甲吡吩嗪

甲吡吩嗪用途

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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甲吡吩嗪名称

[ CAS 号 ]:
1982-37-2

[ 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
methdilazine
Methdilazinum
Metodilazina
Tacryl
Methodilazine
Methdilazinum [INN-Latin]

甲吡吩嗪生物活性

[ 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 ]:

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

[ 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.

甲吡吩嗪物理化学性质

[ 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

甲吡吩嗪毒性和生态

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

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甲吡吩嗪安全信息

[ 海关编码 ]:
2934300000

甲吡吩嗪合成路线

详细合成路线

甲吡吩嗪海关

[ 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%