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
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