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维库溴铵

维库溴铵用途

【用途一】
用于外科手术麻醉的辅助药
【用途二】
中效非去极化肌肉松弛药，有较强的肌肉松弛作用。其持续时间较短，恢复快，且不引起支气管痉挛和血压下降，对心血管系统几无影响。用于气管插管及外科手术。

维库溴铵名称

[ CAS 号 ]:
50700-72-6

[ 中文名 ]:
维库溴铵

[ 英文名 ]:
Vecuronium bromide

[中文别名 ]:

[英文别名 ]:

MFCD00867762
EINECS 256-723-9
Vecuronium Bromide Hydrate
Vecuronium bromide
Norcuron

维库溴铵生物活性

[ 描述 ]:

Vecuronium bromide是一种中度持续时间的非去极化神经肌肉麻醉剂。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 胆碱受体

信号通路 >> 神经信号通路 >> 胆碱受体

研究领域 >> 神经疾病

[参考文献]

[1]. Meretoja, O.A., Vecuronium infusion requirements in pediatric patients during fentanyl-N2O-O2 anesthesia. Anesth Analg, 1989. 68(1): p. 20-4.

[2]. Agoston, S., et al., The neuromuscular blocking action of ORG NC 45, a new pancuronium derivative, in anaesthetized patients. A pilot study. Br J Anaesth, 1980. 52 Suppl 1: p. 53S-59S.

[3]. Shingu, K., et al., [Neuromuscular blocking effects of Org 9426 (rocuronium bromide); a comparative study with vecuronium bromide in Japanese patients]. Masui, 2006. 55(9): p. 1140-8.

[相关活性小分子]

维库溴铵物理化学性质

[ 熔点 ]:
227-229°C

[ 分子式 ]:
C₃₄H₅₇BrN₂O₄

[ 分子量 ]:
637.731

[ 精确质量 ]:
636.350159

[ PSA ]:
55.84000

[ LogP ]:
2.86660

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
水溶性：实际上不溶；易溶于：乙醇,二氯甲烷；极微溶：丙酮；不溶：乙醚

维库溴铵MSDS

详细MSDS(安全技术说明书)

维库溴铵毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TN4875000

CHEMICAL NAME :: Piperidinium, 1-(3-alpha,17-beta-diacetoxy-2-beta-piperidino-5-alph a-androstan-16-beta-y l)- 1-methyl-, bromide

CAS REGISTRY NUMBER :: 50700-72-6

LAST UPDATED :: 199206

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C34-H57-N2-O4.Br

MOLECULAR WEIGHT :: 637.84

WISWESSER LINE NOTATION :: L E5 B666TJ A1 E1 FOV1 OOV1 G- AT6KTJ A1& P- AT6NTJ &E

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 130 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change

REFERENCE :: AACRAT Anesthesia and Analgesia (New York). (Elsevier Science Pub. Co., Inc., 52 Vanderbilt Ave., New York, NY 10017) V.36- 1957- Volume(issue)/page/year: 66,188,1987

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 123 ug/kg/40M-I

TOXIC EFFECTS :: Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic)

REFERENCE :: BJANAD British Journal of Anesthesia. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1923- Volume(issue)/page/year: 57,807,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 455 mg/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2630 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1730 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 41 mg/kg

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 142 ug/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,465,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 148 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 51 ug/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,807,1986

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

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3600 ng/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 32,465,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6300 ug/kg/5W-C

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,817,1986

维库溴铵安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-37/39

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

[ 海关编码 ]:
2933399090

维库溴铵制备

1.其合成和潘库溴铵相似，仅在最后一步中，和一分子的溴甲烷反应，生成单季铵盐而得到维库溴铵。

2. 17-乙酰氧基-5α-雄甾-2,16-二烯的制备
在反应瓶中加入5α-雄甾-2-烯-17-酮150g(0.55mol)、甲苯500ml、对甲苯磺酸13g(0.07mol)和乙酸异丙烯酯73ml,加热搅拌回流,在回流下反应37h.减压蒸除溶剂至干,剩余物加二氯甲烷350ml溶解,用水(300ml×3)洗涤至中性,无水MgSO4干燥,过滤,滤液减压蒸干,剩余物用甲醇600ml重结晶,活性炭脱色,过滤,滤液冷却析晶,得白色粉末17-乙酰氧基-5α-雄甾-2,16-二烯138.5g,收率80%,mp86~88ºC.

