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EFFECTIVENES OF PYRIDINIUM CHLORIDE DERIVATIVES ON ACETYLCHOLINESTERASE ACTIVITY INHIBITED BY SOMAN IN VITRO AND IN VIVO (CROSBI ID 506016)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa

Lucić Vrdoljak, Ana ; Velikić, Gorana ; Radić, Božica ; Peraica, Maja ; Fuchs, Radovan ; Lovrić, Jasna EFFECTIVENES OF PYRIDINIUM CHLORIDE DERIVATIVES ON ACETYLCHOLINESTERASE ACTIVITY INHIBITED BY SOMAN IN VITRO AND IN VIVO // Programme and presentation abstracts of the 4th SISPAT international symposium on protection against toxic substances. Singapur: Applied science and analysis, 2004. str. 112-112-x

Podaci o odgovornosti

Lucić Vrdoljak, Ana ; Velikić, Gorana ; Radić, Božica ; Peraica, Maja ; Fuchs, Radovan ; Lovrić, Jasna

engleski

EFFECTIVENES OF PYRIDINIUM CHLORIDE DERIVATIVES ON ACETYLCHOLINESTERASE ACTIVITY INHIBITED BY SOMAN IN VITRO AND IN VIVO

In this paper three new pyridinium compounds: 1-phenacyl-2-methylpiridinium chloride, 1-benzoylethylpyridinium chloride, and 1-benzoylethylpyridinium-4-aldoxime chloride have been synthesized, and tested in vitro using human erythrocyte acetylcholinesterase (AChE) inhibited by soman and in vivo in soman poisoned mice. The inhibitory power (IC50), as well as reactivating (% R) and protective capacity (P50) of each compound was tested on soman-inhibited human erythrocyte AChE. Their acute toxicity (LD50) was tested in mice and observed in 24-hour period. All tested compounds were found to be reversible inhibitors of AChE. Their AChE binding affinity was compared with their protective effect (PI) on soman phosphonylated enzyme. These compounds have shown weak protective effectiveness without reactivating potency either in vitro or in vivo. Our results show that tested compounds are relatively toxic (their LD50 was from 80.0 to 105.0 mg/kg body weight) and inadequate antidotes in soman poisoning. Their protective effect is more likely to be related to other mechanisms of the cholinergic system.

oximes; AChE; soman

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Podaci o prilogu

112-112-x.

2004.

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objavljeno

Podaci o matičnoj publikaciji

Programme and presentation abstracts of the 4th SISPAT international symposium on protection against toxic substances

Singapur: Applied science and analysis

Podaci o skupu

The 4th SISPAT international symposium on protection against toxic substances

poster

06.12.2004-10.12.2004

Singapur

Povezanost rada

Temeljne medicinske znanosti