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Issue 4, 2014
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New arginine substituted derivative of poly(allylamine hydrochloride) for heparin reversal

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Abstract

New derivatives of polyallylamine containing arginine moieties (PAH-ARG) were synthesized. The in vitro tests performed in heparinized blood plasma showed that the complexation of heparin by PAH-ARG polymers allowed the reduction of the activated partial thromboplastin time (aPTT) values to the normal level. The dose of PAH-ARG required for complete reversal of aPTT (prolonged by 1 U of heparin) was half of that required for protamine sulfate, the currently used heparin antagonist. The efficacy of these polymers in the neutralization of heparin was confirmed by in vivo tests using a rat model. PAH-ARG polymers were nontoxic to the fibroblast cells.

Graphical abstract: New arginine substituted derivative of poly(allylamine hydrochloride) for heparin reversal

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Supplementary files

Article information


Submitted
06 Dec 2013
Accepted
28 Dec 2013
First published
09 Jan 2014

Med. Chem. Commun., 2014,5, 489-495
Article type
Concise Article

New arginine substituted derivative of poly(allylamine hydrochloride) for heparin reversal

K. Kamiński, B. Kałaska, P. Koczurkiewicz, M. Michalik, K. Szczubiałka, A. Mogielnicki, W. Buczko and M. Nowakowska, Med. Chem. Commun., 2014, 5, 489
DOI: 10.1039/C3MD00374D

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