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尼莫唑

尼莫唑用途

Nimorazole (K-1900) 是抗感染类硝基咪唑。

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尼莫唑名称

[ CAS 号 ]:
6506-37-2

[ 中文名 ]:
尼莫拉唑

[ 英文名 ]:
Nimorazole

[中文别名 ]:

[英文别名 ]:

Morpholine, 4-[2- (5-nitroimidazol-1-yl)ethyl]-
Nulogyl
4-[2-(5-Nitroimidazol-1-yl)ethyl]morpholine
1-(β-Morpholinoethyl)-5-nitroimidazole
Nimorazole
Morpholine, 4-[2-(5-nitro-1H-imidazol-1-yl)ethyl]-
Acterol
Acterol forte
Esclama
Nimorazol

尼莫唑生物活性

[ 描述 ]:

Nimorazole (K-1900) 是抗感染类硝基咪唑。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[ 靶点 ]

Antiparasitic

[体外研究]

尼莫拉唑显着改善了声门上咽和咽部肿瘤放射治疗的效果,并且可以给予没有重大副作用[1,2]。尼莫唑是唯一一种在头颈癌的随机对照试验中显示出显着效果的药物[3]。

[参考文献]

[1]. Overgaard, J., et al., A randomized double-blind phase III study of nimorazole as a hypoxic radiosensitizer of primary radiotherapy in supraglottic larynx and pharynx carcinoma. Results of the Danish Head and Neck Cancer Study (DAHANCA) Protocol 5-85. Radiother Oncol, 1998. 46(2): p. 135-46.

[2]. Roy, R.B., S.M. Laird, and L. Heasman, Treatment of trichomoniasis in the female. A comparison of metronidazole and nimorazole. Br J Vener Dis, 1975. 51(4): p. 281-4.

[3]. Henk, J.M., K. Bishop, and S.F. Shepherd, Treatment of head and neck cancer with CHART and nimorazole: phase II study. Radiother Oncol, 2003. 66(1): p. 65-70.

[相关活性小分子]

尼莫唑物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
443.0±35.0 °C at 760 mmHg

[ 分子式 ]:
C₉H₁₄N₄O₃

[ 分子量 ]:
226.232

[ 闪点 ]:
221.7±25.9 °C

[ 精确质量 ]:
226.106583

[ PSA ]:
76.11000

[ LogP ]:
-0.08

[ 外观性状 ]:
light yellow solid

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.637

[ 储存条件 ]:
-20℃

尼莫唑毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QE7400000

CHEMICAL NAME :: Morpholine, 4-(2-(5-nitroimidazol-1-yl)ethyl)-

CAS REGISTRY NUMBER :: 6506-37-2

LAST UPDATED :: 199612

DATA ITEMS CITED :: 20

MOLECULAR FORMULA :: C9-H14-N4-O3

MOLECULAR WEIGHT :: 226.27

WISWESSER LINE NOTATION :: T6N DOTJ A2- AT5N CNJ ENW

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 :: 1540 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1200 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1090 mg/kg

TOXIC EFFECTS :: Behavioral - excitement

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1530 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - tremor Behavioral - ataxia

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1200 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Lungs, Thorax, or Respiration - respiratory stimulation

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1140 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14 gm/kg/5W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72800 mg/kg/26W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9275 mg/kg/5W-I

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2800 mg/kg

SEX/DURATION :: female 8-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 700 mg/kg

SEX/DURATION :: female 8-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 700 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4200 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 2800 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - live birth index (measured after birth)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 700 mg/kg

SEX/DURATION :: female 7-13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Microorganism - not otherwise specified

DOSE/DURATION :: 250 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 26,483,1974

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尼莫唑安全信息

[ 海关编码 ]:
2934999090

尼莫唑海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

尼莫唑