Literature DB >> 6547103

Effect of PAM-2 Cl, HI-6, and HGG-12 in poisoning by tabun and its thiocholine-like analog in the rat.

S Cetković, M Cvetković, D Jandrić, M Cosić, B Bosković.   

Abstract

It has been shown that HI-6 was the most potent oxime so far known in poisoning by sarin, VX , and soman, but its protective effect in tabun poisoning, allegedly due to poor reactivation of inhibited ChE, was much less pronounced. We have found that the thiocholine-like analog of tabun , O-ethyl, N-N- dimethyamino -S-(2-diethylaminoethyl)- thiophosphatemethylsul fomethylate (Ta-S-N+), was very useful in resolving this problem and established the relationship between reactivating and protective effects of PAM-2 Cl, HI-6, and HGG-12 in rats. PAM-2 Cl (protective ratio (PR) = 22.1) and HI-6 (PR = 24.8), combined with atropine, were very effective against Ta-S-N+ poisoning and reactivating inhibited RBC AChE in vitro and rat blood ChE in vivo. The inefficiency of PAM-2 Cl (PR = 1.6) and HI-6 (PR = 2) in tabun poisoning was due to their inadequacy to reactive tabun -inhibited ChEs . The protective effects of HGG-12 in tabun (PR = 2.8) and Ta-S-N+ poisoning (PR = 2.6) were low, and in the absence of any reactivation of inhibited ChEs , have been attributed to its direct pharmacological effects, which were much more potent in the comparison with PAM-2 Cl or HI-6. It is concluded that the reactivation of inhibited ChE is of decisive importance in the efficient protection in poisoning by tabun and other known chemical warfare nerve agents, whereas their direct pharmacological effects are of limited value, allowing survival of animals only against a few LD50s .

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Year:  1984        PMID: 6547103     DOI: 10.1093/toxsci/4.2part2.116

Source DB:  PubMed          Journal:  Fundam Appl Toxicol        ISSN: 0272-0590


  8 in total

1.  HI-6 therapy of soman and tabun poisoning in primates and rodents.

Authors:  M G Hamilton; P M Lundy
Journal:  Arch Toxicol       Date:  1989       Impact factor: 5.153

2.  Efficacy of a combination of acetylcholinesterase reactivators, HI-6 and obidoxime, against tabun and soman poisoning of mice.

Authors:  J G Clement; J D Shiloff; C Gennings
Journal:  Arch Toxicol       Date:  1987       Impact factor: 5.153

3.  Pharmacokinetics of the oximes HI 6 and HLö 7 in dogs after i.m. injection with newly developed dry/wet autoinjectors.

Authors:  U Spöhrer; H Thiermann; R Klimmek; P Eyer
Journal:  Arch Toxicol       Date:  1994       Impact factor: 5.153

Review 4.  Unequal efficacy of pyridinium oximes in acute organophosphate poisoning.

Authors:  Biljana Antonijevic; Milos P Stojiljkovic
Journal:  Clin Med Res       Date:  2007-03

5.  HLö 7 dimethanesulfonate, a potent bispyridinium-dioxime against anticholinesterases.

Authors:  P Eyer; I Hagedorn; R Klimmek; P Lippstreu; M Löffler; H Oldiges; U Spöhrer; I Steidl; L Szinicz; F Worek
Journal:  Arch Toxicol       Date:  1992       Impact factor: 5.153

6.  Efficacy of HLö-7 and pyrimidoxime as antidotes of nerve agent poisoning in mice.

Authors:  J G Clement; A S Hansen; C A Boulet
Journal:  Arch Toxicol       Date:  1992       Impact factor: 5.153

7.  Treatment of tabun poisoned guinea-pigs with atropine, HLö 7 or HI 6: effect on respiratory and circulatory function.

Authors:  F Worek; T Kirchner; L Szinicz
Journal:  Arch Toxicol       Date:  1994       Impact factor: 5.153

Review 8.  Oxime-mediated reactivation of organophosphate-inhibited acetylcholinesterase with emphasis on centrally-active oximes.

Authors:  Janice E Chambers; Mary B Dail; Edward C Meek
Journal:  Neuropharmacology       Date:  2020-06-13       Impact factor: 5.250

  8 in total

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