Home Neuronal Signaling Histamine Receptor antagonist Bilastine

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Bilastine Histamine Receptor antagonist

Cat.No.S3721

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

Chemical Structure

Molecular Weight: 463.61

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Quality Control

Batch: S372101 4-Methylpyridine]29 mg/mL]false]DMSO]1 mg/mL]false]Water]Insoluble]false Purity: 99.87%
99.87

Solubility

In vitro
Batch:

4-Methylpyridine : 29 mg/mL

DMSO : 1 mg/mL (2.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 463.61 Formula

C28H37N3O3

 Storage (From the date of receipt)
CAS No. 202189-78-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCOCCN1C2=CC=CC=C2N=C1C3CCN(CC3)CCC4=CC=C(C=C4)C(C)(C)C(=O)O

Mechanism of Action

Targets/IC50/Ki
H1 receptor
(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. This compound is lack of significant antagonism against serotonin, bradykinin, leukotriene D4, calcium, muscarinic M3-receptors, α1-adrenoceptors, β2-adrenoceptors, and H2- and H3- receptors.
In vivo
Bilastine is efficacious in all nasal symptoms including obstruction and in eye symptoms in patients with allergic rhinoconjunctivitis. This compound is well tolerated. In the fasting state it 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02213367 Completed
Chronic Urticaria
Charite University Berlin Germany
 July 2014 Phase 3
NCT01271075 Completed
Cold Contact Urticaria
Charite University Berlin Germany|Faes Farma S.A.
 September 2010 Phase 2|Phase 3
NCT01124123 Completed
Healthy
Faes Farma S.A.
 May 2010 Phase 1
NCT01081574 Completed
Allergic Rhinoconjunctivitis|Chronic Urticaria
Faes Farma S.A.
 January 2010 Phase 1|Phase 2

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