泮库溴铵

泮库溴铵用途

【用途一】
非去极化肌肉松弛药，起效快，作用强。作用和氯化筒箭毒碱类似，但无神经节阻断和血压下降等副作用，也不会引起支气管痉挛，还可能兴奋心脏β受体或抗迷走作用使心率增快，血压上升及增加心输出量。用于外科手术或矫形手术麻醉的辅助用药，以得到充分的肌肉松弛作用，也可用于破伤风等惊厥性疾病。

泮库溴铵名称

[ CAS 号 ]:
15500-66-0

[ 中文名 ]:
泮库溴铵

[ 英文名 ]:
Pancuronium dibromide

[中文别名 ]:

巴活朗

[英文别名 ]:

EINECS 239-532-5
MFCD00079223
Pancuronium dibromide
Pancuronium Bromide

泮库溴铵生物活性

[ 描述 ]:

Pancuronium Dibromide是竞争性AChR拮抗剂,IC50为5.5 nM。

[ 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]. Fryer, A.D. and J. Maclagan, Pancuronium and gallamine are antagonists for pre- and post-junctional muscarinic receptors in the guinea-pig lung. Naunyn Schmiedebergs Arch Pharmacol, 1987. 335(4): p. 367-71.

[2]. Maestrone, E., et al., Extracellular pancuronium affects sodium current in chick embryo sensory neurones. Br J Pharmacol, 1994. 111(1): p. 283-7.

[3]. Lowenick, C.V., et al., Open channel and competitive block of nicotinic receptors by pancuronium and atracurium. Eur J Pharmacol, 2001. 413(1): p. 31-5.

[相关活性小分子]

泮库溴铵物理化学性质

[ 熔点 ]:
214 - 217ºC

[ 分子式 ]:
C₃₅H₆₀Br₂N₂O₄

[ 分子量 ]:
732.67000

[ 精确质量 ]:
730.29200

[ PSA ]:
52.60000

[ LogP ]:
0.03610

[ 外观性状 ]:
白色至近似于白色的结晶粉末,无气味

[ 储存条件 ]:
Desiccate at RT

泮库溴铵MSDS

详细MSDS(安全技术说明书)

泮库溴铵毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TN4930000

CHEMICAL NAME :: Piperidinium, 1,1'-(2-beta,16-beta-(3-alpha,17-beta-dihydroxy-5-alp ha-androstanylene)) bis(1-methyl-, dibromide, diacetate

CAS REGISTRY NUMBER :: 15500-66-0

LAST UPDATED :: 199504

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C35-H60-N2-O4.2Br

MOLECULAR WEIGHT :: 732.79

WISWESSER LINE NOTATION :: L E5 B666TJ A1 E1 FOV1 OOV1 G- AT6KTJ A1& P- AT6KTJ A1 &E 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 143 ug/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - chronic pulmonary edema Blood - hemorrhage

REFERENCE :: JATOD3 Journal of Analytical Toxicology. (Preston Pub. Inc., POB 48312, Niles, IL 60648) V.1- 1977- Volume(issue)/page/year: 4,275,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Parenteral

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 100 ug/kg

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

REFERENCE :: ADCHAK Archives of Disease in Childhood. (British Medical Journal, POB 560B, Kennebunkport, ME 04046) V.1- 1926- Volume(issue)/page/year: 59,73,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 1 mg/kg

TOXIC EFFECTS :: Behavioral - muscle weakness

REFERENCE :: PEDIAU Pediatrics. (American Academy of Pediatrics, P.O. Box 1034, Evanston, IL 60204) V.1- 1948- Volume(issue)/page/year: 77,848,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 202 mg/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 22,187,1970

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 479 ug/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 22,187,1970

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 436 ug/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 22,187,1970

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 153 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,353,1982

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 21200 ug/kg

TOXIC EFFECTS :: Behavioral - general anesthetic Behavioral - altered sleep time (including change in righting reflex) Lungs, Thorax, or Respiration - respiratory depression

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 22,187,1970

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 120 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 :: 167 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,353,1982

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 13 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,715,1971

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

ROUTE OF EXPOSURE :: Intracerebral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3500 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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 16 ug/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,353,1982

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - pig

DOSE/DURATION :: 67 ug/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Lungs, Thorax, or Respiration - cyanosis Nutritional and Gross Metabolic - body temperature increase

REFERENCE :: BJANAD British Journal of Anesthesia. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1923- Volume(issue)/page/year: 44,91,1972

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Bird - chicken

DOSE/DURATION :: 63 ug/kg

TOXIC EFFECTS :: Peripheral Nerve and Sensation - spastic paralysis with or without sensory change Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,715,1971 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 36 ug/kg

SEX/DURATION :: female 8-16 day(s) after conception

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

REFERENCE :: SKKNAJ Sankyo Kenkyusho Nempo. Annual Report of Sankyo Research Laboratories. (Sankyo K.K. Sogo Kenkyusho, 1-2-58 Hiro-machi, Shinagawa-ku, Tokyo 140, Japan) No.15- 1963- Volume(issue)/page/year: 22,187,1970 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4372 No. of Facilities: 63 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 9551 (estimated) No. of Female Employees: 8705 (estimated)

泮库溴铵安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
Missing Phrase - N15.00950417

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
3

[ RTECS号 ]:
TN4930000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

泮库溴铵制备

下列化合物和乙酸异丙烯醇酯反应，进行烯醇酯化，再用对氯过苯甲酸环氧化，氢氧化钾水解，并使其中一个环氧开环成羰基，接着和哌啶反应，硼氢化钠还原，乙酰化，最后和二分子的溴甲烷反应，季铵化成盐得到泮库溴铵。

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