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烟拉文

烟拉文用途

Nicaraven是一种新颖的化学合成的羟基自由基清除剂。

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烟拉文名称

[ CAS 号 ]:
79455-30-4

[ 中文名 ]:
烟拉文

[ 英文名 ]:
Nicaraven

[中文别名 ]:

N,N'-亚丙基双烟酰胺

[英文别名 ]:

(+-)-N,N'-Propylenebis(nicotinamide)
1,2-Bis(nicotinamido)propane
N,N'-propane-1,2-diyldipyridine-3-carboxamide
Nicaraven
N,N'-1,2-Propanediyldinicotinamide
N,N'-Propylenenicotinamide
N,N'-(Propane-1,2-diyl)dinicotinamide
N,N'-Propane-1,2-diyldinicotinamide
(±)-N,N'-Propylenedinicotinamide
N,N'-propylenedinicotinamide

烟拉文生物活性

[ 描述 ]:

Nicaraven是一种新颖的化学合成的羟基自由基清除剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

[体外研究]

在健康志愿者血小板中,在浓度范围为350μM或更高的尼加拉文中,二磷酸腺苷(ADP)诱导的最大聚集率被显着抑制。 1.75 mM的nicaraven显着抑制胶原蛋白诱导的最大聚集率[1]。

[体内研究]

Nicaraven抑制肝脏脂质过氧化,改善肝脏和全身血流动力学和能量代谢,抑制肝脏酶释放,肝静脉血内皮素-1升高,组织学损伤和中性粒细胞浸润肝脏[1]。 Nicaraven增加骨髓和外周血中c-kit(+)干/祖细胞的数量,年龄匹配的非照射健康小鼠的恢复率约为60-90％。来自造血干/祖细胞的集落形成作为功能指标的效力完全受到nicaraven治疗的保护[2]。尼卡拉文的给药显着增加了数量,改善了集落形成能力,并减少了造血干/祖细胞的DNA损伤。与接受安慰剂的小鼠相比,给予尼卡拉的小鼠的尿氧水平8-氧代-2'-脱氧鸟苷(DNA氧化的标志物)显着降低。尼卡拉文的给药显着降低了小鼠血浆中炎性细胞因子IL-6和TNF-α的水平[3]。

[动物实验]

小鼠：为了研究尼卡拉文对造血干/祖细胞辐射损伤的保护作用及相关机制，12只小鼠每天接受1Gyγ射线连续5天（总共5Gy），然后每次暴露后不久，分别给予尼卡拉通（100mg / kg /天，Nicaraven组; n = 6）或仅盐水（安慰剂组; n = 6）腹膜内注射。在最后一次暴露后2天处死小鼠，收集尿液，血液和骨髓细胞样品并用于以下实验[3]。

[参考文献]

[1]. Komiya T, et al. A novel free radical scavenger, nicaraven, inhibits human platelet aggregation in vitro. Clin Neuropharmacol. 1999 Jan-Feb;22(1):11-4.

[2]. Yokota R, et al. A novel hydroxyl radical scavenger, nicaraven, protects the liver from warm ischemia and reperfusion injury. Surgery. 2000 Jun;127(6):661-9.

[3]. Ali H, et al. The potential benefits of nicaraven to protect against radiation-induced injury in hematopoietic stem/progenitor cells with relative low dose exposures.

[4]. Nicaraven attenuates radiation-induced injury in hematopoietic stem/progenitor cells in mice. PLoS One. 2013;8(3):e60023.

[相关活性小分子]

烟拉文物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
635.9±40.0 °C at 760 mmHg

[ 分子式 ]:
C₁₅H₁₆N₄O₂

[ 分子量 ]:
284.313

[ 闪点 ]:
338.4±27.3 °C

[ 精确质量 ]:
284.127319

[ PSA ]:
83.98000

[ LogP ]:
0.44

[ 外观性状 ]:
white solid

[ 蒸汽压 ]:
0.0±1.9 mmHg at 25°C

[ 折射率 ]:
1.584

[ 储存条件 ]:
-20℃

烟拉文毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US4667270

CHEMICAL NAME :: 3-Pyridinecarboxamide, N,N'-(1-methyl-1,2-ethanediyl)bis-

CAS REGISTRY NUMBER :: 79455-30-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 9

MOLECULAR FORMULA :: C15-H16-N4-O2

MOLECULAR WEIGHT :: 284.35

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 840 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

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: 23(Suppl 1),S9,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 590 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - hair

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: 23(Suppl 1),S5,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0029602

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

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: 23(Suppl 1),S13,1995 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 22680 mg/kg/4W-I

TOXIC EFFECTS :: Endocrine - changes in adrenal weight Blood - normocytic anemia Nutritional and Gross Metabolic - weight loss or decreased weight gain

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: 23(Suppl 1),S21,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 49140 mg/kg/26W-I

TOXIC EFFECTS :: Endocrine - changes in spleen weight Blood - normocytic anemia Blood - other changes

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: 23(Suppl 1),S69,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 9450 mg/kg/5W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Sense Organs and Special Senses (Eye) - effect, not otherwise specified

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: 23(Suppl 1),S41,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 26400 mg/kg/26W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Sense Organs and Special Senses (Eye) - effect, not otherwise specified

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: 23(Suppl 1),S103,1995 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 12 gm/kg

SEX/DURATION :: male 60 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

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: 23(Suppl 1),S155,1995

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烟拉文

烟拉文用途

烟拉文名称

烟拉文生物活性

烟拉文物理化学性质

烟拉文毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

烟拉文合成路线

详细合成路线

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