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]。
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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 ]:
- MJ 5022
- Bristaline
- Methdilazine monohydrochloride
- Methdilazine Hcl
- Tacaryl hydrochloride
- Disyncran
- Dilosyn
- Methdilazine hydrochloride
- METHDILAZINE HYDROCHLORIDE
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 ]:
[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]
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
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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%
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