79307-93-0

• 常用中文名：盐酸氮卓斯汀
• 常用英文名：azelastine hydrochloride
• CAS号：79307-93-0
• 分子式：C₂₂H₂₅Cl₂N₃O
• 分子量：418.359
• 相关类别： 原料药 抗变态反应药 抗组胺药
• 发布时间：2018-08-13 13:12:29
• 更新时间：2024-01-08 18:39:23
• Azelastine盐酸盐是第二代H1受体拮抗剂。

名称

• 中文名: 盐酸氮卓斯汀
• 英文名: azelastine hydrochloride
• 中文别名: 盐酸氮斯汀; 4-(4-氯苄基)-2-(1-甲基氮杂卓-4-基)-1-酞嗪酮盐酸盐; 4-(4-氯苄基)-2-(六氢-1-甲基-1H-氮卓-4-基)-1-(2H)-酞嗪盐酸盐; 盐酸氮䓬斯汀; 氮䓬斯汀盐酸盐; 盐酸氮斯丁
• 英文别名: Azelastine hydrochloride; 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, hydrochloride (1:1); 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone hydrochloride; 4-((4-Chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)phthalazin-1(2H)-one hydrochloride; UNII:0L591QR10I; 1(2H)-phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride; 4-(4-Chlorobenzyl)-2-(1-methyl-4-azepanyl)-1(2H)-phthalazinone hydrochloride (1:1); 4-(4-chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one hydrochloride; azelastinum [INN_la]; 4-(4-Chlorobenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-one hydrochloride (1:1); MFCD00242783; 4-(4-Chlorbenzyl)-2-(1-methylazepan-4-yl)phthalazin-1(2H)-onhydrochlorid; 4-(4-chlorobenzyl)-2-(1-méthylazépan-4-yl)phtalazin-1(2H)-one chlorhydrate; Azelastine (hydrochloride)

物化性质

• 密度: 1.25 g/cm3
• 沸点: 533.9ºC at 760 mmHg
• 熔点: 225-229ºC
• 分子式: C₂₂H₂₅Cl₂N₃O
• 分子量: 418.359
• 闪点: 276.7ºC
• 精确质量: 417.137482
• PSA: 38.13000
• LogP: 5.03740
• 外观性状: 白色结晶粉末
• 储存条件: 通风低温干燥,与库房食品原料分开存放
• 稳定性: Incompatible with strong oxidizing agents.
• 水溶解性: 水溶性：可溶

生物活性

• 描述: Azelastine盐酸盐是第二代H1受体拮抗剂。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 炎症/免疫
• 参考文献:

  [1]. Kempuraj, D., et al., Azelastine is more potent than olopatadine n inhibiting interleukin-6 and tryptase release from human umbilical cord blood-derived cultured mast cells. Ann Allergy Asthma Immunol, 2002. 88(5): p. 501-6.

  [2]. Canonica, G.W., et al., Topical azelastine in perennial allergic conjunctivitis. Curr Med Res Opin, 2003. 19(4): p. 321-9.

  [3]. Lieberman, P., M.A. Kaliner, and W.J. Wheeler, Open-label evaluation of azelastine nasal spray in patients with seasonal allergic rhinitis and nonallergic vasomotor rhinitis. Curr Med Res Opin, 2005. 21(4): p. 611-8.

