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1982-37-2

1982-37-2结构式
1982-37-2结构式
  • 常用中文名：甲吡吩嗪
  • 常用英文名：10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine
  • CAS号：1982-37-2
  • 分子式：C18H20N2S
  • 分子量：296.43000
  • 相关类别： 信号通路 抗感染 细菌
  • 发布时间：2018-03-29 08:00:00
  • 更新时间：2024-01-02 17:47:33
  • 甲地嗪是一种口服活性抗生素(组胺拮抗剂)。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]。

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中文名 甲吡吩嗪
英文名 10-[(1-methylpyrrolidin-3-yl)methyl]phenothiazine
中文别名 盐酸甲吡
英文别名 10-[(1-methyl-3-pyrrolidinyl)methyl]phenothiazine
Tacazyl
10-(1-methyl-pyrrolidin-3-ylmethyl)-phenothiazine
10-(1-Methyl-pyrrolidin-3-ylmethyl)-phenothiazin
10-<1-Methyl-pyrrolidinyl-(3)-methyl>-phenothiazin.
methdilazine
Methdilazinum
Metodilazina
Tacryl
Methodilazine
Methdilazinum [INN-Latin]
Disyncram
Tacaryl
Metodilazina [INN-Spanish]
10-(1-methyl-pyrrolidin-3-ylmethyl)-10H-phenothiazine
描述 甲地嗪是一种口服活性抗生素(组胺拮抗剂)。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
靶点

MIC: 5-15 μg/mL (mycobacterium)

体外研究 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：分枝杆菌：耻垢分枝杆菌798/1546,M.,偶发菌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 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]。甲地嗪(口服,每天10 mg/kg,28天)可提高结核分枝杆菌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.

密度 1.185 g/cm3
沸点 430.4ºC at 760 mmHg
分子式 C18H20N2S
分子量 296.43000
闪点 214.1ºC
精确质量 296.13500
PSA 31.78000
LogP 4.24390
计算化学

1.疏水参数计算参考值（XlogP）:无

2.氢键供体数量:0

3.氢键受体数量:3

4.可旋转化学键数量:2

5.互变异构体数量:无

6.拓扑分子极性表面积:31.8

7.重原子数量:21

8.表面电荷:0

9.复杂度:339

10.同位素原子数量:0

11.确定原子立构中心数量:0

12.不确定原子立构中心数量:1

13.确定化学键立构中心数量:0

14.不确定化学键立构中心数量:0

15.共价键单元数量:1

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SP2975000
CHEMICAL NAME :
Phenothiazine, 10-((1-methyl-3-pyrrolidinyl)methyl)-
CAS REGISTRY NUMBER :
1982-37-2
LAST UPDATED :
199510
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C18-H20-N2-S
MOLECULAR WEIGHT :
296.46
WISWESSER LINE NOTATION :
T C666 BN ISJ B1- CT5NTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
4 mg/kg
TOXIC EFFECTS :
Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - other changes
REFERENCE :
34ZIAG "Toxicology of Drugs and Chemicals," Deichmann, W.B., New York, Academic Press, Inc., 1969 Volume(issue)/page/year: -,379,1969
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
162 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 18,185,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
225 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
183 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
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
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972

海关编码 2934300000
58689-43-3结构式

58689-43-3

92-84-2结构式

92-84-2

~%

1982-37-2结构式

1982-37-2

文献：Journal of Organic Chemistry, , vol. 26, p. 1529 - 1530
92-84-2结构式

92-84-2

~%

1982-37-2结构式

1982-37-2

文献：Arzneimittel Forschung, , vol. 9, p. 715
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%

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