奥索马嗪

奥索马嗪用途

Oxomemazine 是一种基于吩噻嗪的组胺 H1 受体 (histamine H1-receptor) 阻滞剂,具有明显的抗毒蕈碱活性。Oxomemazine 是毒菌碱 M1 受体的选择性拮抗剂,在高 (histamine H1-receptor= 84 nM, M1受体) 和低 (histamine H1-receptor=1.65 μM, M2受体) 亲和力位点上显示了 20 倍的差异。Oxomemazine 一种用于咳嗽治疗相关研究的一种抗组胺和抗胆碱能试剂。

奥索马嗪名称

[ CAS 号 ]:
3689-50-7

[ 中文名 ]:
双氧异丁嗪

[ 英文名 ]:
Oxomemazine

[中文别名 ]:

奥索马嗪

[英文别名 ]:

EINECS 222-996-8
Oxomemazine [INN:DCF]
Oxomemazine
RP 6847
Dysedon

奥索马嗪生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 谷氨酸受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H1 Receptor

mGluR 1:84 nM (Ki)

mGluR2:1.65 μM (Ki)

[参考文献]

[1]. S W Lee, et al.Selectivity of oxomemazine for the M1 muscarinic receptors.Arch Pharm Res. 1994 Dec;17(6):443-51.

[2]. M S Siddegowda, et al.Oxomemazine hydro-chloride. Acta Crystallogr Sect E Struct Rep Online. 2011 Aug 1;67(Pt 8):o1875.

奥索马嗪物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
492.4±34.0 °C at 760 mmHg

[ 分子式 ]:
C₁₈H₂₂N₂O₂S

[ 分子量 ]:
330.444

[ 闪点 ]:
251.6±25.7 °C

[ 精确质量 ]:
330.140198

[ PSA ]:
49.00000

[ LogP ]:
2.85

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.598

[ 储存条件 ]:
室温，密封，干燥

奥索马嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SO5775000

CHEMICAL NAME :: Phenothiazine, 10-(3-(dimethylamino)-2-methylpropyl)-, 5,5-dioxide

CAS REGISTRY NUMBER :: 3689-50-7

BEILSTEIN REFERENCE NO. :: 0289178

LAST UPDATED :: 199612

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C18-H22-N2-O2-S

MOLECULAR WEIGHT :: 330.48

WISWESSER LINE NOTATION :: T C666 BN ISWJ B1Y1&1N1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: Standard Draize test

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 20,573,1982

TYPE OF TEST :: Rinsed with water

ROUTE OF EXPOSURE :: Administration into the eye

SPECIES OBSERVED :: Rodent - rabbit

REFERENCE :: FCTOD7 Food and Chemical Toxicology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.20- 1982- Volume(issue)/page/year: 20,573,1982 ** ACUTE TOXICITY DATA **

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 140 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: THERAP Therapie. (Doin, Editeurs, 8, Place de l'Odeon, F-75006 Paris, France) V.1- 1946- Volume(issue)/page/year: 26,1203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 185 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - irritability Skin and Appendages - hair

REFERENCE :: NYKZAU Nippon Yakurigaku Zasshi. Japanese Journal of Pharmacology. (Nippon Yakuri Gakkai, c/o Kyoto Daigaku Igakubu Yakurigaku Kyoshitsu, Konoe-cho, Yoshida, Sakyo-ku, Kyoto 606, Japan) V.40- 1944- Volume(issue)/page/year: 57,460,1961

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 260 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 135,364,1962

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes

REFERENCE :: AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 135,364,1962 *** REVIEWS *** TOXICOLOGY REVIEW TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 15,57,1977

奥索马嗪安全信息

[ 海关编码 ]:
2934300000

奥索马嗪海关

[ 海关编码 ]: 2934300000

[ 中文概述 ]:
2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 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 ]:
2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%