萘甲唑啉

萘甲唑啉用途

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]。

萘甲唑啉名称

[ CAS 号 ]:
835-31-4

[ 中文名 ]:
萘甲唑林

[ 英文名 ]:
naphazoline

[中文别名 ]:

[英文别名 ]:

naphazoline
Sanorin
Clearine
Naphthizine
2-(1-Naphthylmethyl)-4,5-dihydro-1H-imidazole
Clera
EINECS 212-641-5
MFCD00012554
Naphcon
Coldan

萘甲唑啉生物活性

[ 描述 ]:

[ 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.

萘甲唑啉物理化学性质

[ 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

萘甲唑啉毒性和生态

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

萘甲唑啉安全信息

[ 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

萘甲唑啉合成路线

详细合成路线

萘甲唑啉上下游产品

萘甲唑啉上游产品

萘甲唑啉下游产品

萘甲唑啉海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%