CAS 36167-63-2|Halofantrine hydrochloride

Malaria[1].HERG channel[2].

[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.

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

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