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(+)-[[2Z-[2-[[(2S,3S)-2-[[(氨基羰基)氧代]甲基]-4-氧-1-硫代-3-吖丁啶基]氨基]-1-(2-氨基-4-噻唑基)-2-氧代亚乙基]氨基]氧代]乙酸二钠盐

用途

卡鲁南二钠是一种强效抗生素。卡鲁南二钠显示出抗菌活性。卡鲁南二钠诱发癫痫[1][2]。

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名称

[ CAS 号 ]:
86832-68-0

[ 中文名 ]:
(+)-[[2Z-[2-[[(2S,3S)-2-[[(氨基羰基)氧代]甲基]-4-氧-1-硫代-3-吖丁啶基]氨基]-1-(2-氨基-4-噻唑基)-2-氧代亚乙基]氨基]氧代]乙酸二钠盐

[ 英文名 ]:
(Z)-Carumonam

[中文别名 ]:

[英文别名 ]:

Ro 17-2301/006
Amasulin (TN)
Carumonam
CRMN
MFCD00875847
Mobactam
Carumonam disodium salt
Amasulin

生物活性

[ 描述 ]:

卡鲁南二钠是一种强效抗生素。卡鲁南二钠显示出抗菌活性。卡鲁南二钠诱发癫痫[1][2]。

[ 相关类别 ]:

研究领域 >> 感染

研究领域 >> 神经疾病

信号通路 >> 抗感染 >> 细菌

[体外研究]

卡鲁南二钠(0-100µg/mL)表现出抗菌活性,对大肠杆菌(头孢唑林敏感)、大肠杆菌(抗头孢唑林)、肺炎克雷伯杆菌(抗头孢唑啉)、肺炎克雷伯菌(耐头孢唑林的)、氧化克雷伯菌、阴沟肠杆菌、粘质沙雷氏菌(庆大霉素敏感)、粘质沙雷氏菌(抗庆大霉素)、普通变形杆菌、奇异变形杆菌、morganii变形杆菌、rettgeri变形杆菌、不稳定变形杆菌的微型计算机90值分别为 0.2、3.13、0.2、0.39、0.2、6.25、0.2、3.13、0.05、0.025、0.78、0.013、0.025µg/mL[1]

[体内研究]

卡鲁南二钠(1.31-6.89 mmol/kg；腹腔注射)诱导 DBA/2、瑞士和第57页小鼠癫痫发作[2]。动物模型：16-24g,42-48天DBA/2；18-28、42-48天Swiss和C57小鼠[2]剂量：1.31-6.89 mmol/kg给药：I.p.结果：DBA/2、Swiss和C5 7小鼠诱发癫痫发作。

[参考文献]

[1]. Imada A, et al. In vitro and in vivo antibacterial activities of carumonam (AMA-1080), a new N-sulfonated monocyclic beta-lactam antibiotic. Antimicrob Agents Chemother. 1985 May;27(5):821-7.

[2]. De Sarro A, et al. Comparative epileptogenic properties of two monobactam derivatives in C57, Swiss and DBA/2 mice. J Antimicrob Chemother. 1996 Sep;38(3):475-84.

物理化学性质

[ 密度 ]:
2.1±0.1 g/cm3

[ 熔点 ]:
250ºC (dec.)(lit.)

[ 分子式 ]:
C₁₂H₁₄N₆O₁₀S₂

[ 分子量 ]:
466.404

[ 精确质量 ]:
466.021271

[ PSA ]:
295.73000

[ LogP ]:
-2.26

[ 折射率 ]:
1.820

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AF2450000

CHEMICAL NAME :: Acetic acid, (((2-((2-(((aminocarbonyl)oxy)methyl)-4-oxo-1-sulfo-3 -azotidinyl)amino)-1- (2- amino-4-thiazolyl)-2-oxoethylidene)amino)oxy)-, disodium salt, (2S-(2-alpha,3-alpha(Z)))-

CAS REGISTRY NUMBER :: 86832-68-0

LAST UPDATED :: 199707

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C12-H14-N6-O10-S2.2Na

MOLECULAR WEIGHT :: 512.42

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 :: >10 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 gm/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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - hair

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4650 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8870 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 :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8870 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Nutritional and Gross Metabolic - body temperature decrease

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7740 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - dyspnea

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 gm/kg/5W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in bladder weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Metabolism (Intermediary) - other proteins

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 gm/kg/5W-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Blood - normocytic anemia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 10500 mg/kg/5W-I

TOXIC EFFECTS :: Liver - other changes Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 35 gm/kg/5W-I

TOXIC EFFECTS :: Liver - changes in liver weight Liver - other changes Kidney, Ureter, Bladder - changes in bladder weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 13 gm/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Fertility - abortion

MUTATION DATA

TYPE OF TEST :: DNA repair

TEST SYSTEM :: Bacteria - Bacillus subtilis

DOSE/DURATION :: 250 ug/disc

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14,3887,1986

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安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
S26-S36