A. Lucic, B. Radić, I. Primožič
1996
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Quality indicators
Journal
Toxicology Letters
Abstract
New synthesized oximes derivatives of imidazole and quinuclidines were tested in vitro using human erythrocyte acetylcholinesterase (AChE) inhibited by soman and in vivo using soman poisoned mice. The inhibitory power of oximes (IC 50), acute toxicity (LD 50) as well as reactivating and protecitve capacities with respect to soman-inhibted AChE were tested for each of the synthesized oximes. Derivatives of imidazoles demonstrated mostly weak reactivating and protective characteristics, both in vitro and in vivo. Only BMR-3 oxime was powerful reactivator of soman inhibte human AChe (55 %). BMR-4 oxime given together with atropine sulfate, provided a good in vivo protection against 1.8 and 2.2 x LD 50 of soman. On the contrary, all tested quinuclidne compounds are protective agents against soman in vivo (PP-1, PP-2, PP-3, PP-4 protect against 2-2.5 x LD 50 of soman). Bm-1 oxime has the best protection against soman inhibition of the AChE of all tested compounds (protect against 4 LD 50 of soman). Quinuclidines in vitro activity as reactivators of soman inhibited AChE, and their protective power against soman inhibition of AChE in vitro are negligible. The results indicate that in vivo effectiveness of quinuclidine oximes against soman poisoning is not related to their reactivatin or protective potentials for AChE; their good protective effect is more likely to be related to other mechanisms of the cholinergic system.