中文名 | Azelastine |
英文名 | Azelastine |
别名 | 氮卓司丁 氮卓斯丁 氮卓司汀 氮卓斯汀 4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓)二氮杂萘酮 4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓-4-基)二氮杂萘酮 4-[(4-氯苯基)甲基]-2-(六氢-1-甲基-1H-氮杂卓-4-基)-1(2H)-酞嗪酮 1(2H)-二氮杂萘酮,4-((4-氯苯基)甲基)-2-(六氢-1-甲基-1H-氮杂卓-4-基)- |
英文别名 | Azelastine KBio3_002992 Azelastinum [INN-Latin] 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 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one hydrochloride 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1-(2h)-phthalazinon 1(2h)-phthalazinone,4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin |
CAS | 58581-89-8 |
EINECS | 253-720-4 |
化学式 | C22H24ClN3O |
分子量 | 381.9 |
密度 | 1.1505 (rough estimate) |
熔点 | 111 - 115°C |
沸点 | 533.9±60.0 °C(Predicted) |
溶解度 | 氯仿 (微溶),DMSO (微溶,加热),甲醇 (微溶) |
折射率 | 1.5790 (estimate) |
酸度系数 | pKa 9.82(H2O t=25 I=0.025) (Uncertain) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | White to Off-White |
物化性质 | 油状物。溶于二氯甲烷。单水合物:从乙醇-水结晶。可鉴定出两种不同的晶型。盐酸氮革斯汀(Azelastine Hydrochloride):C22H24ClN3O?HCl。[79307-93-0]。白色结晶性粉末,无臭,味苦。溶于氯仿、二氯甲烷或冰醋酸,略溶于甲醇,微溶于无水乙醇或水,不溶于丙酮或乙醚。熔点225~229℃。急性毒性LD50雄、雌小鼠,雄、雌大鼠,雄、雌豚鼠(mg/kg):124,139,310,417,126,130口服;36.5,35.5,26.9,30.3,23.0,24.8静脉注射;597.0,57.2,143.0,115.0,46.2,52.2肌肉注射;63.0,54.2,66.5,59.6。41.0.37.3皮下注射。 |
上游原料 | 3-甲氧基丙酸 二苯基甲烷 1-甲基吡咯烷 4-(4-氯苄基)-1-(2H)-酞嗪酮 |
参考资料 展开查看 | 1. Li, Meng, et al. "Chiral separation of five antihistamine drug enantiomers and enantioselective pharmacokinetic study of carbinoxamine in rat plasma by HPLC-MS/MS." New Journal of Chemistry 44.15 (2020): 5819-5827.https://doi.org/10.1039/D0NJ00095G |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.618 ml | 13.092 ml | 26.185 ml |
5 mM | 0.524 ml | 2.618 ml | 5.237 ml |
10 mM | 0.262 ml | 1.309 ml | 2.618 ml |
5 mM | 0.052 ml | 0.262 ml | 0.524 ml |