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盐酸卤泛群

盐酸卤泛群用途

Halofantrine hydrochloride (SKF-102886)是一种通过抑制人ERG通道来延迟整流钾电流的阻滞剂,是一种有效的抗疟疾药。

盐酸卤泛群名称

[ CAS 号 ]:
36167-63-2

[ 中文名 ]:
盐酸卤泛群

[ 英文名 ]:
Halofantrine hydrochloride

[中文别名 ]:

卤泛群盐酸盐

[英文别名 ]:

UNII:2B7ENL644K
MFCD00879136
EINECS 252-895-4
Halofantrine hydrochloride
UNII:H77DL0Y630

盐酸卤泛群生物活性

[ 描述 ]:

Halofantrine hydrochloride (SKF-102886)是一种通过抑制人ERG通道来延迟整流钾电流的阻滞剂,是一种有效的抗疟疾药。

[ 相关类别 ]:

信号通路 >> 抗感染 >> 寄生物

研究领域 >> 感染

[ 靶点 ]

Malaria[1].HERG channel[2].

[参考文献]

[1]. Krishna S, et al. Pharmacokinetics, efficacy and toxicity of parenteral halofantrine in uncomplicated malaria. Br J Clin Pharmacol. 1993 Dec;36(6):585-91.

[2]. Tie, H., et al., Inhibition of HERG potassium channels by the antimalarial agent halofantrine. Br. J. Pharmacol. 130, 1967-1975, (2000) Traebert.

盐酸卤泛群物理化学性质

[ 密度 ]:
1.244g/cm3

[ 沸点 ]:
596.2ºC at 760mmHg

[ 分子式 ]:
C₂₆H₃₁Cl₃F₃NO

[ 分子量 ]:
536.885

[ 闪点 ]:
314.4ºC

[ 精确质量 ]:
535.142334

[ PSA ]:
23.47000

[ LogP ]:
9.44630

[ 储存条件 ]:
2-8°C

盐酸卤泛群毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SF7790000

CHEMICAL NAME :: 9-Phenanthrenemethanol, 1,3-dichloro-alpha-(2-(dibutylamino)ethyl)-6-(trifluo romethyl)-, hydrochloride

CAS REGISTRY NUMBER :: 36167-63-2

LAST UPDATED :: 199503

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C26-H30-Cl2-F3-N-O.Cl-H

MOLECULAR WEIGHT :: 536.93

WISWESSER LINE NOTATION :: L B666J DG FG IYQ2N4&4 MXFFF &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7143 ug/kg

TOXIC EFFECTS :: Liver - liver function tests impaired Kidney, Ureter, Bladder - urine volume decreased Kidney, Ureter, Bladder - hematuria

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,909,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 18 mg/kg/D

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Gastrointestinal - other changes

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 5,547,1980

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 72 mg/kg/3D-I

TOXIC EFFECTS :: Cardiac - cardiomyopathy including infarction

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 341,1054,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 7143 ug/kg

TOXIC EFFECTS :: Liver - jaundice, other or unclassified Kidney, Ureter, Bladder - urine volume decreased Blood - other hemolysis with or without anemia

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 340,909,1992

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 3400 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2050 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: ACTRAQ Acta Tropica. (Schwabe & Co., Steintorstr. 13, CH-4010 Basel, Switzerland) V.1- 1944- Volume(issue)/page/year: 37,232,1980 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 240 mg/kg

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

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

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 4,85,1984

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 120 mg/kg

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

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

REFERENCE :: TOXID9 Toxicologist. (Soc. of Toxicology, Inc., 475 Wolf Ledge Parkway, Akron, OH 44311) V.1- 1981- Volume(issue)/page/year: 4,85,1984

盐酸卤泛群安全信息

[ 危害声明 ]:
H413

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

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

[ RTECS号 ]:
SF7790000

盐酸卤泛群文献

Effect of serum lipoproteins on stereoselective halofantrine metabolism by rat hepatocytes.

Chirality 24(7) , 558-65, (2012)

Experimental hyperlipidemia has shown to decrease cytochrome P450 3A4 and 2C11 expression and to increase liver concentrations and the plasma protein binding of halofantrine (HF) enantiomers. The pres...

Discordant temporal evolution of Pfcrt and Pfmdr1 genotypes and Plasmodium falciparum in vitro drug susceptibility to 4-aminoquinolines after drug policy change in French Guiana.

Antimicrob. Agents Chemother. 56(3) , 1382-9, (2012)

Analysis of the evolution of drug target genes under changing drug policy is needed to assist monitoring of Plasmodium falciparum drug resistance in the field. Here we genotype Pfcrt and Pfdmr1 of 700...

Using resin to generate a non-invasive intestinal bile-depleted rat model was unsuccessful.

Eur. J. Pharm. Sci. 47(2) , 347-51, (2012)

The purpose of this study was to evaluate if a rat model, based upon co-administration of the anion-exchanging resin, cholestyramine, could replace surgery when evaluating the importance of bile on dr...

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