140-64-7 Usage
Chemical Properties
White or almost white powder or colourless crystals, hygroscopic.
Uses
Different sources of media describe the Uses of 140-64-7 differently. You can refer to the following data:
1. Pentamidine isethionate salt has been used:as a positive control for anti-leishmanial, anti-plasmodial and cytotoxic assaysas a prototypical compound to analyse the inhibitor effect on human ether-a-go-go-related gene (HERG) K+ channel traffickingas an anti-leishmanial agent in promastigotes
2. Antiparasitic
Definition
ChEBI: An organosulfonate salt obtained by reaction of pentamidine with two equivalents of 2-hydroxyethylsulfonic acid.
Therapeutic Function
Antiprotozoal
General Description
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.
Air & Water Reactions
Hygroscopic. May be sensitive to prolonged exposure to air. Aqueous solutions deteriorate on storage. Water soluble.
Reactivity Profile
Can decompose on prolonged exposure to light.
Fire Hazard
Flash point data for Pentamidine isethionate are not available; however, Pentamidine isethionate is probably combustible.
Biological Activity
Antimicrobial. Neuroprotective; inhibits constitutive nitric oxide synthase in the brain and acts as a NMDA glutamate receptor antagonist.
Biochem/physiol Actions
Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
Clinical Use
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.
Drug interactions
Potentially hazardous interactions with other drugs
Anti-arrhythmics: increased risk of ventricular
arrhythmias with amiodarone - avoid; possible
increased risk of ventricular arrhythmias with
disopyramide.
Antibacterials: increased risk of ventricular
arrhythmias with delamanid, moxifloxacin and
parenteral erythromycin - avoid with moxifloxacin;
increased risk of ventricular arrhythmias with
parenteral pentamidine and telithromycin.
Antidepressants: increased risk of ventricular
arrhythmias with tricyclics; increased risk of
ventricular arrhythmias with citalopram and
escitalopram - avoid.
Antimalarials: increased risk of ventricular
arrhythmias with piperaquine with artenimol -
avoid.
Antipsychotics: increased risk of ventricular
arrhythmias with amisulpride, droperidol and
phenothiazines - avoid with amisulpride and
droperidol.
Antivirals: increased risk of hypocalcaemia with
parenteral pentamidine and foscarnet; increased risk
of ventricular arrhythmias with saquinavir - avoid.
Cytotoxics: increased risk of ventricular arrhythmias
with vandetanib - avoid.
Ivabradine: increased risk of ventricular arrhythmias.
Metabolism
Extensively hepatically metabolised.
Renal clearance accounts for <5% of the plasma clearance
of pentamidine.
Check Digit Verification of cas no
The CAS Registry Mumber 140-64-7 includes 6 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 3 digits, 1,4 and 0 respectively; the second part has 2 digits, 6 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 140-64:
(5*1)+(4*4)+(3*0)+(2*6)+(1*4)=37
37 % 10 = 7
So 140-64-7 is a valid CAS Registry Number.
140-64-7Relevant articles and documents
Synthesis, Spectroscopic Properties and Antileishmanial Screening of some Pentamidine Analogues
Nandi, Gopa,Mukherjee, S.,Basu, M. K.,Mahato, Shashi B.
, p. 527 - 532 (2007/10/02)
Pentamidine, the diamidine drug of choice is used for the treatment of antimony resistant leishmanial infection.A modified method for preparation of the water-soluble isethionate salt of pentamidine has been developed using p-hydroxybenzaldehyde as starting material.Beside the synthesis of the dimethoxy analogues of pentamidine hydrochloride and pentamidine isethionate, two compounds have been prepared by substitution of amidino groups of pentamidine and its dimethoxy analogue by imidazoline moieties.Cmr spectral data of the compounds have been assigned and the in vitro antileishmanial activity of the analogues were compared with pentamidine isethionate using Leishmania donovani UR-6 strain.