Bepotastine Besilate , 98% , 190786-44-8

CAS NO.：190786-44-8

Empirical Formula: C27H31ClN2O6S

Molecular Weight: 547.07

MDL number: MFCD01938491

EINECS: 1806241-263-5

PRODUCT Properties

• Melting point: 161-163°
• alpha: D20 +6.0° (c = 5 in methanol)
• storage temp.: Inert atmosphere,Room Temperature
• solubility: DMSO (Slightly, Heated), Methanol (Slightly, Heated)
• form: Solid
• color: White to Light Beige
• optical activity: [α]/D 4.5 to 6.5°, c =1 in methanol
• Stability: Hygroscopic

Description and Uses

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 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).

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302-H315-H319-H335
• Precautionary statements: P261-P305+P351+P338