Naslov
Effectiveness of imidazole and quinuclidine derivatives on acetylcholinesterase inhibited by soman in vitro and in vivo

Autori
Lucić, Ana ; Radić, Božica ; Primožič, Ines ; Rončević, Renata ; Binenfeld, Zlatko

Vrsta, podvrsta i kategorija rada
Radovi u zbornicima skupova, cjeloviti rad (in extenso), znanstveni

Izvornik
The second Chemical and Biological Medical Treatment Symposium : proceedings / Price, Richard - Spiez : ASA, 1997, 35-38

Skup
Chemical and Biological Medical Treatment Symposium (2 ; 1996)

Mjesto i datum
Spiez, Švicarska, 07.07.1996. - 12.07.1996

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
soman ; quinuclidinium oximes ; AChE

Sažetak
In this paper, new synthesized oxime derivatives of imidazole and quinuclidines were tested in vitro using human erythrocyte AChE inhibited by soman and in vivo using soman poisoned mice. The inhibitory power (IC50, concentration of the test compounds, oximes, that inhibit to 50 % of the AChE activity), acute toxicity (LD 50 ), as well as reactivating and protective capacities, with respect to soman-inhibited AChE were tested for each of the synthesized oximes. Antidotal characteristics of the new syntesized oximes were compared and related to their chemical structures. Derivatives of imidazoles demonstrated mostly weak reactivating and protective characteristics, both for the in vitro and in vivo cases. These characteristics were independent of the substituents on N phenyl imidazolium oximes. Of the imidazoles, only BMR-3 oxime strongly reactivated the soman inhibited AChE (55%), i.e., in vitro, for human erythrocytes. BMR-4 oxime, in combination with atropine sulfate, provided effective protection in vivo (for mice) against 1.8 and 2.2 LD50 of soman. On the contrary, all tested quinuclidine oximes showed very good protection in vivo (for example, BM-1 protects against 4 x LD 50 of soman), but were ineffective in vitro, i.e., against soman-inhibited human erythrocyte AChE. The results indicate that in vivo effectiveness of quinuclidine oximes against soman poisoning is not telated to their reactivating or protective potentials for AChE measured in in vitro experiments ; their good protective effect is more likely to be related to other mechanisms of the cholinergic system.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Kliničke medicinske znanosti

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