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

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

Pregled bibliografske jedinice broj: 515496

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

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

A conjugate of pyridine-4-aldoxime and atropine as a potential antidote against organophosphorus compounds poisoning // Acta biochimica Polonica, 58 (2011), 2; 193-198 (međunarodna recenzija, članak, znanstveni)

CROSBI ID: 515496 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

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

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

Izvornik
Acta biochimica Polonica (0001-527X) 58 (2011), 2; 193-198

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
antidotal potential; atropine; genotoxicity; pyridine-4-aldoxime; organophosphates

Sažetak
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 % LD50 doses of the new oxime survived after administration of 10.0 or 16.0 LD50 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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija

POVEZANOST RADA

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