Desloratadine

Catalog No.S4012 Synonyms: SCH-34117, NSC 675447

Desloratadine Chemical Structure

Molecular Weight(MW): 310.82

Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

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In DMSO USD 140 In stock
USD 110 In stock
USD 370 In stock
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Biological Activity

Description Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
Features Desloratadine is the active metabolite of loratadine.
Targets
Histamine H1 receptor [1]
51 nM
In vitro

Desloratadine is a competitive antagonist of carbachol-induced contractions in isolated rabbit iris smooth muscle with pA2 of 6.67. [1] 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. [2] 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. [3] [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. [4]

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. [1] 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. [2] 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. [5]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Male guinea-pigs
  • Formulation: 20% polyethylene glycol-300
  • Dosages: 10 mg/kg
  • Administration: Subcutaneous
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 62 mg/mL (199.47 mM)
DMSO 26 mg/mL (83.64 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* 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 310.82
Formula

C19H19ClN2

CAS No. 100643-71-8
Storage powder
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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Histamine Receptor Signaling Pathway Map

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