Introduction：Basic information about Azelastine CAS 58581-89-8, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Azelastine Basic information
| Product Name: | Azelastine |
| Synonyms: | 1(2h)-phthalazinone,4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin;4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1-(2h)-phthalazinon;4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one hydrochloride;4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1-one;4-[(4-chlorophenyl)methyl]-2-(1-methyl-4-azepanyl)-1-phthalazinone;4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one;Azelastinum [INN-Latin];KBio3_002992 |
| CAS: | 58581-89-8 |
| MF: | C22H24ClN3O |
| MW: | 381.9 |
| EINECS: | 253-720-4 |
| Product Categories: | TELAZOL;API |
| Mol File: | 58581-89-8.mol |
|
Azelastine Chemical Properties
| Melting point | 111 - 115°C |
| Boiling point | 533.9±60.0 °C(Predicted) |
| density | 1.1505 (rough estimate) |
| refractive index | 1.5790 (estimate) |
| storage temp. | 2-8°C |
| solubility | Chloroform (Slightly), DMSO (Slightly, Heated), Methanol (Slightly) |
| pka | pKa 9.82(H2O t=25 I=0.025) (Uncertain) |
| form | Solid |
| color | White to Off-White |
| BCS Class | 1? |
| Stability: | Stable under recommended storage conditions., Stable Under Recommended Storage C |
| InChI | InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3 |
| InChIKey | MBUVEWMHONZEQD-UHFFFAOYSA-N |
| SMILES | C1(=O)C2=C(C=CC=C2)C(CC2=CC=C(Cl)C=C2)=NN1C1CCCN(C)CC1 |
| CAS DataBase Reference | 58581-89-8(CAS DataBase Reference) |
Safety Information
| Hazardous Substances Data | 58581-89-8(Hazardous Substances Data) |
| Toxicity | LD50 orl-rat: 310 mg/kg ARZNAD 31,1184,81 |
Azelastine Usage And Synthesis
| Description | Azelastine has potent, long-lasting histamineH1-receptor blocking activity and several otherinteresting anti-inflammatory properties relatedto its antiallergic efficacy . |
| Uses | anesthetic, anticonvulsant |
| Definition | ChEBI: A phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position. |
| Brand name | Astelin(Medpointe); Optivar (Medpointe). |
| Clinical Use | Azelastine, although not a close structural analogue to the benzimidazoles, has somestructural similarities to them. It is used as a nasal spray for allergic rhinitis and as eye dropsfor allergic conjunctivitis.Like olopatadine, azelastine also stabilizes mast cells, preventingdegranulation and subsequent release of histamine, leukotrienes, and PGD2. It is available inEurope for systemic use in the treatment of asthma and seasonal allergies. Besidesantihistaminic effects, it also may block release of histamine and other inflammatorymediators from mast cells. When administered orally, the N-dealkylated metabolite appears tocontribute significantly to its pharmacological effects. |
| Safety Profile | Poison by ingestion,subcutaneous, intravenous, and intraperitoneal routes.Experimental reproductive effects. When heated todecomposition it emits toxic fumes of NOx and Cl- . |
Azelastine Preparation Products And Raw materials
| Raw materials | Acetophenone-->Hydrazine sulfate-->3-METHOXYPROPIONIC ACID-->Diphenylmethane-->1-Methylpyrrolidine-->4-(4-Chloro-benzyl)-2H-phthalazin-1-one |
