product name Desloratadine
Description: Desloratadine (also known as SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM. 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.
References: Eur J Pharmacol. 1999 Jun 18;374(2):249-54; J Allergy Clin Immunol. 2001 Apr;107(4):751-62.
310.82
Formula
C19H19ClN2
CAS No.
100643-71-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 26 mg/mL (83.6 mM)
Water: <1 mg/mL
Ethanol: 62 mg/mL (199.5 mM)
Solubility (In vivo)
30% Propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
Synonyms
SCH-34117, NSC 675447
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427899
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
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| 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 |
| Animal model | Male guinea-pigs |
| Formulation & Dosage | Dissolved in 20% polyethylene glycol-300; 10 mg/kg; s.c. injection |
| References | Eur J Pharmacol. 1999 Jun 18;374(2):249-54; J Allergy Clin Immunol. 2001 Apr;107(4):751-62. |
