A conjugate of pyridine-4-aldoxime and atropine as a potential antidote against organophosphorus compounds poisoning. | Zendy

Jasna Lovrić | Zendy; Suzana Berend | Zendy; Ana Lucić Vrdoljak | Zendy; Božica Radić | Zendy; Maja Katalinić | Zendy; Zrinka Kovarik | Zendy; Davor Želježić | Zendy; Nevenka Kopjar | Zendy; Slavko Rast | Zendy; Milan Mesić | Zendy

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A conjugate of pyridine-4-aldoxime and atropine as a potential antidote against organophosphorus compounds poisoning.

Author(s) -

Jasna Lovrić,

Suzana Berend,

Ana Lucić Vrdoljak,

Božica Radić,

Maja Katalinić,

Zrinka Kovarik,

Davor Želježić,

Nevenka Kopjar,

Slavko Rast,

Milan Mesić

Publication year - 2011

Publication title -

acta biochimica polonica

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.452

H-Index - 78

eISSN - 1734-154X

pISSN - 0001-527X

DOI - 10.18388/abp.2011_2264

Subject(s) - tabun , soman , antidote , paraoxon , atropine , pralidoxime , nerve agent , acetylcholinesterase , pharmacology , chemistry , in vivo , in vitro , oxime , sarin , toxicity , cholinesterase , toxicology , biochemistry , anesthesia , medicine , enzyme , biology , organic chemistry , microbiology and biotechnology

A conjugate of pyridine-4-aldoxime and atropine (ATR-4-OX) was synthesized and its antidotal efficiency was tested in vitro on tabun- or paraoxon-inhibited acetylcholinesterase (AChE) of human erythrocytes as well as in vivo using soman-, tabun- or paraoxon-poisoned mice. Its genotoxic profile was assessed on human lymphocytes in vitro and was found acceptable for further research. ATR-4-OX showed very weak antidotal activity, inadequate for soman or tabun poisoning. Conversely, it was effective against paraoxon poisoning both in vitro and in vivo. All animals treated with 5 % or 25 % LD(50) doses of the new oxime survived after administration of 10.0 or 16.0 LD(50) doses of paraoxon, respectively. Based on the persistence of toxicity symptoms in mice, the atropine moiety had questionable effects in attenuating such symptoms. It appears that ATR-4-OX has a therapeutic effect related to the reactivation of phosphylated AChE, but not to receptor antagonization.

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