bilastine

Modify Date: 2025-08-21 22:54:51

bilastine Structure
bilastine structure
Common Name bilastine
CAS Number 202189-78-4 Molecular Weight 463.612
Density 1.2±0.1 g/cm3 Boiling Point 639.1±55.0 °C at 760 mmHg
Molecular Formula C28H37N3O3 Melting Point 202 °C
MSDS N/A Flash Point 340.3±31.5 °C

 Use of bilastine


Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].

 Names

Name 2-[4-[2-[4-[1-(2-ethoxyethyl)benzimidazol-2-yl]piperidin-1-yl]ethyl]phenyl]-2-methylpropanoic acid
Synonym More Synonyms

 bilastine Biological Activity

Description Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria. Target: Histamine H1 ReceptorBilastine binds to histamine H1-receptors as indicated by its displacement of [3H]-pyrilamine from H1-receptors expressed in guinea-pig cerebellum and human embryonic kidney (HEK) cell lines. The studies conducted on guinea-pig smooth muscle demonstrated the capability of bilastine to antagonise H1-receptors. Bilastine is selective for histamine H1-receptors as shown in receptor-binding screening conducted to determine the binding capacity of bilastine to 30 different receptors [1]. Bilastine distribution has an apparent volume of distribution of 1.29 L/kg, and has an elimination half-life of 14.5 h and plasma protein binding of 84-90% [2].
Related Catalog
References

[1]. Corcostegui, R., et al., Preclinical pharmacology of bilastine, a new selective histamine H1 receptor antagonist: receptor selectivity and in vitro antihistaminic activity. Drugs R D, 2005. 6(6): p. 371-84.

[2]. Jauregizar, N., et al., Pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effect of bilastine. Clin Pharmacokinet, 2009. 48(8): p. 543-54.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 639.1±55.0 °C at 760 mmHg
Melting Point 202 °C
Molecular Formula C28H37N3O3
Molecular Weight 463.612
Flash Point 340.3±31.5 °C
Exact Mass 463.283478
PSA 67.59000
LogP 5.06
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.594

 Synonyms

Benzeneacetic acid, 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl]ethyl]-α,α-dimethyl-
Ilaxten
2-[4-(2-{4-[1-(2-Ethoxyethyl)-1H-benzimidazol-2-yl]-1-piperidinyl}ethyl)phenyl]-2-methylpropanoic acid
Bilaxten
Bilastine (INN)
bilastine
Bilatex
2-[4-(2-{4-[1-(2-ethoxyethyl)-1h-benzimidazol-2-yl]piperidin-1-yl}ethyl)phenyl]-2-methylpropanoic acid
Bilasten
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