835-31-4

• 常用中文名：萘甲唑啉
• 常用英文名：naphazoline
• CAS号：835-31-4
• 分子式：C₁₄H₁₄N₂
• 分子量：210.274
• 相关类别： 原料药 神经系统用药 拟胆碱药
• 发布时间：2018-05-20 08:00:00
• 更新时间：2024-01-02 18:15:43
• 萘唑啉(萘唑啉)是一种有效的α-肾上腺素能受体激动剂。萘甲唑啉可降低血管通透性,促进血管收缩。萘唑啉可降低炎症因子(TNF-α、IL-1β和IL-6)、细胞因子(IFN-γ和IL-4)、IgE、GMCSF和NGF的水平萘甲唑啉可用于非细菌性结膜炎研究[1][2]。

名称

• 中文名: 萘甲唑林
• 英文名: 2-(naphthalen-1-ylmethyl)-4,5-dihydro-1H-imidazole
• 中文别名: 2-(1-萘甲基)-4,5-二氢-1H-咪唑; 萘达帕汀; 2-(1-萘甲)咪唑啉鹽酸鹽; 萘甲唑啉
• 英文别名: naphazoline; Sanorin; Clearine; Naphthizine; 2-(1-Naphthylmethyl)-4,5-dihydro-1H-imidazole; Clera; EINECS 212-641-5; MFCD00012554; Naphcon; Coldan; Antan; Nafazolina; 1H-Imidazole, 4,5-dihydro-2-(1-naphthalenylmethyl)-

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 440.5±24.0 °C at 760 mmHg
• 熔点: 254ºC
• 分子式: C₁₄H₁₄N₂
• 分子量: 210.274
• 闪点: 220.2±22.9 °C
• 精确质量: 210.115692
• PSA: 24.39000
• LogP: 3.88
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.640
• 储存条件: 2-8°C

生物活性

• 描述: 萘唑啉(萘唑啉)是一种有效的α-肾上腺素能受体激动剂。萘甲唑啉可降低血管通透性,促进血管收缩。萘唑啉可降低炎症因子(TNF-α、IL-1β和IL-6)、细胞因子(IFN-γ和IL-4)、IgE、GMCSF和NGF的水平萘甲唑啉可用于非细菌性结膜炎研究[1][2]。
• 相关类别:
  研究领域 >> 心血管疾病
  信号通路 >> 免疫及炎症 >> 白细胞介素相关
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  研究领域 >> 炎症/免疫
  信号通路 >> 蛋白酪氨酸激酶 >> VEGFR
• 靶点:

  TNF-α

  IL-1β

  IL-6

  IL-4

• 体内研究: 萘甲唑啉(0.2 mg/kg,10µl/眼；IP,一次)降低组胺或抗原诱导的小鼠结膜血管通透性,并通过对炎症、NGF和VEGF的影响降低小鼠结膜炎[1]。动物模型：雌性野生型BALB/c小鼠(4-5周,18±2 g,n=8/组,使用组胺或抗原(卵清蛋白)建立过敏性结膜炎小鼠模型)[1]剂量：0.2 mg/mL,10µl/眼给药：腹腔注射(IP),一次结果：显著抑制组胺或抗原诱导的结膜血管通透性高的小鼠结膜色素渗漏。降低炎症反应和IL-1β、IL-6、IFN-γ和IL-4的水平。降低抗原诱导的结膜血管通透性高的小鼠中IgE、GMCSF、NGF和VEGF的水平。
• 参考文献:

  [1]. Quan L, et, al. Treatment with olopatadine and naphazoline hydrochloride reduces allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF. Mol Med Rep. 2016 Apr;13(4):3319-25.

  [2]. Yamaguchi I, et, al. Central and peripheral adrenergic mechanisms regulating gastric secretion in the rat. J Pharmacol Exp Ther. 1977 Oct;203(1):125-31.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NJ4200000 CHEMICAL NAME : 2-Imidazoline, 2-(1-naphthylmethyl)- CAS REGISTRY NUMBER : 835-31-4 BEILSTEIN REFERENCE NO. : 0151864 LAST UPDATED : 199612 DATA ITEMS CITED : 8 MOLECULAR FORMULA : C14-H14-N2 MOLECULAR WEIGHT : 210.30 WISWESSER LINE NOTATION : L66J B1- BT5M CN BUTJ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 385 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 9,280,1950 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 270 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 29,729,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 62 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 29,729,1979 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 514 mg/kg TOXIC EFFECTS : Behavioral - tremor Behavioral - convulsions or effect on seizure threshold REFERENCE : RPTOAN Russian Pharmacology and Toxicology (English Translation). Translation of FATOAO. (Euromed Pub., 33, Woodlands Rd., Surbiton, Surrey, UK) V.30- 1967- Volume(issue)/page/year: 37,198,1974 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 170 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 9,280,1950 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 950 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 9,280,1950 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 800 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : FEPRA7 Federation Proceedings, Federation of American Societies for Experimental Biology. (Bethesda, MD) V.1-46, 1942-87. Volume(issue)/page/year: 9,280,1950 TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - species unspecified DOSE/DURATION : 10 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 192,141,1939

安全

• 危害码 (欧洲): T: Toxic;
• 风险声明 (欧洲): R25
• 安全声明 (欧洲): 45
• 危险品运输编码: UN 2811 6.1/PG 2
• WGK德国: 3
• RTECS号: NJ4375000
• 海关编码: 2934999090

合成路线

86-87-3 6780-13-8 ~% 835-31-4

文献：DE687196 , ; DRP/DRBP Org.Chem. Przemysl Chemiczny, , vol. 32, p. 463 Chem.Abstr., , p. 11627 CH221216 , ; US2441867 , ;

132-75-2 141-43-5 ~% 835-31-4

文献：Monatshefte fuer Chemie, , vol. 80, p. 815,818

68211-49-4 ~% 835-31-4

文献：US2813862 , ;

132-75-2 ~% 835-31-4

文献：Journal of the Chemical Society, , p. 497,500 US2505247 , ; DE842063 , ; DRP/DRBP Org.Chem.

132-75-2 14034-59-4 ~% 835-31-4

文献：Journal of the Chemical Society, , p. 497,500 US2505247 , ; DE842063 , ; DRP/DRBP Org.Chem.

100621-70-3 107-15-3 ~% 835-31-4

文献：US2813862 , ;

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海关编码	2934999090
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