Ebastine

Catalog No.S4262

Ebastine Chemical Structure

Molecular Weight(MW): 469.66

Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.

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Biological Activity

Description Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
Targets
Histamine H1 receptor [1]
In vitro

Ebastine at concentrations approximating those found in plasma under certain conditions suppresses in a voltage-independent manner the I(Kr) (Kd = 0.14 μM, maximum block 74%) more effectively than the slowly delayed rectifier K+ current (I(Ks)) (Kd = 0.8 μM, maximum block 60%) in guinea pig ventricular myocytes. Ebastine also suppresses IKr in HERG-expressing X. laevis oocytes with the K d value of 0.3 μM and a maximal block of 46% at 3 μM. Ebastine produces negligible effect on rat transient K+ current at concentrations of <100 nM. [1] Ebastine is shown to block the release of anti-IgE-induced prostaglandin D2 (PGD2) and leukotriene C4/D4 from human nasal polyp cells (IC30 values of 2.57 and 9.6 μM, respectively) and to inhibit the release of cytokines. [2] Ebastine is a novel histamine H1 receptor antagonist that combines potency with a rapid onset (fast absorption) and long duration (slow elimination) of action, at least partially mediated via the formation of an acid metabolite (carebastine) that is even more potent as an antihistamine. Ebastine has negligible activity against acetylcholine (no atropine-like adverse effects on secretions and visual accommodation) and only poorly penetrates the blood-brain barrier (no sedative adverse effects). Ebastine is without effects on the central nervous and cardiovascular systems, even after oral administration of high doses, and does not interact pharmacologically with a wide range of other drugs covering most areas of potential coadministration. Ebastine shows clear selectivity for histamine H1 as opposed to H2 receptors, has moderate activity against other potential mediators of allergic phenomena such as leukotriene C4 and platelet-activating factor, and is clearly effective against anaphylactic reactions resulting from exposure of suitably sensitised tissues or animals to antigen. [3]

Protocol

Solubility (25°C)

In vitro Ethanol 11 mg/mL (23.42 mM)
DMSO 4 mg/mL warmed (8.51 mM)
Water 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 469.66
Formula

C32H39NO2

CAS No. 90729-43-4
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01908465 Recruiting Irritable Bowel Syndrome (IBS) Katholieke Universiteit Leuven November 2013 Phase 4
NCT01940393 Completed Urticaria Grupo de Alergología Clínica y Experimental August 2013 Phase 4
NCT01144832 Completed Irritable Bowel Syndrome Katholieke Universiteit Leuven October 2009 Phase 4

Tech Support

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.

Handling Instructions

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID