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盐酸氯苯胍

盐酸氯苯胍用途

Robenidine hydrochloride 是一种抗球虫药, 对 MRSA 和 VRE 也有抑制活性,其 MIC50 值分别为 8.1 和 4.7 μM。

盐酸氯苯胍名称

[ CAS 号 ]:
25875-50-7

[ 中文名 ]:
盐酸氯苯胍

[ 英文名 ]:
Robenidine hydrochloride

[中文别名 ]:

[英文别名 ]:

EINECS 247-307-8
MFCD01724404
Robenidine hydrochloride

盐酸氯苯胍生物活性

[ 描述 ]:

Robenidine hydrochloride 是一种抗球虫药, 对 MRSA 和 VRE 也有抑制活性,其 MIC50 值分别为 8.1 和 4.7 μM。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[ 靶点 ]

MIC50: 8.1 μM (MRSA), 4.7 μM (VRE)[1]

[体外研究]

Robenidine(化合物1)抑制MRSA和VRE的生长,MIC值分别为8.1和4.7μM。 Robenidine对MBC/MIC90比率≤2的所有金黄色葡萄球菌菌株均具有杀菌作用。观察到MIC值的显着和负面影响,2％血清的Robenidine降低4倍,50％血清无活性[1]。

[体内研究]

在单独的氟苯尼考(FFC)组中,平均血浆浓度超过1μg/ mL浓度的时间约为6小时;然而,通过Robenidine(ROB)预处理将其降低至4小时。终末消除半衰期(t1/2z),浓度-时间曲线下面积(AUC),第一力矩曲线下面积(AUMC)和平均停留时间(MRT)显着降低,而消除速率常数(λz) )用Robenidine预处理的家兔体内清除率(CLz)明显增加[2]。

[细胞实验]

在该研究中使用MRSA临床分离株，并且使用改良的MIC测定法测定罗替尼定（化合物1）的MIC50。罗哌啶的抗微生物稀释液在100％DMSO中完成，每孔加入2μL。在96孔板中以200μL的总体积进行测定。 Robenidine的最终浓度为0.7至345.3μM。将板在37℃下孵育20至24小时，然后测定MIC [1]。

[动物实验]

将兔子分成四组（n = 8，每组）。对照组中的兔子在整个研究过程中喂食无抗球虫剂。另一组中的兔子连续20天喂食含有罗替尼啶（ROB）（66ppm）的口粮。在喂食第20天结束时，将单剂量的氟苯尼考（FFC）以25mg / kg体重（bw）静脉内注射到所有组中的每只兔的左耳静脉中。在5,10,15,30和45分钟以及1,1.5,2,4,6,8和12小时，从每只兔的右耳静脉收集血液（约1mL）样品到肝素涂层的管中。在管理FFC之后。在以3,000g离心10分钟后收获血浆并储存在-20℃直至分析[2]。

[参考文献]

[1]. Abraham RJ, et al. Robenidine Analogues as Gram-Positive Antibacterial Agents. J Med Chem. 2016 Mar 10;59(5):2126-38.

[2]. Liu C, et al. Influence of three coccidiostats on the pharmacokinetics of florfenicol in rabbits. Exp Anim. 2015;64(1):73-9.

[相关活性小分子]

盐酸氯苯胍物理化学性质

[ 沸点 ]:
488.1ºC at 760 mmHg

[ 熔点 ]:
252-254°C

[ 分子式 ]:
C₁₅H₁₄Cl₃N₅

[ 分子量 ]:
370.664

[ 闪点 ]:
249ºC

[ 精确质量 ]:
369.031494

[ PSA ]:
72.63000

[ LogP ]:
5.15890

[ 外观性状 ]:
灰白色固体

[ 蒸汽压 ]:
1.12E-09mmHg at 25°C

[ 储存条件 ]:
0-6°C

盐酸氯苯胍MSDS

详细MSDS(安全技术说明书)

盐酸氯苯胍毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: ME8651000

CHEMICAL NAME :: Guanidine, 1,3-bis((p-chlorobenzylidene)amino)-, monohydrochloride

CAS REGISTRY NUMBER :: 25875-50-7

LAST UPDATED :: 198910

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C15-H13-Cl2-N5.Cl-H

MOLECULAR WEIGHT :: 370.69

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 :: 390 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 21,794,1973

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 390 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JAFCAU Journal of Agricultural and Food Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1953- Volume(issue)/page/year: 23,724,1975

盐酸氯苯胍安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22

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

[ RTECS号 ]:
ME8651000

盐酸氯苯胍制备

对氯苯甲醛与N，N'-二氨基胍盐酸盐缩合制得。N，N'-二氨基胍盐酸盐（1,3-Diaminoguanidine monohydrochloride,CH7N5·HCl，[36062-19-8]）的制备：从硫氰酸钠出发，与水合肼加成、重排制得氨基硫脲。然后用硫酸二甲酯甲基化、肼解，制得N，N'-二氨基胍盐酸盐。最后，以氨化钙置换成N，N'-二氨基胍盐酸盐。

盐酸氯苯胍文献

Effect of subcutaneously administered diclazuril on the output of Eimeria species oocysts by experimentally infected rabbits.

Vet. Rec. 162(5) , 153-5, (2008)

The effect of subcutaneously injected diclazuril on the output of Eimeria species oocysts was studied in experimentally infected rabbits. Diclazuril was administered either prophylactically at 0.5, 1 ...

Use of antigen mimics to produce specific antibodies to anti-coccidial drugs.

J. Immunol. Methods 323(1) , 31-8, (2007)

A range of polyclonal antibodies was successfully produced to the coccidiostatic drugs diclazuril and robenidine. Initial attempts to make immunogenic complexes of both drugs were ineffective due to d...

Sensitivity of field isolates of Eimeria tenella to anticoccidial drugs in the chicken.

Res. Vet. Sci. 47(1) , 125-8, (1989)

Thirty isolates of Eimeria tenella obtained from broiler and breeder farms were examined for their sensitivity to anticoccidial drugs. All were sensitive to robenidine, 28 were sensitive to methyl ben...

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