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奈替米星硫酸盐

奈替米星硫酸盐用途

Netilmicin硫酸盐是氨基糖苷类抗生素化合物。

奈替米星硫酸盐名称

[ CAS 号 ]:
56391-57-2

[ 中文名 ]:
硫酸奈替米星

[ 英文名 ]:
Netilmicin sulfate

[中文别名 ]:

[英文别名 ]:

certomycin
EINECS 260-147-3
1-N-Ethylsisomicin sulfate salt
Netilmicin sulfate
Zetamicin
MFCD01311715
Netillin
Netilmicin sulfate salt
UNII-S741ZJS97U
Nettacin

奈替米星硫酸盐生物活性

[ 描述 ]:

Netilmicin硫酸盐是氨基糖苷类抗生素化合物。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 细菌

研究领域 >> 感染

[参考文献]

[1]. Campoli-Richards DM, et al. Netilmicin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1989 Nov;38(5):703-56.

[2]. Adams E, et al. Determination of netilmicin sulfate by liquid chromatography with pulsed electrochemical detection. J Chromatogr A. 1998 Jul 3;812(1-2):151-7.

[3]. Ciftci M, et al. Effects of some drugs on rat erythrocyte 6-phosphogluconate dehydrogenase: an in vitro and in vivo study. Pol J Pharmacol. 2002 May-Jun;54(3):275-80.

[相关活性小分子]

奈替米星硫酸盐物理化学性质

[ 密度 ]:
1.32 g/cm3

[ 沸点 ]:
684.3ºC at 760 mmHg

[ 熔点 ]:
>194ºC (dec.)

[ 分子式 ]:
C₂₁H₄₁N₅O_7.5/₂H₂O₄S

[ 分子量 ]:
720.78

[ 闪点 ]:
367.7ºC

[ PSA ]:
814.36000

[ LogP ]:
1.50400

[ 外观性状 ]:
白色至灰白色粉末

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: soluble10mg/mL | Soluble in water

奈替米星硫酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WK2286000

CAS REGISTRY NUMBER :: 56391-57-2

LAST UPDATED :: 199604

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C21-H41-N5-O7.5/2H2-O4-S

MOLECULAR WEIGHT :: 720.80

WISWESSER LINE NOTATION :: T6O BUTJ B1Z EZ FO- BL6TJ AZ CQ EM2 DO- BT6OTJ CQ DM1 EQ E1 ..H2.S-O4

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

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 36,1249,1985

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 231 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 169 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 40700 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 167 mg/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 189 mg/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage)

REFERENCE :: AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 10,827,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 68900 ug/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 22 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 63100 ug/kg

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

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 420 mg/kg/14D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 375 mg/kg/30D-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition Kidney, Ureter, Bladder - changes in bladder weight

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,461,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1365 mg/kg/26W-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - interstitial nephritis Kidney, Ureter, Bladder - changes in bladder weight Blood - pigmented or nucleated red blood cells

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,499,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 138 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 550 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,614,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 650 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,643,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 455 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: JJANAX Japanese Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo 141, Japan) V.21- 1968- Volume(issue)/page/year: 35,659,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4347 No. of Facilities: 25 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 2440 (estimated) No. of Female Employees: 1459 (estimated)

奈替米星硫酸盐安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H312 + H332-H360

[ 警示性声明 ]:
P201-P261-P280-P308 + P313

[ 个人防护装备 ]:
Eyeshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R60;R20/21/22

[ 安全声明 (欧洲) ]:
S53-S36/37/39-S45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
WK2286000

[ 海关编码 ]:
2942000000

奈替米星硫酸盐制备

参考文献[12~15]推荐如下路线和方法$

(1)3,2’,6’-三（N-乙酰）西索米星（023-2）的制备

在反应瓶中加入二甲基甲酰胺（DMF）/水的混合溶液100ml(DMF/水,体积比6:2)和乙酸铜5.5g(0.03mol),搅拌悬浮,再加入西索米星(023-1)4.5g(0.01mol),搅拌下加三乙胺调至PH8.5~10.5,在搅拌30min后降温至5 ºC 慢慢滴加乙酸酐3.1g(0.03mol)的3.5mlDMF溶液,滴加时控温在0~10 ºC ,在强烈搅拌下,并不断用三乙胺调节反应液的PH保持8.5~10.5,滴毕,室温(25 ºC)搅拌反应30min~1h.用TLC跟踪显示反应达终点后(如果未达到终点应补乙酸酐的DMF溶液适量),将反应液减压下浓缩,浓缩液用水稀释,冷至(0~10 ºC )保持4h.过滤去固体,滤液用阳离子交换树脂处理,氨水洗脱等处理后得023-2 5.2g,收率90%.

