Catalog No.S4012 Synonyms: SCH-34117, NSC 675447
Molecular Weight(MW): 310.82
Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
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Choose Selective Histamine Receptor Inhibitors
|Description||Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.|
|Features||Desloratadine is the active metabolite of loratadine.|
Desloratadine is a competitive antagonist of carbachol-induced contractions in isolated rabbit iris smooth muscle with pA2 of 6.67.  Desloratadine binds to the human H1 receptor with Ki value of 0.87 nM in displacing tritiated mepyramine. Desloratadine (100 nM to 10 μM) inhibits both IgE-mediated and non–IgE-mediated generation of the cytokines IL-4 and IL-13 by human basophils. Desloratadine (300 nM to 100 μM) inhibits both IgE and non–IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μM to 10 μM) is also shown to inhibit platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion in eosinophils obtained from patients with allergic rhinitis or allergic asthma.  Desloratadine (1 μM-10 μM) dose-dependently inhibits the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μM-10 μM) dose-dependently inhibits IL-13 secretion from basophils activated with IL-3 and PMA from human basophils. Desloratadine (10 μM) pretreatment results in a substantial decrease of the induced cytokine message in cultured basophils. Desloratadine (10 μM) pretreatment causes approximately an 80% reduction in the IL-4 message accumulated with anti-IgE activation in cultured basophils. Desloratadine (10 μM) also inhibits the histamine and IL-4 protein secreted into the supernatants of cultured basophils.  [3H]Desloratadine binds to the human histamine H1 receptor expressed in CHO cells with Kd of 1.1 nM. Desloratadine is 52, 57, 194, and 153 times more potent than cetirizine, ebastine, fexofenadine, and loratadine, respectively, in competition-binding studies. 
|In vivo||Desloratadine (1 mg/mL, 3 mg/mL and 10 mg/mL) induces a dose-dependent and long lasting mydriasis in the guinea-pig in vivo.  Desloratadine inhibits histamine-induced paw edema with ED50 of 0.15 mg/kg in mice. Desloratadine inhibits an increase in microvascular permeability in response to a histamine challenge to the upper airway of guinea pigs with ED50 of 0.9 μg.  Desloratadine (5 mg/kg) causes inhibition of oxotremorine-induced tremor by disrupting blood-brain barrier in conscious mice. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. Desloratadine (1.0 mg/kg) significantly inhibits oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) decreases in dP/dt indicated by a shift in the dose-response curve to the right in the pithed rat. |
-  Cardelús I, et al. Eur J Pharmacol, 1999, 374(2), 249-25
-  Geha RS, et al. J Allergy Clin Immunol, 2001, 107(4), 751-762.
-  Schroeder JT, et al. Clin Exp Allergy, 2001, 31(9), 1369-1377.
|In vitro||Ethanol||62 mg/mL (199.47 mM)|
|DMSO||26 mg/mL (83.64 mM)|
|In vivo||Add solvents to the product individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
* 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.
|Synonyms||SCH-34117, NSC 675447|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02904304||Not yet recruiting||Cold||Ache Laboratorios Farmaceuticos S.A.||January 2018||Phase 3|
|NCT02646020||Active, not recruiting||Non-small Cell Lung Cancer||Sun Yat-sen University||December 2015||Phase 2|
|NCT02320396||Completed||Seasonal Allergic Rhinitis||Merck Sharp & Dohme Corp.||January 2015||Phase 3|
|NCT01529242||Recruiting||Cutaneous Hypersensitivity||EMS||February 2014||Phase 3|
|NCT01529229||Completed||Allergic Rhinitis||EMS||November 2013||Phase 3|
|NCT01985789||Completed||Asthma||Don Cockcroft|University of Saskatchewan||November 2013||Phase 4|
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