Mizolastine

Base Information

• Chemical Name: Mizolastine
• CAS No.: 108612-45-9
• Molecular Formula: C24H25FN6O
• Molecular Weight: 432.501
• Hs Code.: 2933990090
• European Community (EC) Number: 620-519-1
• UNII: 244O1F90NA
• DSSTox Substance ID: DTXSID5046801
• Nikkaji Number: J546.910D
• Wikipedia: Mizolastine
• Wikidata: Q417830
• NCI Thesaurus Code: C66171
• Pharos Ligand ID: STJQJDUR9UZN
• Metabolomics Workbench ID: 153497
• ChEMBL ID: CHEMBL94454
• Mol file: 108612-45-9.mol

Synonyms:Mistalin;Mistamine;mizolastine;Mizolen;Mizollen;SL 85.0324;SL-85.0324;Zolim;Zolistan

Chemical Property of Mizolastine

Chemical Property:

• Melting Point: 217°
• Refractive Index: 1.682
• PKA: 9.73±0.40(Predicted)
• PSA: 70.05000
• Density: 1.34 g/cm³
• LogP: 3.47720
• Storage Temp.: Refrigerator
• Solubility.: Chloroform (Slightly, Heated), DMSO, Methanol (Slightly, Heated)
• XLogP3: 3.2
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 5
• Rotatable Bond Count: 5
• Exact Mass: 432.20738760
• Heavy Atom Count: 32
• Complexity: 728

Purity/Quality:

99% ^*data from raw suppliers

Mizolastine ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Canonical SMILES: CN(C1CCN(CC1)C2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)F)C5=NC=CC(=O)N5
• Recent ClinicalTrials: A Bioequivalence Study of Domestic (Made in China) and Imported Mizolastine Tablets in Healthy Volunteers
• Description: Mizolastine was marketed in Germany and Switzerland as Mizollen for the symptomatic relief of seasonal and perennial allergic rhinoconjunctivitis and urticaria. Mizolastine is a new long-acting, orally active antihistaminic agent with a rapid onset of action ; the two most recent H1 antagonists launched were fexofenadine, metabolite of terfenadine (Sepracor, 1996) and Olopatadine (Kyowa Hakko, 1997). Mizolastine can be prepared in 2 steps from 2-chloro 1- (4-fluorobenzyl)benzimidazole by successive condensations of appropriate amine and thioether. Mizolastine selectively blocks the peripheral H1 receptors (but not the serotonergic, noradrenergic, muscarinic receptors) with a minimal occupancy of brain receptors, and therefore does not elicit any sedative effects. Moreover, Mizolastine does not produce cardiac rhythm disorders which have been associated with certain non-sedating antihistamines in humans.
• Uses: A highly selective histamine H1-receptor antagonist (with no anticholinergic, antiadrenergic, or antiserotonin activity) for use in the treatment of allergic disorders, especially rhinitis and urticaria. Allergic rhinitis;Blocking H1 receptors
• Clinical Use: Antihistamine: Symptomatic relief of allergy, e.g. hayfever, urticaria
• Drug interactions: Potentially hazardous interactions with other drugs Anti-arrhythmics: increased risk of ventricular arrhythmias - avoid with amiodarone, disopyramide, flecainide, mexiletine, procainamide and propafenone. Antibacterials: metabolism possibly inhibited by macrolides - avoid; increased risk of ventricular arrhythmias with moxifloxacin - avoid. Antidepressants: risk of ventricular arrhythmias with citalopram and escitalopram - avoid. Antifungals: metabolism inhibited by itraconazole and ketoconazole and possibly imidazoles - avoid. Antimalarials: avoid with piperaquine with artenimol. Antivirals: concentration possibly increased by ritonavir; increased risk of ventricular arrhythmias with saquinavir - avoid. Beta-blockers: increased risk of ventricular arrhythmias with sotalol - avoid. Ciclosporin: use with caution due to inhibition of ciclosporin metabolism. Cytotoxics: possible increased risk of ventricular arrhythmias with vandetanib. Avoid concomitant treatment with any drug that could prolong QT interval. Caution with drugs that inhibit cytochrome P450 enzymes (may elevate mizolastine levels)