CAS 202189-78-4|bilastine

Introduction：Basic information about CAS 202189-78-4|bilastine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. bilastine BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

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	/	Flash Point	340.3±31.5 °C

Names

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

bilastine BiologicalActivity

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	Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology
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.

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

Signaling Pathways >>GPCR/G Protein >>Histamine ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch Areas >>Inflammation/Immunology

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
InChIKey	ACCMWZWAEFYUGZ-UHFFFAOYSA-N
SMILES	CCOCCn1c(C2CCN(CCc3ccc(C(C)(C)C(=O)O)cc3)CC2)nc2ccccc21

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

Recommended......