MSDS

盐酸氮斯丁 修改号码：5 模块1. 化学品 产品名称： Azelastine Hydrochloride 修改号码： 5 模块2. 危险性概述 GHS分类 　物理性危害未分类 　健康危害 急性毒性（经口） 第4级 　环境危害未分类 GHS标签元素 　图标或危害标志 　信号词警告 　危险描述吞咽有害。 　防范说明 [预防]使用本产品时切勿吃东西，喝水或吸烟。 处理后要彻底清洗双手。 [急救措施] 食入：若感不适，呼叫解毒中心/医生。漱口。 [废弃处置] 根据当地政府规定把物品/容器交与工业废弃处理机构。 模块3. 成分/组成信息 单一物质/混和物单一物质 化学名(中文名)：盐酸氮斯丁 百分比： >98.0%(LC)(T) CAS编码： 79307-93-0 俗名： 4-(4-Chlorobenzyl)-2-(1-methylazepan-4-yl)-1-phthalazinone Hydrochloride 分子式： C22H24ClN3O·HCl 模块4. 急救措施 吸入： 将受害者移到新鲜空气处，保持呼吸通畅，休息。若感不适请求医/就诊。 盐酸氮斯丁 修改号码：5 模块4. 急救措施 皮肤接触： 立即去除/脱掉所有被污染的衣物。用水清洗皮肤/淋浴。 若皮肤刺激或发生皮疹：求医/就诊。 眼睛接触：用水小心清洗几分钟。如果方便，易操作，摘除隐形眼镜。继续清洗。 如果眼睛刺激：求医/就诊。 食入： 若感不适，呼叫解毒中心/医生。漱口。 紧急救助者的防护：救援者需要穿戴个人防护用品，比如橡胶手套和气密性护目镜。 模块5. 消防措施 合适的灭火剂：干粉，泡沫，雾状水，二氧化碳 特殊危险性：小心，燃烧或高温下可能分解产生毒烟。 特定方法：从上风处灭火，根据周围环境选择合适的灭火方法。 非相关人员应该撤离至安全地方。 周围一旦着火：如果安全，移去可移动容器。 消防员的特殊防护用具：灭火时，一定要穿戴个人防护用品。 模块6. 泄漏应急处理 个人防护措施，防护用具， 使用个人防护用品。远离溢出物/泄露处并处在上风处。 紧急措施：泄露区应该用安全带等圈起来，控制非相关人员进入。 环保措施：防止进入下水道。 控制和清洗的方法和材料：清扫收集粉尘，封入密闭容器。注意切勿分散。附着物或收集物应该立即根据合适的 法律法规处置。 模块7. 操作处置与储存 处理 技术措施：在通风良好处进行处理。穿戴合适的防护用具。防止粉尘扩散。处理后彻底清洗双手 和脸。 注意事项：如果粉尘或浮质产生，使用局部排气。 操作处置注意事项：避免接触皮肤、眼睛和衣物。 贮存 储存条件：保持容器密闭。冷冻储存。 远离不相容的材料比如氧化剂存放。 热敏 包装材料：依据法律。 模块8. 接触控制和个体防护 工程控制：尽可能安装封闭体系或局部排风系统，操作人员切勿直接接触。同时安装淋浴器和洗 眼器。 个人防护用品 　呼吸系统防护：防尘面具。依据当地和政府法规。 　手部防护：防护手套。 　眼睛防护：安全防护镜。如果情况需要，佩戴面具。 　皮肤和身体防护：防护服。如果情况需要，穿戴防护靴。 模块9. 理化特性 固体 外形（20°C）： 外观： 晶体-粉末 颜色：白色类白色 气味：无资料 pH:无数据资料 盐酸氮斯丁 修改号码：5 模块9. 理化特性 熔点： 226°C 沸点/沸程无资料 闪点：无资料 爆炸特性 　爆炸下限：无资料 　爆炸上限：无资料 密度：无资料 溶解度： [水]溶于 [其他溶剂]无资料 模块10. 稳定性和反应性 化学稳定性：一般情况下稳定。 危险反应的可能性：未报道特殊反应性。 须避免接触的物质氧化剂 危险的分解产物: 一氧化碳, 二氧化碳, 氮氧化物 (NOx), 氯化氢 模块11. 毒理学信息 急性毒性： orl-rat LD50:580 mg/kg ivn-rat LD50:24600 ug/kg scu-rat LD50:80500 ug/kg 对皮肤腐蚀或刺激：无资料 对眼睛严重损害或刺激：无资料 生殖细胞变异原性：无资料 致癌性： IARC =无资料 NTP =无资料 生殖毒性：无资料 RTECS 号码: TH9203900 模块12. 生态学信息 生态毒性： 鱼类：无资料 甲壳类：无资料 藻类：无资料 残留性 / 降解性：无资料 潜在生物累积 （BCF):无资料 土壤中移动性 　log水分配系数：无资料 　土壤吸收系数 （Koc）：无资料 　亨利定律无资料 constant(PaM3/mol): 模块13. 废弃处置 如果可能，回收处理。请咨询当地管理部门。建议在可燃溶剂中溶解混合，在装有后燃和洗涤装置的化学焚烧炉中 焚烧。废弃处置时请遵守国家、地区和当地的所有法规。 模块14. 运输信息 联合国分类：与联合国分类标准不一致 盐酸氮斯丁 修改号码：5 模块14. 运输信息 UN编号：未列明 模块15. 法规信息 《危险化学品安全管理条例》（2002年1月26日国务院发布，2011年2月16日修订）: 针对危险化学品的安全使用、 生产、储存、运输、装卸等方面均作了相应的规定。 模块16 - 其他信息 N/A

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : TH9203900 CHEMICAL NAME : 1(2H)-Phthalazinone, 4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1H-a zepin-4-yl)-, monohydrochloride CAS REGISTRY NUMBER : 79307-93-0 LAST UPDATED : 199206 DATA ITEMS CITED : 21 MOLECULAR FORMULA : C22-H24-Cl-N3-O.Cl-H MOLECULAR WEIGHT : 418.40 WISWESSER LINE NOTATION : T66 BVNNJ E1R DG& C- DT7NTJ A1 &GH HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 580 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 80500 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 24600 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 115 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 143 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 59600 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 25400 ug/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Gastrointestinal - changes in structure or function of salivary glands REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 57200 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 107 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Gastrointestinal - nausea or vomiting REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5235,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 126 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 37300 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 23 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 46200 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5231,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1050 mg/kg/5W-C TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5238,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 5460 mg/kg/26W-C TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5273,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 10920 mg/kg/52W-C TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5287,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 700 mg/kg/5W-C TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Related to Chronic Data - death REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,5251,1986 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 6729 mg/kg SEX/DURATION : male 11 week(s) pre-mating female 2 week(s) pre-mating - 7 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - other measures of fertility REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1225,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 330 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1225,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 755 mg/kg SEX/DURATION : female 7-17 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1225,1981 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 390 mg/kg SEX/DURATION : female 6-18 day(s) after conception TOXIC EFFECTS : Reproductive - Fertility - abortion Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,1225,1981

安全

• 符号: GHS07
• 信号词: Warning
• 危害声明: H302
• 警示性声明: P301 + P312 + P330
• 危害码 (欧洲): Xn
• 风险声明 (欧洲): 22
• 危险品运输编码: NONH for all modes of transport