01
Bepotastine Besilate 190786-44-8
Product Specification
| Appearance: | white to light-yellow crystalline powder |
| Specific Rotation（5%solution in methanol): | +4.0°～+8.0° |
| Identification : | UV、HPLC |
| Chromatographic purity (% area normalization,by HPLC)： | Not less than 99.0%、Maximum single impurity:NMT 0.5% |
| Optical isomer： | Not more than 1.0% |
| Loss on Drying(at 105℃ till constant weight)： | Not more than 1.0% |
| Residue on Ignition ： | Not more than 0.1% |
| Heavy Metals： | Not more than 20ppm |
| Assay (on dried basis,by titration)： | Not less than 98.5% |
description1
PRODUCT DESCRIPTION
Betotastine was introduced in Japan for the treatment of allergic rhinitis. This structurally-related derivative of chlorpheniramine and ebastine is prepared by condensation of optically-resolved 4-[1-(4-chlorophenyl)-1-(2-pyridyl)-methoxy]piperidine with ethyl 4-bromobutyrate followed by ester hydrolysis. Betotastine is the seventh marketed non-sedating histamine H1 antagonist. Its very low sedative side effect is due to very poor penetration in the central nervous system. Besides its potent and long-acting activity in models of allergic rhinitis, betotastine was also shown to act as a PAF antagonist and inhibit LTD4 in tracheal smooth muscle and ileum, IL-5 production by human peripheral blood mononuclear cells as well as eosinophil infiltration in the airway and peripheral blood. As a consequence, it is currently being developed against other allergic and respiratory disorders.
Bepotastine is an antagonist of the histamine H1 receptor that is selective over H3, α1-, α2-, and β-adrenergic, dopamine D2long, serotonin 5-HT2, muscarinic acetylcholine, and benzodiazepine receptors. It reduces dye leakage from the nasal passages of rats acutely sensitized to an antigen (ED50 = 0.03 mg/kg) and inhibits histamine-induced bronchoconstriction in the anesthetized dog (ED50 = 3.2 μg/kg). Bepotastine prevents conjunctival vascular hyperpermeability in a guinea pig model of conjunctivitis in a dose-dependent manner. Formulations containing bepotastine have been used in the treatment of itching associated with allergic conjunctivitis.
Bepotastine is a histamine H1 receptor anatagonist. Bepotastine suppresses some allergic inflammatory processes such as allergic rhinitis, chronic urticaria or pruritus associated with skin conditions (eczema/dermatitis, prurigo or pruritus cutaneus).