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吡咯烷四磷酸

吡咯烷四磷酸用途

Pyronaridine tetraphosphate 是一种含甘露醇的抗疟疾药物,对耐药的镰状疟原虫,间日疟原虫, 卵形疟原虫和三日疟原虫均具有良好的疗效。

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吡咯烷四磷酸名称

[ CAS 号 ]:
76748-86-2

[ 中文名 ]:
4-[(7-氯-2-甲氧基-1,5-二氢吡啶并[3,2-b]喹啉-10-基)亚氨]-2,6-二(吡咯烷-1-基甲基)环己-2,5-二烯-1-酮磷酸盐 (1:4)

[ 英文名 ]:
Pyronaridine tetraphosphate

[英文别名 ]:

Pyronaridine phosphate
Pyronaridine Tetraphosphate
UNII-2T289F9ACO
Pyranoridine phosphate

吡咯烷四磷酸生物活性

[ 描述 ]:

Pyronaridine tetraphosphate 是一种含甘露醇的抗疟疾药物,对耐药的镰状疟原虫,间日疟原虫, 卵形疟原虫和三日疟原虫均具有良好的疗效。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 感染

[参考文献]

[1]. Vivas L, et al. Anti-malarial efficacy of pyronaridine and artesunate in combination in vitro and in vivo. Acta Trop. 2008 Mar;105(3):222-8.

[相关活性小分子]

吡咯烷四磷酸物理化学性质

[ 密度 ]:
1.357g/cm3

[ 沸点 ]:
657.2ºC at 760 mmHg

[ 熔点 ]:
233-236° (dec)

[ 分子式 ]:
C₂₉H₄₄ClN₅O₁₈P₄

[ 分子量 ]:
910.030

[ 闪点 ]:
351.3ºC

[ 精确质量 ]:
909.132019

[ PSA ]:
424.03000

[ LogP ]:
2.32020

[ 折射率 ]:
1.72

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
acetic acid: soluble5mg/mL

吡咯烷四磷酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SK4920000

CAS REGISTRY NUMBER :: 76748-86-2

LAST UPDATED :: 199509

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C29-H32-Cl-N5-O2.4H3-O4-P

MOLECULAR WEIGHT :: 910.11

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1368 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 :: 251 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 60 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 80 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2800 mg/kg/14D-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2320 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating female 2 week(s) pre-mating - 3 week(s) post-birth

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1100 mg/kg

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

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 990 mg/kg

SEX/DURATION :: female 7-9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 252 mg/kg

SEX/DURATION :: female 7-9 day(s) after conception

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

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Bacteria - Salmonella typhimurium

DOSE/DURATION :: 100 ug/plate

REFERENCE :: CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 3,51,1982

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吡咯烷四磷酸安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H361

[ 警示性声明 ]:
P280-P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
63-22-41

[ 安全声明 (欧洲) ]:
26-36/37-39

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

[ RTECS号 ]:
SK4920000

吡咯烷四磷酸文献

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Antimicrob. Agents Chemother. 59(1) , 170-7, (2014)

4-(tert-Butyl)-2-((tert-butylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)-phenol (JPC-2997) is a new aminomethylphenol compound that is highly active in vitro against the chloroquine-sensitive D6...

In vitro interactions between piperaquine, dihydroartemisinin, and other conventional and novel antimalarial drugs.

Antimicrob. Agents Chemother. 50 , 2883-2885, (2006)

In an in vitro assessment of antimalarial combinations, dihydroartemisinin (DHA) showed no interaction or was mildly antagonistic when combined with piperaquine, pyronaridine, or naphthoquine. Interac...

In vitro activities of piperaquine and other 4-aminoquinolines against clinical isolates of Plasmodium falciparum in Cameroon.

Antimicrob. Agents Chemother. 47 , 1391-1394, (2003)

The spread of chloroquine-resistant Plasmodium falciparum calls for a constant search for new drugs. The in vitro activity of piperaquine, a new Chinese synthetic drug belonging to the bisquinolines, ...

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