Home Neuronal Signaling Histamine Receptor antagonist Desloratadine For research use only.

Desloratadine

Synonyms: SCH-34117, NSC 675447

Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

Desloratadine Chemical Structure

Desloratadine Chemical Structure

CAS: 100643-71-8

Selleck's Desloratadine has been cited by 1 publication

Purity & Quality Control

Batch: S401201 Ethanol] 62 mg/mL] false] DMSO] 26 mg/mL] false] Water] Insoluble] false Purity: 99.98%
99.98

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Biological Activity

Description Desloratadine (SCH-34117, NSC 675447) 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
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
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]
Animal Research Animal Models Male guinea-pigs
Dosages 10 mg/kg
Administration Subcutaneous
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02904304 Suspended Cold Ache Laboratorios Farmaceuticos S.A. December 2020 Phase 3
NCT00761527 Completed Rhinitis Allergic Seasonal|Rhinitis Allergic Perennial|Urticaria Organon and Co March 2008 --

Chemical lnformation & Solubility

Molecular Weight 310.82 Formula

C19H19ClN2
CAS No. 100643-71-8 SDF Download Desloratadine SDF
Smiles C1CC2=C(C=CC(=C2)Cl)C(=C3CCNCC3)C4=C1C=CC=N4
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 62 mg/mL

DMSO : 26 mg/mL ( (83.64 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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