Azelastine HCl - CAS 79307-93-0
Catalog number: B0084-098591
Category: Inhibitor
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Molecular Formula:
C22H25Cl2N3O
Molecular Weight:
418.36
COA:
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Targets:
Histamine Receptor
Description:
Azelastine HCl is a potent, second-generation, selective, histamine antagonist. It inhibits histamine via competing with histamine for the H1 receptor.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-098591 1 g $199 In stock
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Brife Description:
histamine antagonist
Purity:
>98%
Synonyms:
ZELASTINE HYDROCHLORIDE; AC1Q1SYE; HYDROGEN AZELASTINE CHLORIDE; AKOS026749829; DR002552
MSDS:
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Application:
histamine antagonist
InChIKey:
YEJAJYAHJQIWNU-UHFFFAOYSA-N
InChI:
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
Canonical SMILES:
[H+].CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.[Cl-]
1.Lack of effect of azelastine and ketoconazole coadministration on electrocardiographic parameters in healthy volunteers.
Morganroth J1, Lyness WH, Perhach JL, Mather GG, Harr JE, Trager WF, Levy RH, Rosenberg A. J Clin Pharmacol. 1997 Nov;37(11):1065-72.
Azelastine, an antihistamine with additional pharmacologic properties, was evaluated for a possible influence on pharmacokinetic and electrocardiographic parameters due to its coadministration with CYP3A4 inhibitor ketoconazole (200 mg every 12 hrs). Twelve volunteers entered this three-period, open-label study. Electrocardiographic parameters (PR, QRS and QTc intervals and U-wave morphology) were monitored after 14 days of azelastine HCl (4.4 mg every 12 hrs), after 7 days of either azelastine/ketoconazole or azelastine/placebo, and after a 21-day washout period, which was then followed by a 7-day administration of ketoconazole alone. None of the treatments resulted in meaningful alterations of electrocardiographic variables. Pharmacokinetic parameters could not be estimated because ketoconazole metabolites interfered with azelastine assay procedures. In vitro tests with human liver microsomes were used to characterize azelastine's inhibition spectrum.
2.High performance liquid chromatographic determination of azelastine and desmethylazelastine in guinea pig plasma and lung tissue.
Langevin CN1, Pivonka J, Wichmann JK, Kucharczyk N, Sofia RD. Biomed Chromatogr. 1993 Jan-Feb;7(1):7-11.
Analytical methods have been developed for the simultaneous quantitation of azelastine (AZ) and desmethylazelastine (DAZ) in guinea pig plasma and lung tissue. The methods require a 1.00 mL plasma sample and a minimum 0.100 g lung sample. Both methods employ liquid/liquid organic extraction and back-extraction into dilute acid. Quantitation is performed by high performance liquid chromatography on a 2 x 250 mm 5 microns Hypersil CPS column using fluorescence detection. The linear quantitative ranges for AZ.HCl and DAZ.HBr in plasma are 0.156-160 ng/mL and 0.313-160 ng/mL, respectively. The linear quantitative ranges for AZ.HCl and DAZ.HBr in lung tissue are 0.039-20 micrograms/g for both.
3.Investigation on the efficacy and tolerance of azelastine (HCL) nasal spray versus ebastine tablets in patients with seasonal allergic rhinit
Conde Hernández J1, Palma Aguilar JL, Delgado Romero J. Allergol Immunopathol (Madr). 1995 Mar-Apr;23(2):51-7.
We compared the efficacy and tolerance of Azelastine nasal spray (0.14 mg in each nostril twice a day) versus Ebastine tablets (10 mg) as a single night dose in a Phase IV open, randomized, parallel-group clinical trial lasting 14 days, conducted with 63 patients diagnosed of seasonal allergic rhinitis. The symptoms assessed before and after the treatment period were: sneezing, nasal pruritus, rhinorrhea, nasal obstruction, conjunctival erythema, eye pruritus, eye watering, photophobia, pharyngeal pruritus and cough. Each symptom was rated by the patients according to a 4-point scale: absent: 0, mild: 1, moderate: 2, and severe: 3. The score required to be included in the study was 8 or above. In addition, the resistance of nasal fossae was assessed, before and after the treatment, by active anterior rhinomanometry, as well as the appearance of adverse events. Both drugs were equally effective both in the control of symptoms and in decreasing the airway resistance and no statistically significant differences were observed in the variables tested in both groups.
4.[The problem of recurrence of rhino-sinusal polyposis: pilot trial with locally administered azelastine HCL in the prevention of relapses].
Bussi M1, Carlevato MT, Majore L, Battaglio S, Napoli P, Cortesina G. Acta Otorhinolaryngol Ital. 1995 Apr;15(2):101-6.
Recurrent nasal polyposis is one of the most common unsolved problem in clinical rhinology. In the last few years a great number of histopathological, immunohistochemical and immunological studies on nasal polyps have been carried out by several Authors. Notwithstanding this, the aetiology of these formations still remains unknown. Many data suggest that the presence of polyps is the result of various inflammatory, allergic and pseudo-allergic processes which finally lead to the formation of the oedema constitutive of the polyp itself. In the present report a preliminary trial was carried out in order to evaluate the possibility of preventing recurrences by means of a locally administered anti-H1 receptors drug (Azelastine HCl). In the reported first phase of the study 10 allergic patients with bilateral polyposis were evaluated. Attention was given to the anti-edemigen activity of the drug, as well as to its influence on the local production of Secretory IgA, 7SIgA and albumines.
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CAS 79307-93-0 Azelastine HCl

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