Mizolastine CAS NO.108612-45-9

Product Name:    Mizolastine
Synonyms:    4(1h)-pyrimidinone,2-((1-(1-((4-fluorophenyl)methyl)-1h-benzimidazol-2-yl)-4-p;iperidinyl)methylamino)-;2-[[1-[1-[(4-fluorophenyl)methyl]benzoimidazol-2-yl]-4-piperidyl]-methyl-amino]-3h-pyrimidin-4-one;MIZOLASTINE;2-[[1-[1-[(4-fluorophenyl)methyl]-1H-benzimidazol-2-yl]-4-piperidinyl]methylamino]-4(1H)-pyrimidinone;Mizolastine HCl;2-[[1-[1-(4-fluorobenzyl)benzimidazol-2-yl]-4-piperidyl]-methyl-amino]-1H-pyrimidin-6-one;2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methyl-amino]-1H-pyrimidin-6-one
CAS:    108612-45-9
MF:    C24H25FN6O
MW:    432.49
EINECS:    1308068-626-2
Product Categories:    Other APIs;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;Antihistaminic;APIs
Mol File:    108612-45-9.mol

Melting point     217°
density     1.34±0.1 g/cm3(Predicted)
pka    9.73±0.40(Predicted)
Merck     14,6221

Abstract    Mizolastine (Mizollen) is a non-sedating antihistamine. It blocks H1 receptors and is commonly fast-acting. It does not prevent the actual release of histamine from mast cells, just prevents it binding to receptors.
Medical efficacy    Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H(1) receptors. Mizolastine has demonstrated antiallergic effects in animals and healthy volunteers and anti-inflammatory activity in animal models. Double-blind trials
have shown mizolastine to be significantly more effective than placebo and as effective as other second generation antihistamine agents, such as loratadine or cetirizine, in the management of patients with perennial or seasonal allergic rhinitis and in patients with
chronic idiopathic urticaria.
It not only has a strong anti-histamine but also has inflammatory neurotransmitters inhibit action, such as inhibit the generation of leukotrienes, reduce edema. Thus in theory, mizolastine has both anti-histamine and anti-allergic effects. The role of anti-inflammatory activity, for the treatment of acute urticaria preferred drug, significantly the onset of action is faster than other antihistamines, and the medication can reduce the number of the wheal hours after 1-3 hours, itching abated, and maintain a long time, up to 24 hours.
At present, the clinical treatment is mainly used for the treatment of adults or children over 12 years of age suffering from urticaria and other skin allergy symptoms, seasonal allergic rhinitis (hay fever) and perennial allergic rhinitis.