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

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

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Programme and presentation abstracts of the 4th SISPAT international symposium on protection against toxic substances / - Singapur : Applied science and analysis, 2004, 112-112

Skup
The 4th SISPAT international symposium on protection against toxic substances

Mjesto i datum
Singapur, 06.12.2004. - 10.12.2004

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
oximes; AChE; soman

Sažetak
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.

Izvorni jezik
Engleski

Znanstvena područja
Temeljne medicinske znanosti

POVEZANOST RADA