| Name | Ebastine |
| Description | Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness. |
| In vivo | Compared to H2 receptors, Ebastine showed selectivity for histamine H1, moderate activity against other potential mediators of allergic phenomena such as leukotriene C4 and platelet-activating factor, and was apparently effective in targeting allergic reaction antigens induced by exposure of appropriately sensitized tissues or animals to allergies.Ebastine inhibited, in human nasal polyp cells, anti-IgE-induced prostaglandin D2 and leukotriene C4/D4 with IC30 of 2.57 μM and 9.6 μM, respectively, and inhibited cytokine release.Ebastine also inhibited hERG-expressing IKr in African Xenopus oocytes with a Kd value of 0.3 μM, with a maximal inhibition of 46% at 3 μM.Ebastine exerted a small effect on transient potassium currents in rats at a concentration of less than 100 nM. Ebastine had a small effect on the transient potassium current in rats at concentrations less than 100 nM. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 4.69 mg/mL (10 mM)
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| Keywords | Inhibitor | LAS-W090 | RP-64305 | antiallergic | urticaria | rhinitis | Histamine Receptor | antihistamine | idiopathic | RP 64305 | LAS-W-090 | inhibit | allergic | Ebastine |
| Inhibitors Related | Chlorphenesin | Meclizine dihydrochloride | Mirtazapine | Lidocaine | Famotidine | Mebhydrolin napadisylate | Amitriptyline hydrochloride | Alginic acid | Trazodone hydrochloride | Mianserin hydrochloride |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
