy SS, Hassan NY, El-Zeany BA. Simultaneous determination
of Fluticasone propionate and Azelastine hydrochloride in the presence of
pharmaceutical dosage form additives. Spectrochim Acta A Mol Biomol Spectrosc.
2016 May 5;160:50-57. doi: 10.1016/j.saa.2016.02.010. Epub 2016 Feb 18. PubMed
PMID: 26921606.

5: Klimek L, Bousquet J, Price D. Safety evaluation of MP29-02 (a novel
intranasal formulation of azelastine hydrochloride and fluticasone propionate)
for allergic rhinitis. Expert Opin Drug Saf. 2016 Jan;15(1):117-29. doi:
10.1517/14740338.2016.1122755. Epub 2015 Dec 23. Review. PubMed PMID: 26581312.

6: Ridolo E, Montagni M, Melli V, Bonzano L, Incorvaia C, Canonica GW. A role for
the intranasal formulation of azelastine hydrochloride/fluticasone propionate in
the treatment of allergic rhinitis. Ther Deliv. 2015;6(6):653-9. doi:
10.4155/tde.15.7. Epub 2015 Apr 27. Review. PubMed PMID: 25913181.

7: Bousquet J, Bachert C, Bernstein J, Canonica GW, Carr W, Dahl R, Demoly P,
Devillier P, Hellings P, Fokkens W, Klimek L, Lieberman P, Meltzer E, Price D,
Ryan D, Wahn U. Advances in pharmacotherapy for the treatment of allergic
rhinitis; MP29-02 (a novel formulation of azelastine hydrochloride and
fluticasone propionate in an advanced delivery system) fills the gaps. Expert
Opin Pharmacother. 2015 Apr;16(6):913-28. doi: 10.1517/14656566.2015.1020789.
Epub 2015 Mar 7. Review. PubMed PMID: 25747125.

8: Harrow B, Hofmeister J, Gever LN, Karafilidis J, Lacey MJ, Scheibling CM,
Schneider JE. Can Improved Treatment of Allergic Rhinitis Improve Workplace
Productivity? The Role of Intranasal Formulation of Azelastine Hydrochloride and
Fluticasone Propionate (Dymista). Value Health. 2014 Nov;17(7):A598. doi:
10.1016/j.jval.2014.08.2069. Epub 2014 Oct 26. PubMed PMID: 27202061.

9: Fu LL, Liu J, Chen Y, Wang FT, Wen X, Liu HQ, Wang MY, Ouyang L, Huang J, Bao
JK, Wei YQ. In silico analysis and experimental validation of azelastine
hydrochloride (N4) targeting sodium taurocholate co-transporting polypeptide
(NTCP) in HBV therapy. Cell Prolif. 2014 Aug;47(4):326-35. doi:
10.1111/cpr.12117. Epub 2014 Jun 26. Erratum in: Cell Prolif. 2014 Dec;47(6):624.
PubMed PMID: 24965018.

10: Berger WE, Shah S, Lieberman P, Hadley J, Price D, Munzel U, Bhatia S.
Long-term, randomized safety study of MP29-02 (a novel intranasal formulation of
azelastine hydrochloride and fluticasone propionate in an advanced delivery
system) in subjects with chronic rhinitis. J Allergy Clin Immunol Pract. 2014
Mar-Apr;2(2):179-85. doi: 10.1016/j.jaip.2013.09.019. Epub 2014 Jan 1. PubMed
PMID: 24607046.