3. 2α,3α,16α,17α-二环氧-17β-乙酰氧基-5α-雄甾烷的制备
在反应瓶中加入17-乙酰氧基-5α-雄甾-2,16-二烯60g(0.19mol)和乙醚525ml搅拌溶解,于室温下搅拌滴加间氯过氧苯甲酸76g(纯度86%,0.38mol)和乙醚330ml的溶液,在3h内加完.滴毕,室温搅拌反应18h.反应毕,蒸去乙醚,剩余物加二氯甲烷700ml溶解,用1.25mol/LNaOH水溶液洗涤2次,然后水洗至中性,无水MgSO4干燥,过滤,滤液浓缩至干,用乙醚重结晶,得纯品2α,3α,16α,17α-二环氧-17β-乙酰氧基-5α-雄甾烷36.8g,收率56%,mp164~167ºC.

4. 2β,16β-二(1-哌啶基)-5α-雄甾烷-3α-羟基-17-酮的制备
在反应瓶中加入2α,3α,16α,17α-二环氧-17β-乙酰氧基-5α-雄甾烷25g(0.07mol)和哌啶223ml,搅拌加热回流120h.减压蒸干,加水析出产物,过滤,滤饼用水洗,加入2mol/L盐酸75ml,调至pH1~2,过滤,滤液加入2.5mol/LNaOH溶液60ml,立即析出白色固体,过滤,滤饼溶于二氯甲烷90ml,水洗至中性,无水MgSO4干燥,过滤,滤液减压蒸除溶剂,固体用丙酮重结晶,得白色粉末22.6g,收率71%,mp176~180ºC.(文献[6]报道mp179~185ºC,收率66%)

5. 2β,16β-二(1-哌啶基)-5α-雄甾烷-3α,17β-二醇的制备
在反应瓶中加入2β,16β-二(1-哌啶基)-5α-雄甾烷-3α-羟基-17-酮12g(0.03mol)、二氯甲烷15.6ml和甲醇46.8ml,搅拌下15min内加入硼氢化钾4.7g(0.09mol)加料后立即开始析出白色固体,室温搅拌反应18h.过滤,滤饼用水洗,得白色固体2β,16β-二(1-哌啶基)-5α-雄甾烷-3α,17β-二醇18.2g,收率96%,mp152~158ºC.(文献[6]报道mp155~158ºC,收率94%)

6. 2β,16β-二(1-哌啶基)-3α,17β-乙酰氧基-5α-雄甾烷的制备
装好无水氯化钙干燥管,向瓶中加入干燥的二氯甲烷40ml、2β,16β-二(1-哌啶基)-5α-雄甾烷-3α,17β-二醇4.2g(0.9mmol)和乙酰氯1.98ml,室温搅拌反应25h.用饱和Na2CO3水溶液洗至水层呈中性,有机层用无水MgSO4干燥,过滤,滤液浓缩至干,得白色固体2β,16β-二(1-哌啶基)-3α,17β-乙酰氧基-5α-雄甾烷4.2g,收率84.5%,mp136.6~138.8ºC.

7. 维库溴铵的合成
在反应瓶中加入2β,16β-二(1-哌啶基)-3α,17β-乙酰氧基-5α-雄甾烷0.8g(1.5mmol)、溴甲烷0.17g(1.8mmol)和乙腈5ml,在N2保护下,回流搅拌反应40h.将反应液浓缩至干,剩余物经氧化铝柱色谱,用异丙醇/乙酸乙酯(体积比1:1)洗脱,经后处理得油状物,用丙酮10ml溶解后,在异丙醚中析出白色固体维库溴铵0.51g,收率53.2%,mp226.5~228ºC..(文献[6]报道mp227~229ºC)

维库溴铵海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

维库溴铵文献

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Am. J. Respir. Cell. Mol. Biol. 50(6) , 1031-9, (2014)

Disturbances in respiration are common and debilitating features of Rett syndrome (RTT). A previous study showed that the 5-HT1a receptor agonist (R)-(+)-8-hydroxy-dipropyl-2-aminotetralin hydrobromid...

Developing dual hemofiltration plus cardiopulmonary bypass in rodents.

J. Surg. Res. 195(1) , 196-203, (2015)

Emerging therapies for prolonged cardiac arrest (CA) include advanced circulatory interventions like emergency cardiopulmonary bypass (ECPB) and continuous venovenous hemofiltration (CVVHF). However, ...

Population of sensory neurons essential for asthmatic hyperreactivity of inflamed airways.

Proc. Natl. Acad. Sci. U. S. A. 111(31) , 11515-20, (2014)

Asthma is a common debilitating inflammatory lung disease affecting over 200 million people worldwide. Here, we investigated neurogenic components involved in asthmatic-like attacks using the ovalbumi...

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