3689-50-7

• 常用中文名：奥索马嗪
• 常用英文名：Oxomemazine
• CAS号：3689-50-7
• 分子式：C₁₈H₂₂N₂O₂S
• 分子量：330.444
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 组胺受体
• 发布时间：2018-09-04 23:02:08
• 更新时间：2024-01-02 11:32:38
• 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。

名称

• 中文名: 双氧异丁嗪
• 英文名: 3-(5,5-dioxophenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine
• 中文别名: 奥索马嗪
• 英文别名: N,N,b-Trimethyl-10H-phenothiazine-10-propanamine 5,5-Dioxide; EINECS 222-996-8; Oxomemazine [INN:DCF]; 3-(5,5-dioxido-10H-phenothiazin-10-yl)-N,N,2-trimethylpropan-1-amine; 3-(9,9-Dioxo-10-phenothiazinyl)-2-methyl-1-dimethylaminopropane; Oxomemazine; 3-(5,5-Dioxido-10H-phenothiazin-10-yl)-N,N,2-trimethyl-1-propanamine; 10-(3-Dimethylamino-2-methylpropyl)phenothiazine 5,5-Dioxide; RP 6847; Dysedon; 10H-Phenothiazine-10-propanamine, N,N,β-trimethyl-, 5,5-dioxide; Dioxo-5.5-(2'-methyl-3'dimethylamino-propyl)-10 phenothiazin Oxomemazin Doxergan; 10-(3-(Dimethylamino)-2-methylpropyl)phenothiazine 5,5-dioxide

物化性质

• 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

生物活性

• 描述: 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。
• 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.

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

安全

• 海关编码: 2934300000

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%