泛托法隆

中文名称:

泛托法隆

中文同义词:

泛托法隆;3,4-二甲氧基-N-甲基-N- [3-[4-[[2-(1-甲基乙基)-1-氮茚基]磺酰基]苯氧基]丙基]苯乙胺

英文名称:

Fantofarone

英文同义词:

Fantofarone;2-Isopropyl-1-[[4-[3-[[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino]propoxy]phenyl]sulfonyl]indolizine;SR-33557;3,4-Dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]benzeneethanamine;FANTOFARONE;SR-33557;SR33557; 114432-13-2;CS-2766;Benzeneethanamine, 3,4-dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]-

CAS号:

114432-13-2

分子式:

C31H38N2O5S

分子量:

550.71

EINECS号:

相关类别:

API

Mol文件:

114432-13-2.mol

熔点 

82-83°

密度 

dz 1.21 g/cm3

酸度系数(pKa)

8.34 ± 0.05(at 25℃)

CAS 数据库

114432-13-2

生物活性

Fantofarone 是钙离子通道 (Calcium Channel) 的强效拮抗剂。

靶点

Calcium Channel.

体外研究

It can be seen that the calcium channel blockers VIZ and Fantofarone (SR) possess a weak intrinsic antimalarial property compared to CQ, and both appear slightly more potent on the CQ-resistant than on the CQ-sensitive parasites. Interestingly, Fantofarone is ca . 10 times more potent than verapamil. Fantofarone (SR) is 10 times more potent than the phenylalkylamine verapamil (VR) on the two P. fdciparum strains. As revealed by the isobolograms, the two calcium channel blockers potentiate the CQ sensitivity activity on the CQ-resistant P. fufcipurum strain, verapamil appearing 2 to 3 times more potent than Fantofarone. Furthermore, when used at similar subinhibitory fractions of their IC 50 , VR is 2 to 3 times more potent than Fantofarone in decreasing CQ resistance.

体内研究

Treatment with isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.), a reduction is observed in the occurrence and severity of vasospasm, whereas verapamil (0.2 mg/kg, i.v.) is much less effective. Although it totally inhibits distal AIV, isosorbide dinitrate does not significantly affect proximal diameter decrease. The most potent compound with regard to both the distal and proximal vasospasms is Fantofarone, which significantly reduces AIV throughout the experiment. Verapamil does not reduce AIV significantly.