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长春西汀

长春西汀用途

Vinpocetine(Cavinton; Ethyl apovincaminate) 是PDE1选择性抑制剂,IC50为21 μM,同时也是压敏钠离子通道。

长春西汀名称

[ CAS 号 ]:
42971-09-5

[ 中文名 ]:
长春西汀

[ 英文名 ]:
Vinpocetine

[中文别名 ]:

[英文别名 ]:

EINECS 256-028-0
vinpocetine
MFCD00211233
Eburnamenine-14-carboxylic acid ethyl ester

长春西汀生物活性

[ 描述 ]:

Vinpocetine(Cavinton; Ethyl apovincaminate) 是PDE1选择性抑制剂,IC50为21 μM,同时也是压敏钠离子通道。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 磷酸二酯酶(PDE)

信号通路 >> 跨膜转运 >> 钠通道

研究领域 >> 心血管疾病

研究领域 >> 神经疾病

[参考文献]

[1]. Patyar S, et al. Role of vinpocetine in cerebrovascular diseases.Pharmacol Rep. 2011;63(3):618-28.

[2]. Vaizova OE, et al. Endothelium-protective effects of vinpocetine, pentoxifylline and enalapril in patients with chronic brain ischemia.Eksp Klin Farmakol. 2011;74(4):10-3.

[3]. El-Laithy HM, et al. Novel sugar esters proniosomes for transdermal delivery of vinpocetine: preclinical and clinical studies.Eur J Pharm Biopharm. 2011 Jan;77(1):43-55.

[4]. Alexandre E. Medina Vinpocetine as a potent antiinflammatory agent PNAS June 1, 2010 vol. 107 no. 22 9921-9922

[5]. Kye-Im Jeon et al. Vinpocetine inhibits NF-κB-dependent inflammation via an IKK-dependent but PDE-independent mechanism PNAS May 25, 2010 vol. 107 no. 21 9795-9800

[相关活性小分子]

长春西汀物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
419.5±45.0 °C at 760 mmHg

[ 熔点 ]:
147-153ºC dec

[ 分子式 ]:
C₂₂H₂₆N₂O₂

[ 分子量 ]:
350.454

[ 闪点 ]:
207.5±28.7 °C

[ 精确质量 ]:
350.199432

[ PSA ]:
34.47000

[ LogP ]:
5.14

[ 外观性状 ]:
白色结晶固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.666

[ 储存条件 ]:
室温

长春西汀MSDS

长春西汀毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JW4792000

CHEMICAL NAME :: Eburnamenine-14-carboxylic acid, ethyl ester, (3-alpha,16-alpha)-

CAS REGISTRY NUMBER :: 42971-09-5

LAST UPDATED :: 199806

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C22-H26-N2-O2

MOLECULAR WEIGHT :: 350.50

WISWESSER LINE NOTATION :: T D6 B5666 2AB S CN MN&&TTTJ Q2 SVO2

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 :: 503 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,1938,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 119 mg/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: 35,1919,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 32 mg/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: 35,1919,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 534 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,1938,1976

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 117 mg/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: 35,1919,1984

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/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: 35,1919,1984 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4375 mg/kg/5W-I

TOXIC EFFECTS :: Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume increased 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: 10,1847,1982

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 14560 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - urine volume increased Endocrine - changes in adrenal weight

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: 10,1847,1982 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: female 14-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,1938,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 450 mg/kg

SEX/DURATION :: female 7-15 day(s) after conception

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 26,1938,1976

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/kg

SEX/DURATION :: female 7-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

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: 11,1125,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1 gm/kg

SEX/DURATION :: female 7-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

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: 11,1125,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 65 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - abortion

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: 11,3585,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1750 mg/kg

SEX/DURATION :: female 14 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes

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: 11,3585,1983

长春西汀安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
JW4792000

[ 海关编码 ]:
2933990090

长春西汀合成路线

长春西汀上下游产品

长春西汀上游产品

长春西汀下游产品

长春西汀制备

长春西汀可以从夹竹桃科植物小长春花(Vinca minor)中提取到的(+)-长春胺(Vincamine)为原料，经脱水为阿扑文卡明(Apovincamine),再水解得其酸(Apovincaminic acid).该酸(1.0g,0.003mol)和0.17g氢氧化钾溶于80ml干燥乙醇,加入溴乙烷(0.4g,0.0036mol),回流3h。反应完毕后，冷却，蒸发至干。剩余物溶于500ml2％的硫酸，并调PH值至8。用二氯甲烷提取，碳酸钾干燥，蒸发去绝大部分的二氯甲烷后，加入乙醇。在0℃放置过夜，过滤收集析出的结晶，用冷乙醇洗，干燥，得0.66g长春西汀。

也可从夹竹桃科植物柳叶小甘草的叶或长春花种子提取到的(-)-水甘草碱为原料，经多步合成制得。全合成法是以色胺为原料，经如下反应得到。

长春西汀海关

[ 海关编码 ]: 2933990090

[ 中文概述 ]:
2933990090. 其他仅含氮杂原子的杂环化合物. 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, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

长春西汀文献

Vinpocetine and α-tocopherol prevent the increase in DA and oxidative stress induced by 3-NPA in striatum isolated nerve endings.

J. Neurochem. 124(2) , 233-40, (2013)

Vinpocetine is a neuroprotective drug that exerts beneficial effects on neurological symptoms and cerebrovascular disease. 3-nitropropionic acid (3-NPA) is a toxin that irreversibly inhibits succinate...

[Current possibilities of the correction of oxidative stress in acute brain ischaemia].

Zh. Nevrol. Psikhiatr. Im. S. S. Korsakova 112(11) , 79-82, (2012)

Piracetam and vinpocetine ameliorate rotenone-induced Parkinsonism in rats.

Indian J. Pharmacol. 44(6) , 774-9, (2012)

To evaluate the neuroprotective effect of the nootropic drugs, piracetam (PIR) and vinpocetine (VIN), in rotenone-induced Parkinsonism in rats.Sixty male rats were divided into 6 groups of 10 rats eac...

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