中文名称:

磷酸哌喹

中文同义词:

磷酸哌喹;1,3-双[4-(7-氯-喹啉-4-基)哌嗪-1-基]丙烷磷酸盐;磷酸喹哌;哌喹磷酸盐

英文名称:

4,4-(1,3-Propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline) phosphate

英文同义词:

4,4-(1,3-propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline) phosphate;PIPERAQUINE PHOSPHATE;Quinoline, 4,4-(1,3-propanediyldi-4,1-piperazinediyl)bis(7-chloro-, phosphate;antimalarial drugs PIPERAQUINE PHOSPHATE;2-(9-methyldecyl)-5-(4-methylpentyl)benzene-1,3-diol;4,4-(1,3-Propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline);4,4-(1,3-Propanediyldi-4,1-piperazinediyl)bis(7-chloroquinoline) phosphate USP/EP/BP;85547-56-4

CAS号:

85547-56-4

分子式:

C29H32Cl2N6.H3PO4

分子量:

633.51

EINECS号:

1312995-182-4

相关类别:

原料药;医药中间体;原料;医药原料;科研试剂

Mol文件:

85547-56-4.mol

生物活性

Piperaquine phosphate 是一种双喹啉抗疟药，可以与青蒿素联用于抗疟研究。

体内研究

Piperaquine (10-90 mg/kg; a single i.p.) decreases parasitemia at all of the doses tested in mice. Piperaquine (90 mg/kg; a single i.p.) exhibits the t 1/2 , apparent clearance, and apparent volume of distribution 17.8 days, 33.5 mg•h/L, 1.55 L/h/kg, and 956 L/kg, respectively, in healthy mice and 16.1 days, 27.3 mg•h/L, 1.9 L/h/kg, and 1,059 L/kg in malaria-infected mice. Animal Model: Male BALB/c mice (7 to 8 weeks) are inoculated with Plasmodium berghei parasites Dosage: 0, 10, 30, 90 mg/kg Administration: A single i.p. administration Result: The median survival time was 10 days at dose of 10 mg/kg. The median survival time was 54 days at dose of 30 mg/kg. All mice were active and alert and had stable body weights throughout the course of the study at dose of 90 mg/kg. Animal Model: Male Swiss mice (6 weeks old) Dosage: 90 mg/kg (Pharmacokinetic Analysis) Administration: A single i.p. administration Result: t 1/2 =17.8 d; AUC=33.5 mg•h/L; apparent clearance=1.55 L/h/kg; apparent volume of distribution=956 L/kg.

Animal Model:

Male BALB/c mice (7 to 8 weeks) are inoculated with Plasmodium berghei parasites

Dosage:

0, 10, 30, 90 mg/kg

Administration:

A single i.p. administration

Result:

The median survival time was 10 days at dose of 10 mg/kg. The median survival time was 54 days at dose of 30 mg/kg. All mice were active and alert and had stable body weights throughout the course of the study at dose of 90 mg/kg.

Animal Model:

Male Swiss mice (6 weeks old)

Dosage:

90 mg/kg (Pharmacokinetic Analysis)

Administration:

A single i.p. administration

Result:

t 1/2 =17.8 d; AUC=33.5 mg•h/L; apparent clearance=1.55 L/h/kg; apparent volume of distribution=956 L/kg.