100643-71-8
desloratadine
CAS: 100643-71-8
Molecular Formula: C19H19ClN2
100643-71-8 - Names and Identifiers
| Name | desloratadine |
| Synonyms | AzoMyr Opulis Aerius NSC 675447 Neoclarityn desloratadine Desloratadine(Clarinex) Desloratadine for system suitability 8-chloro-11-(piperidin-4-ylidene)-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine 5H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 8-chloro-6,11-dihydro- 11-(4-piperidinylidene)- Loratadine Related Compound A (15 mg) (8-chloro-6,11-dihydro-11(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b] pyridine) |
| CAS | 100643-71-8 |
| EINECS | 638-878-8 |
| InChI | InChI=1/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2 |
| InChIKey | JAUOIFJMECXRGI-UHFFFAOYSA-N |
100643-71-8 - Physico-chemical Properties
| Molecular Formula | C19H19ClN2 |
| Molar Mass | 310.82 |
| Density | 1?+-.0.06 g/cm3(Predicted) |
| Melting Point | 150-151°C |
| Boling Point | 467.9±45.0 °C(Predicted) |
| Flash Point | 236.8°C |
| Solubility | DMSO: >10mg/mL |
| Vapor Presure | 6.25E-09mmHg at 25°C |
| Appearance | White-like powder |
| Color | White to Light orange to Yellow |
| Merck | 14,2922 |
| pKa | 10.27±0.20(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.625 |
| MDL | MFCD00871949 |
| Use | Respiratory and anti-allergic medications |
| In vitro study | Desloratadine is a competitive antagonist of Carbachol-induced contraction of isolated rabbit Iris smooth muscle with a 6.67 pa2. Desloratadine binds to the human H1 receptor with a Ki value of 0.87 nM in tritiated Mepyramine. Desloratadine (100 nM to 10 μm) inhibits IgE-mediated and non-IgE-mediated cytokine IL-4 and IL-13 production in human basophils. Desloratadine (300 nM to 100 μm) inhibits IgE-mediated and non-IgE-mediated histamine release from human peripheral blood basophils. Desloratadine (0.1 μm to 10 μm) in eosinophils taken from patients with allergic rhinitis or allergic asthma it inhibits platelet-activating factor-induced eosinophil chemotaxis and TNF-α-induced eosinophil adhesion. Desloratadine (1 μm -10 μm) dose-dependently inhibited the release of histamine and LTC4 from human basophils. Desloratadine (0.1 μm -10 μm) dose-dependently inhibited IL-13 secretion in basophils. Pretreatment with Desloratadine (10 μm) resulted in a large decrease in cytokines induced in cultured basophils. In cultured basophils, Desloratadine (10 μm) pretreatment caused an approximately 80% reduction in IL-4 and anti-IgE activation. Desloratadine (10 μm) also inhibited the secretion of histamine and IL-4 proteins into the supernatant of cultured basophils. [ |
| In vivo study | Desloratadine (1 mg/ml, 3 mg/mL and 10 mg/mL) induced dose-dependent and persistent pupil dilation in guinea pigs. Desloratadine inhibited histamine-induced paw swelling in mice with an ED50 of 0.15 mg/kg. Desloratadine inhibited the increase in vascular permeability caused by histamine invasion of the upper respiratory tract in guinea pigs with an ED50 of 0.9 μg. Desloratadine (5 mg/kg) inhibits oxytremorine-induced tumors by disrupting the blood-brain barrier in conscious mice. Desloratadine (1.0 mg/kg) significantly inhibited the oxotremorine-induced (0.00125 mg/kg, 0.0025 mg/kg, and 0.02 mg/kg) dP/dt reduction in rats with brain-destroyed spinal cord, indicated by a shift to the right of the dose-response curve. |
100643-71-8 - Risk and Safety
| WGK Germany | 3 |
| RTECS | DE8011000 |
| HS Code | 2933399090 |
100643-71-8 - Nature
Open Data Verified Data
white crystalline powder, odorless, bitter. Not easy to absorb moisture. The melting point was 150-151 °c. Soluble in chloroform, methanol, ethanol, soluble in dichloromethane, ethyl acetate, acetone, almost insoluble in water.
Last Update：2025-06-10 22:55:16
100643-71-8 - Preparation Method
Open Data Verified Data
loratadine was added to a solution of sodium hydroxide in ethanol and reacted under reflux. The product was extracted with glacial acetic acid and chloroform to obtain desloratadine acetate. This was dissolved in water, basified with dilute potassium carbonate solution and extracted with chloroform. The extract was washed with water, concentrated, impregnated with hexane, and recrystallized to obtain desloratadine.
Last Update：2025-06-10 22:55:16
100643-71-8 - Application
Open Data Verified Data
The United States of America first Lingyi Baoya (Sehering-plough) company development, first listed in the United Kingdom in 2001years. Non-sedating long-acting tricyclic antihistamines, the active metabolite of loratadine. It has the effect of selectively antagonizing the peripheral Hi receptor, and can inhibit the release of inflammatory mediators, the generation of superoxide anion, and the like. The affinity for Hi receptors is 10-20 times that of loratadine, and there is no sedative or anticholinergic effect. For adults and children over 12 years of age with seasonal allergic rhinitis (SAR), chronic idiopathic urticaria (CIU) and unexplained urticaria.
Last Update：2025-08-19 16:24:40
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