(2)5,2’’,4’’-三(三甲基硅)-3,2’,6’-三(N-乙酰)-西索米星(023-3)的制备

在反应瓶中加入023-2 10g(17.45mmol)、1,2-二甲氧基乙烷(DMF)100ml,搅拌溶解,再加入三甲基氯硅烷25ml(21.15g,194mmol),加热至50 ºC ,搅拌反应16h(在保持50~55 ºC 下)减压蒸除DME,得黄色固体023-3 13.5g,收率93.6%左右,含量91%.经硅胶柱色谱纯化可制得分析试样.

(3)5,2’’,4’’-三(三甲基硅)-1-乙基氨基-3,2’,6’-三(N-乙酰)西索米星(023-5)的制备

在反应瓶中加入化合物023-3 8g(9.5mmol)和水80ml,搅拌溶解,用4mol/L盐酸调至PH6.降温至15 ºC ,加入乙醛2.2ml(1.72g,39mmol),搅拌反应30min,生成亚胺化合物023-4溶液.将NaBH4的水溶液5ml[1g(26.47mmol)NaBH4溶于5ml水]匀速滴入上述含023-4的溶液，并用0.5mol/L盐酸严格控制PH6.继续反应30min,加入0.05mol/L硼砂溶液20ml(PH9.5)继续搅拌1h.得023-5的溶液,含量85%,备用.

(4)O-3-脱氧-4-C-甲基-3-(甲氨基)-B-L-阿拉伯吡喃糖苷(1—6)-O-[2,6-二氨基-2,3,4,6-四脱氧-a-D-甘油己糖-4-烯醇型吡喃糖苷基-(1—4)]-2-脱氧-N’-乙基-D-链霉胺硫酸盐(硫酸奈替米星)(023)的合成

在反应瓶中加入上步制备的含化合物023-5的溶液、珠粒状固体NaOH2g(50mmol)和Na2CO3 2.7g(25.5mmol),搅拌溶解,油浴加热升温至110 ºC ,在该温度下搅拌回流36h.降温至10~15 ºC,加入10mol/L H2SO4调反应液PH至6.5~7.0,抽滤,滤液即为奈替米星游离碱的澄清溶液,含量80%.

在上述澄清溶液中加入阳离子交换树脂,搅拌混合充分后,过滤,用7%氨水洗脱,洗脱液浓缩后用甲醇溶解,再上硅胶柱色谱分离纯化,用氯仿/甲醇/水(40:20:7)洗脱分离.将洗脱液减压浓缩至约10ml,加入活性炭0.5g,恒温水浴加热至50 ºC ,脱色30min.抽滤,滤液用10mol/L H2SO4调至PH3.5~5.5,匀速滴至无水乙醇300ml中,3h后抽滤,滤饼干燥,得023 5.93g,收率78.7,含量在97%以上,符合《中国药典》(2005年版)质量标准.该品为非结晶性固体(冷冻干燥).

奈替米星硫酸盐海关

[ 海关编码 ]: 2942000000

奈替米星硫酸盐文献

Polyhydroxyethylaspartamide-based micelles for ocular drug delivery.

Int. J. Pharm. 378(1-2) , 177-86, (2009)

In this paper three copolymers of polyhydroxyethylaspartamide (PHEA), bearing in the side chains polyethylene glycol (PEG) and/or hexadecylamine (C(16)) (PHEA-PEG, PHEA-PEG-C(16) and PHEA-C(16) respec...

Ocular penetration of topical antibiotics: study on the penetration of chloramphenicol, tobramycin and netilmicin into the anterior chamber after topical administration.

Clin. Experiment. Ophthalmol. 41(7) , 644-7, (2013)

To compare penetration in the aqueous humour of topically applied antibiotics.Randomized prospective study, Department of Ophthalmology, University of Perugia, ItalyPatients undergoing cataract surger...

Netilmicin-induced modulation of melanogenesis in HEMa-LP melanocytes.

Acta Pol. Pharm. 70(5) , 803-8, (2013)

It is known that aminoglycoside antibiotics bind well to melanin biopolymer, but the relation between their affinity to melanin and ototoxicity is not well established. The aim of this work was to exa...

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