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METHOD OPTIMIZATION FOR ACETYLCHOLINESTERASE MODULATORS-ALBUMIN INTERACTIONS

Authors :
Kamil Musilek
Jana Zdarova Karasova
Filip Zemek
Kamil Kuca
Source :
Military Medical Science Letters. 80:58-64
Publication Year :
2011
Publisher :
Faculty of Military Health Sciences, University of Defence, 2011.

Abstract

Summary Plasma proteins such as human serum albumin (HSA) and alpha 1-acid glycoprotein (AGP) play an important role in the pharmacokinetic and pharmacodynamic properties of all endogenous or exogenous substances presented in the blood vessels. Their abundance in human blood not only helps to maintain hemostasis, but also makes them ideal candidates as transporters or possible depot reservoirs. Numerous methods e.g. equilibrium dialysis, ultrafiltration. ultracentrifugation, high-performance affinity chromatography were introduced to determine potential interactions with plasma proteins and possible quantification. In this work method was developed for the determination of drug-human serum albumin interactions and applied to obtain pharmacokinetic profile of AChE modulators prepared at the Faculty of Military Health Sciences. For method validation commercially used compounds HI-6 and obidoxime were chosen. HI-6 did not bind at all while obidoxime showed 7 % binding potency.

Details

ISSN :
03727025
Volume :
80
Database :
OpenAIRE
Journal :
Military Medical Science Letters
Accession number :
edsair.doi...........1bda55e3d898b2bf05567b282c71e9ae