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苄硝唑

苄硝唑用途

Benznidazol (Ro 07-1051) 是一种抗寄生虫药物,对哥伦比亚 T. cruzi 菌株的 IC50 值为 20.35 μM,目前已被用于治疗美洲锥虫病。

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苄硝唑名称

[ CAS 号 ]:
22994-85-0

[ 中文名 ]:
苄硝唑

[ 英文名 ]:
Benznidazole

[中文别名 ]:

[英文别名 ]:

MFCD00243089
N-benzyl-2-(2-nitroimidazol-1-yl)acetamide
1H-Imidazole-1-acetamide,2-nitro-N-(phenylmethyl)-

苄硝唑生物活性

[ 描述 ]:

Benznidazol (Ro 07-1051) 是一种抗寄生虫药物,对哥伦比亚 T. cruzi 菌株的 IC50 值为 20.35 μM,目前已被用于治疗美洲锥虫病。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[体内研究]

苯并咪唑(100 mg/kg /天,口服,30天)使感染克氏锥虫的小鼠心电图改变减少,心脏受体的亲和力和密度修改减少,心脏纤维化的孤立区域减少。菌株或SGO-Z12分离株在感染后(pi)(即慢性期)用苯并咪唑处理180天[1]。动物模型：感染克氏锥虫Tulahuen菌株或SGO-Z12的小鼠[1]剂量：100 mg/kg /天给药：口服30天结果：心电图改变减少,心脏的亲和力和密度变化较小受体,以及心脏中几乎没有纤维化的区域。

[参考文献]

[1]. Bustamante JM, et al. Treatment with benznidazole or thioridazine in the chronic phase of experimental Chagas disease improves cardiopathy. Int J Antimicrob Agents. 2007 Jun;29(6):733-7.

[2]. Luna KP, et al. In vitro susceptibility of Trypanosoma cruzi strains from Santander, Colombia, to hexadecylphosphocholine (miltefosine), nifurtimox and benznidazole. Biomedica. 2009 Sep;29(3):448-55.

苄硝唑物理化学性质

[ 密度 ]:
1.35g/cm3

[ 熔点 ]:
189-192ºC(lit.)

[ 分子式 ]:
C₁₂H₁₂N₄O₃

[ 分子量 ]:
260.24900

[ 精确质量 ]:
260.09100

[ PSA ]:
92.74000

[ LogP ]:
2.02180

[ 外观性状 ]:
粉末

[ 折射率 ]:
1.643

[ 储存条件 ]:
-20℃

苄硝唑MSDS

详细MSDS(安全技术说明书)

苄硝唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NI3340000

CHEMICAL NAME :: Imidazole-1-acetamide, N-benzyl-2-nitro-

CAS REGISTRY NUMBER :: 22994-85-0

BEILSTEIN REFERENCE NO. :: 0551486

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C12-H12-N4-O3

MOLECULAR WEIGHT :: 260.28

WISWESSER LINE NOTATION :: T5N CNJ A1VM1R& BNW

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 8 gm/kg

SEX/DURATION :: male 8 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count)

TYPE OF TEST :: Cytogenetic analysis

MUTATION DATA

TYPE OF TEST :: Sister chromatid exchange

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 50 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 320,305,1994

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苄硝唑安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ RTECS号 ]:
NI3340000

[ 海关编码 ]:
2933290090

苄硝唑海关

[ 海关编码 ]: 2933290090

[ 中文概述 ]:
2933290090. 其他结构含非稠合咪唑环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

苄硝唑文献

Targeting the substrate preference of a type I nitroreductase to develop antitrypanosomal quinone-based prodrugs.

Antimicrob. Agents Chemother. 56(11) , 5821-30, (2012)

Nitroheterocyclic prodrugs are used to treat infections caused by Trypanosoma cruzi and Trypanosoma brucei. A key component in selectivity involves a specific activation step mediated by a protein hom...

Microsatellite and mini-exon analysis of Mexican human DTU I Trypanosoma cruzi strains and their susceptibility to nifurtimox and benznidazole.

Vector Borne Zoonotic Dis. 13(3) , 181-7, (2013)

Chagas disease is caused by the protozoan parasite Trypanosoma cruzi, and it affects as many as 10 million people in North and South America, where it represents a major public health problem. T. cruz...

Immunosuppression and Chagas disease: a management challenge.

PLoS Negl. Trop. Dis. 7(1) , e1965, (2013)

Immunosuppression, which has become an increasingly relevant clinical condition in the last 50 years, modifies the natural history of Trypanosoma cruzi infection in most patients with Chagas disease. ...

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苄硝唑