Betotastine
Bepotastine
CAS: 125602-71-3;190786-43-7
Molecular Formula: C21H25ClN2O3
Betotastine - Names and Identifiers
| Name | Bepotastine |
| Synonyms | Betotastine BEPOTASTINE Bepotastine (+)-BEPOTASTINE betotastine besilate -4-(4-((4-Chlorophenyl) 4-[(S)-(4-chlorophenyl)-2-pyridinylMethoxy]- 4-((4-Chlorophenyl)-2-pyridinylmethoxy)-1-piperidinebutanoic acid 4-(4-[(1s)(4-chlorophenyl)-2-pyridylmethoxy]piperidyl)butanoic acid 4-(4-[(1S)(4-CHLOROPHENYL)-2-PYRIDYLMETHOXY]PIPERIDYL)BUTANOIC ACID 4-[4-[(4-Chlorophenyl)pyridin-2-ylmethoxy]piperidin-1-yl]butanoic acid 1-Piperidinebutanoic acid, 4-[(S)-(4-chlorophenyl)-2-pyridinylmethoxy]- 4-{4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid 4-{4-[(S)-(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid (+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]butyric acid |
| CAS | 125602-71-3 190786-43-7 |
| EINECS | 200-258-5 |
| InChI | InChI=1/C21H25ClN2O3/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26)/t21-/m0/s1 |
Betotastine - Physico-chemical Properties
| Molecular Formula | C21H25ClN2O3 |
| Molar Mass | 388.89 |
| Density | 1.26 |
| Melting Point | 56 - 58°C |
| Boling Point | 546.8±50.0 °C(Predicted) |
| Flash Point | 284.5°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Vapor Presure | 8.63E-13mmHg at 25°C |
| Appearance | Solid |
| Color | White to Pale Beige |
| pKa | 4.44±0.10(Predicted) |
| Storage Condition | -20°C Freezer, Under inert atmosphere |
| Refractive Index | 1.605 |
| Use | Anti-allergic drugs |
| In vitro study | Bepotastine possesses additional anti-allergic activity including stabilization of mast cell function, inhibition of eosinophilic infiltration, inhibition of IL-5 production, and inhibition of leukotriene B4 (LTB4) and LTD4 activity. Bepotastine significantly inhibits antigen-induced stimulation of IL-5 production in human peripheral blood mononuclear cells (PBMCs) at concentrations of 10-100 μM and the effect is enhanced when the PBMCs are pre-incubated with Bepotastine. Leukotriene B4 increased Ca2+ concentration in cultured neutrophils, which is suppressed by Bepotastine besilate (1-100 μM). Leukotriene B4 increased Ca2+ concentration in cultured dorsal root ganglion neurons, which is also suppressed by Bepotastine besilate (100 μM). |
| In vivo study | Bepotastine besilate (10 mg/kg) inhibits scratching induced by an intradermal injection of histamine (100 nmol/site), but not serotonin (100 nmol/site). Bepotastine besilate (1-10 mg/kg, oral) dose-dependently suppresses scratching induced by substance P (100 nmol/site) and leukotriene B4 (0.03 nmol/site). Bepotastine in vivo dose-dependently inhibits the acceleration of histamine-induced vascular permeability and inhibits homologous passive cutaneous anaphylaxis in guinea pig studies. In mouse models of itching, oral Bepotastine inhibits the frequency and duration of scratching behavior. |
Betotastine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.571 ml | 12.857 ml | 25.714 ml |
| 5 mM | 0.514 ml | 2.571 ml | 5.143 ml |
| 10 mM | 0.257 ml | 1.286 ml | 2.571 ml |
| 5 mM | 0.051 ml | 0.257 ml | 0.514 ml |
Last Update：2024-01-02 23:10:35
Betotastine - Reference Information
| biological activity | Bepotastine is a non-sedative, selective histamine 1 (H1) receptor antagonist. |
| target | Histamine H1 receptor |
Last Update：2024-04-09 18:58:34
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