Desloratadine

Modify Date: 2024-01-01 23:46:52

Desloratadine Structure
Desloratadine structure
 Common Name Desloratadine
CAS Number 100643-71-8 Molecular Weight 310.821
Density 1.2±0.1 g/cm3 Boiling Point 467.9±45.0 °C at 760 mmHg
Molecular Formula C19H19ClN2 Melting Point 150-151°C
MSDS Chinese USA Flash Point 236.8±28.7 °C

 Use of Desloratadine


Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.Target: Histamine H1 ReceptorDesloratadine 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 [1]. 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 [2]. [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 [3].

 Names

Name desloratadine
Synonym More Synonyms

 Desloratadine Biological Activity

Description Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.Target: Histamine H1 ReceptorDesloratadine 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 [1]. 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 [2]. [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 [3].
Related Catalog
References

[1]. Geha, R.S. and E.O. Meltzer, Desloratadine: A new, nonsedating, oral antihistamine. J Allergy Clin Immunol, 2001. 107(4): p. 751-62.

[2]. Schroeder, J.T., et al., Inhibition of cytokine generation and mediator release by human basophils treated with desloratadine. Clin Exp Allergy, 2001. 31(9): p. 1369-77.

[3]. Anthes, J.C., et al., Biochemical characterization of desloratadine, a potent antagonist of the human histamine H(1) receptor. Eur J Pharmacol, 2002. 449(3): p. 229-37.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 467.9±45.0 °C at 760 mmHg
Melting Point 150-151°C
Molecular Formula C19H19ClN2
Molecular Weight 310.821
Flash Point 236.8±28.7 °C
Exact Mass 310.123688
PSA 24.92000
LogP 6.77
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.626
Storage condition 2-8°C

 Safety Information

Hazard Codes Xi
Risk Phrases R11:Highly Flammable.
Safety Phrases S16-S23-S36/37/39
RIDADR 1993

 Synthetic Route

 Articles8

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 Synonyms

8-Chlor-11-piperidin-4-yliden-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin
8-Chloro-6,11-dihydro-11-(4-piperidinylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
UNII-FVF865388R
AzoMyr
5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro-11-(4-piperidinylidene)-
DESLORATIDINE
MFCD00871949
Opulis
Desloratadine
8-Chloro-11-(4-piperidinylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Allex
Descarboethoxyoratidine
Neoclarityn
Aerius
Sch34117
descarboethoxyloratadine
8-chloro-11-(piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Clarinex
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Desloratadine-d9
1795024-82-6
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381727-29-3
Desloratadine-d5
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Iso Desloratadine
183198-49-4
5-OH desloratadine
117811-12-8
6-OH desloratadine
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