Pentamidine isethionate salt

Химические свойства

White or almost white powder or colourless crystals, hygroscopic.

Использование

Pentamidine isethionate salt has been used:

• as a positive control for anti-leishmanial, anti-plasmodial and cytotoxic assays
• as a prototypical compound to analyse the inhibitor effect on human ether-a-go-go-related gene (HERG) K⁺ channel trafficking
• as an anti-leishmanial agent in promastigotes

Определение

ChEBI: An organosulfonate salt obtained by reaction of pentamidine with two equivalents of 2-hydroxyethylsulfonic acid.

Общее описание

Odorless white or almost white crystals or powder. Odor also reported as a slight butyric odor. Very bitter taste. pH (5% aqueous solution) 4.5-6.5.

Реакции воздуха и воды

Hygroscopic. May be sensitive to prolonged exposure to air. Aqueous solutions deteriorate on storage. Water soluble.

Профиль реактивности

Can decompose on prolonged exposure to light.

Пожароопасность

Flash point data for Pentamidine isethionate are not available; however, Pentamidine isethionate is probably combustible.

Биологическая активность

Antimicrobial. Neuroprotective; inhibits constitutive nitric oxide synthase in the brain and acts as a NMDA glutamate receptor antagonist.

Клиническое использование

4,4’-(Pentamethylenedioxy)dibenzamidine diisethionate(NebuPent, Pentam 300) is a water-soluble crystalline saltthat is stable to light and air. The principal use of pentamidineis for the treatment of pneumonia caused by the opportunisticpathogenic protozoan P. carinii, a frequent secondaryinvader associated with AIDS. The drug may beadministered by slow intravenous infusion or by deep intramuscularinjection for PCP. An aerosol form of pentamidineis used by inhalation for the prevention of PCP inhigh-risk patients infected with HIV who have a previoushistory of PCP infection or a low peripheral CD4+ lymphocytecount.
Pentamidine has been used for the prophylaxis and treatmentof African trypanosomiasis. It also has some value fortreating visceral leishmaniasis. Pentamidine rapidly disappearsfrom the plasma after intravenous injection and is distributedto the tissues, where it is stored for a long period.This property probably contributes to the usefulness of thedrug as a prophylactic agent.