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CAS 202189-78-4 Bilastine 202189-78-4
Bilastine, a potent and selective histamine H1 receptor antagonist, was approved in Europe in 2010 for the treatment of allergic rhinoconjunctivitis (AR) and urticaria (hives or skin rash). The original synthesis of bilastine involves alkylation of 2-piperidinyl-1H-benzimidazole with a phenethyltosylate, the para position of which is substituted with a dimethyloxazoline moiety serving as a masked carboxylic acid group. Alkylation of the benzimidazole nitrogen with 2-chloroethyl ethyl ethers followed by unmasking of the oxazoline moiety with sulfuric acid provided bilastine.
In two major clinical trials, bilastine was effective at relieving allergic rhinitis as assessed by measuring the severity of nasal (obstruction, rhinorrhea, itching, sneezing) and nonnasal (ocular itching, tearing, ocular redness, itching of ears, and/or palate) symptoms.
UsesBilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
UsesLabelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
Product information
Product Name:Bilastine
CAS:202189-78-4
MF:C28H37N3O3
MW:463.61
EINECS:
Mol File:202189-78-4.mol
Melting point:202 °C
Boiling point:639.1±55.0 °C(Predicted)
Density 1.16±0.1 g/cm3(Predicted)
pka4.40±0.10(Predicted)
Description
Bilastine, a potent and selective histamine H1 receptor antagonist, was approved in Europe in 2010 for the treatment of allergic rhinoconjunctivitis (AR) and urticaria (hives or skin rash). The original synthesis of bilastine involves alkylation of 2-piperidinyl-1H-benzimidazole with a phenethyltosylate, the para position of which is substituted with a dimethyloxazoline moiety serving as a masked carboxylic acid group. Alkylation of the benzimidazole nitrogen with 2-chloroethyl ethyl ethers followed by unmasking of the oxazoline moiety with sulfuric acid provided bilastine.
In two major clinical trials, bilastine was effective at relieving allergic rhinitis as assessed by measuring the severity of nasal (obstruction, rhinorrhea, itching, sneezing) and nonnasal (ocular itching, tearing, ocular redness, itching of ears, and/or palate) symptoms.
UsesBilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
UsesLabelled Bilastine. It is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
Company profile
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