Detail of "202189-78-4"

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In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist

All Rights Reserved. In vivo pharmacological characterisation of bilastine, a potent and selective histamine H1 receptor antagonist. Corcostegui, Reyes; Labeaga, Luis; Innerarity, Ana; Berisa, Agustin; Orjales, Aurelio (Department of Research, FAES FARMA, S.A., Leioa, Spain). Drugs in R&D, 7(4), 219-231 (English) 2006 Adis International Ltd.Chemicals with cas numbers 202189-78-4 and 83881-51-0 also play role. CODEN: DRDDFD. ISSN: 1174-5886. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Objective: We set out to establish the in vivo histamine H1 receptor antagonistic (antihistaminic) and antiallergic properties of bilastine. Methods: In vivo antihistaminic activity expts. consisted of measurement of inhibition of increase in capillary permeability and redn. in microvascular extravasation and bronchospasm in rats and guinea pigs induced by histamine and other inflammatory mediators; and protection against lethality induced by histamine and other inflammatory mediators in rats. In vivo antiallergic activity expts. consisted of measurement of passive and active cutaneous anaphylactic reactions as well as type III and type IV allergic reactions in sensitized rodents. Results: In the in vivo antihistaminic activity expts., bilastine was shown to have a pos. effect, similar to that of cetirizine and more potent than that of fexofenadine. The results of the in vivo antiallergic activity expts. showed that the properties of bilastine in this setting are similar to those obsd. for cetirizine and superior to fexofenadine in the model of passive cutaneous anaphylactic reaction. When active cutaneous anaphylactic reaction expts. were conducted, bilastine showed significant activity, less potent than that obsd. with cetirizine but superior to that of fexofenadine. Evaluation of the type III allergic reaction showed that of the antihistamines only bilastine was able to inhibit edema in sensitized mice, although its effect in this respect was much less potent than that obsd. with dexamethasone. In terms of the type IV allergic reaction, neither bilastine, cetirizine nor fexofenadine significantly modified the effect caused by oxazolone. Conclusions: The results of our in vivo preclin. studies corroborate those obtained from previously conducted in vitro expts. of bilastine, and provide evidence that bilastine possesses antihistaminic as well as antiallergic properties, with similar potency to cetirizine and superior potency to fexofenadine. .