1229-35-2

• 常用中文名：盐酸甲吡吩嗪
• 常用英文名：Methdilazine Hydrochloride
• CAS号：1229-35-2
• 分子式：C₁₈H₂₁ClN₂S
• 分子量：332.89100
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2018-04-09 08:00:00
• 更新时间：2024-01-27 21:45:48
• 盐酸甲地嗪是一种口服活性抗生素(组胺拮抗剂)。盐酸甲地嗪在体内外均能抑制多种分枝杆菌,MIC值为5-15μg/mL,可用于传染病研究[1][2]。

名称

• 中文名: 盐酸甲吡吩嗪
• 英文名: 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine,hydrochloride
• 中文别名: 盐酸甲地嗪
• 英文别名: MJ 5022; Bristaline; Methdilazine monohydrochloride; Methdilazine Hcl; 10-(1-methyl-pyrrolidin-3-ylmethyl)-10H-phenothiazine,monohydrochloride; Tacaryl hydrochloride; Disyncran; Dilosyn; Methdilazine hydrochloride; METHDILAZINE HYDROCHLORIDE

物化性质

• 沸点: 430.4ºC at 760mmHg
• 熔点: 187.5-189ºC
• 分子式: C₁₈H₂₁ClN₂S
• 分子量: 332.89100
• 闪点: 214.1ºC
• 精确质量: 332.11100
• PSA: 31.78000
• LogP: 5.04590
• 蒸汽压: 1.3E-07mmHg at 25°C
• 折射率: 1.642

生物活性

• 描述: 盐酸甲地嗪是一种口服活性抗生素(组胺拮抗剂)。盐酸甲地嗪在体内外均能抑制多种分枝杆菌,MIC值为5-15μg/mL,可用于传染病研究[1][2]。
• 相关类别:
  信号通路 >> 免疫及炎症 >> 组胺受体
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 细菌
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体
• 体外研究: 盐酸甲地嗪(约0-20μg/mL,18小时)抑制多种分枝杆菌,MIC值在5μg/mL至15μg/mL之间[1]。细胞增殖试验[1]细胞系：耻垢分枝杆菌798/1546,M.,偶发性1529,阴囊分枝杆菌1323,戈登分枝杆菌1324,核糖核酸分枝杆菌50,M.,黄曲霉1541,地分枝杆菌1450,结核分枝杆菌,H37Ra 16,H37Rv 16,K1,K2,ICRC芽孢杆菌,'Skinsnes'芽孢杆菌。浓度：0-20μg/mL约培养时间：18小时结果：抑制分枝杆菌,MIC值范围为5μg/mL至15μg/mL。
• 体内研究: 盐酸甲地嗪(腹腔注射,10μg/gm体重/天,6周)对H37Rv感染小鼠的分枝杆菌具有拮抗作用[1]。盐酸甲地嗪(口服,每天10 mg/kg,28天)可提高结核分枝杆菌(Mtb)H37Rv感染小鼠的存活率[2]。动物模型：H37Rv感染小鼠[1]剂量：10μg/gm体重/天,6周给药：腹腔注射结果：对分枝杆菌有抗分枝杆菌活性。动物模型：结核分枝杆菌H37Rv感染瑞士白化雄性小鼠[2]剂量：每天10 mg/kg,连续28天给药：口服给药结果：存活时间延长至28天,无疾病迹象,存活率为71.42%。
• 参考文献:

  [1]. A N Chakrabarty, et al. Antimycobacterial activity of methdilazine (Md), an antimicrobic phenothiazine. APMIS. 1993 Jun;101(6):449-54.

  [2]. Noton K Dutta, et al. Activity of the phenothiazine methdilazine alone or in combination with isoniazid or streptomycin against Mycobacterium tuberculosis in mice. J Med Microbiol. 2009 Dec;58(Pt 12):1667-1668.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : SP3150000 CHEMICAL NAME : Phenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-, monohydrochloride CAS REGISTRY NUMBER : 1229-35-2 LAST UPDATED : 199510 DATA ITEMS CITED : 13 MOLECULAR FORMULA : C18-H20-N2-S.Cl-H MOLECULAR WEIGHT : 332.92 WISWESSER LINE NOTATION : T C666 BN ISJ B1- CT5NTJ 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 : 260 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 75 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 22 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 190 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 100 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 25 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 300 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 25 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rabbit DOSE/DURATION : 17 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - guinea pig DOSE/DURATION : 263 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 9880 mg/kg/52W-I TOXIC EFFECTS : Related to Chronic Data - death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 150 mg/kg SEX/DURATION : female 2-4 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) MUTATION DATA TYPE OF TEST : Morphological transformation TEST SYSTEM : Rodent - hamster Embryo DOSE/DURATION : 10 mg/L REFERENCE : ENMUDM Environmental Mutagenesis. (New York, NY) V.1-9, 1979-87. For publisher information, see EMMUEG. Volume(issue)/page/year: 8(Suppl 6),4,1986

安全

• 危险品运输编码: NONH for all modes of transport
• 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%