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盐酸甲吡吩嗪

盐酸甲吡吩嗪用途

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]。

盐酸甲吡吩嗪名称

[ CAS 号 ]:
1229-35-2

[ 中文名 ]:
盐酸甲吡吩嗪

[ 英文名 ]:
Methdilazine Hydrochloride

[中文别名 ]:

[英文别名 ]:

盐酸甲吡吩嗪生物活性

[ 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.

盐酸甲吡吩嗪物理化学性质

[ 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

盐酸甲吡吩嗪毒性和生态

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

盐酸甲吡吩嗪安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2934300000

盐酸甲吡吩嗪海关

[ 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%

推荐生产厂家/供应商：

公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

价格：

联系人：徐经理

产品详情：盐酸甲吡吩嗪

公司名：上海源溪生物科技有限公司

区域：上海市浦东新区

价格：
￥需询单/1g

联系人：赖经理

产品详情：Methdilazine Hydrochloride

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