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吡喹酮

吡喹酮用途

Praziquantel有较好的抗蠕虫(扁形虫)效果。

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吡喹酮作用

本品主要通过5-HT样作用使宿主体内血吸虫、绦虫产生痉挛性麻痹脱落，对多数绦虫成虫和未成熟虫体都有较好效果，同时能影响虫体肌细胞内钙离子通透性，使钙离子内流增加，抑制肌浆网钙泵的再摄取，虫体肌细胞内钙离子含量大增，使虫体麻痹脱落。

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吡喹酮名称

[ CAS 号 ]:
55268-74-1

[ 中文名 ]:
吡喹酮

[ 英文名 ]:
Praziquantel

[中文别名 ]:

[英文别名 ]:

Distocide
WarMnil
embay8440
droncit
rac-praziquantel
Prazinon
Cesol
biltricide
EINECS 259-559-6
Azinox

吡喹酮生物活性

[ 描述 ]:

Praziquantel有较好的抗蠕虫(扁形虫)效果。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[参考文献]

[1]. Coeli, R., et al., Praziquantel treatment decreases Schistosoma mansoni genetic diversity in experimental infections. PLoS Negl Trop Dis, 2013. 7(12): p. e2596.

[2]. Mekonnen, A., et al., Efficacy of Praziquantel against Schistosoma haematobium in Dulshatalo village, western Ethiopia. BMC Res Notes, 2013. 6: p. 392.

[相关活性小分子]

吡喹酮物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
544.1±50.0 °C at 760 mmHg

[ 熔点 ]:
136-142ºC

[ 分子式 ]:
C₁₉H₂₄N₂O₂

[ 分子量 ]:
312.406

[ 闪点 ]:
254.6±22.5 °C

[ 精确质量 ]:
312.183777

[ PSA ]:
40.62000

[ LogP ]:
2.44

[ 外观性状 ]:
白色或几乎白色结晶粉末

[ 蒸汽压 ]:
0.0±1.5 mmHg at 25°C

[ 折射率 ]:
1.615

[ 储存条件 ]:
通风低温干燥

[ 水溶解性 ]:
ethanol: soluble5mg/mL | Freely soluble in ethanol or dichloromethane. Slightly soluble in water

吡喹酮MSDS

吡喹酮毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UQ4150000

CHEMICAL NAME :: 4H-Pyrazino(2,1-a)isoquinolin-4-one, 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-

CAS REGISTRY NUMBER :: 55268-74-1

BEILSTEIN REFERENCE NO. :: 0761557

LAST UPDATED :: 199710

DATA ITEMS CITED :: 22

MOLECULAR FORMULA :: C19-H24-N2-O2

MOLECULAR WEIGHT :: 312.45

WISWESSER LINE NOTATION :: T B666 DN FVNTT&J DV- AL6TJ

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 :: 2840 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 586 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >16 gm/kg

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

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2454 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 376 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7172 mg/kg

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

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >200 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 1050 mg/kg

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

MUTATION DATA

TYPE OF TEST :: Mutation test systems - not otherwise specified

TEST SYSTEM :: Rodent - hamster Liver

DOSE/DURATION :: 2700 umol/L

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 46,461,1990 *** REVIEWS *** TOXICOLOGY REVIEW CHHTAT Zhonghua Yixue Zazhi. Chinese Medical Journal. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1915- Suspended 1967-72. Volume(issue)/page/year: 61,52,1981

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吡喹酮安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
F: Flammable;C: Corrosive;

[ 风险声明 (欧洲) ]:
R11

[ 安全声明 (欧洲) ]:
16-26-36/37/39-45

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

[ WGK德国 ]:
1

[ RTECS号 ]:
UQ4150000

[ 海关编码 ]:
2933790090

吡喹酮合成路线

吡喹酮上下游产品

吡喹酮上游产品

吡喹酮下游产品

吡喹酮制备

以苯乙胺为原料，用氯乙酰氯进行酰化后，再以苯二甲酰胺钾进行胺化反应引入氨基，在三氯氧磷的作用下环合得3，4-二氢异喹啉衍生物，经氢化、水解得到1-氨甲基四氢喹啉，先后用环己甲酰氯和氯乙酰氯酰化，最后脱氯化氢环合得到吡喹酮。

也可以异喹啉为原料，经Reissert反应，在l位引入氰基和氮上苯甲酰化，然后氢化，同时苯甲酰基转移到侧链的氨基上，再在环上的氨基上引入氯乙酰基，然后环合、水解、环己甲酰化得吡喹酮。

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吡喹酮海关

[ 海关编码 ]: 2933790090

[ 中文概述 ]:
2933790090 其他内酰胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:9.0% 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 ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

吡喹酮文献

Cholesterol lowering effect in the gall bladder of dogs by a standardized infusion of Herniaria hirsuta L.

J. Ethnopharmacol. 169 , 69-75, (2015)

Infusions of Herniaria hirsuta L., Herniaria glabra L. and Herniaria fontanesii J.Gay are well known in Moroccon folk medicine for the treatment of biliary dyskinesia, (uro)lithiasis or as a diuretic....

Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.

Chem. Res. Toxicol. 23 , 171-83, (2010)

Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental...

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

更多文献

吡喹酮

吡喹酮用途

吡喹酮作用

吡喹酮名称

吡喹酮生物活性

吡喹酮物理化学性质

吡喹酮MSDS

详细MSDS(安全技术说明书)

吡喹酮毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

吡喹酮安全信息

吡喹酮合成路线

详细合成路线

吡喹酮上下游产品

吡喹酮上游产品

吡喹酮下游产品

吡喹酮制备

吡喹酮海关

吡喹酮文献

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