Bilastine

Catalog No.S3721

Bilastine Chemical Structure

Molecular Weight(MW): 463.61

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.

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Biological Activity

Description Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
Targets
H1 receptor [2]
(in guinea-pig cerebellum)
44.15 nM(Ki)
In vitro

Bilastine has a high specific affinity for the H1-receptor but it has no or very low affinity for 30 other tested receptors[1]. It is lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3- receptors[2].

In vivo Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms in patients with allergic rhinoconjunctivitis. Bilastine is well tolerated. In the fasting state bilastine is quickly absorbed, but the absorption is slowed when it is taken with food or fruit juice. In vivo studies in rats have demonstrated reduction in histamine-stimulated smooth muscular contraction, bronchospasms, endothelial permeability, and microvascular extravasation[1].

Protocol

Solubility (25°C)

In vitro DMSO 1 mg/mL (2.15 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 463.61
Formula

C28H37N3O3

CAS No. 202189-78-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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