2006
DOI: 10.1007/bf03161181
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Reactivation of sarin-inhibited pig brain acetylcholinesterase using oxime antidotes

Abstract: Introduction: Organophosphorus nerve agents inhibit the enzyme, acetylcholinesterase (AChE; EC 3.1.1.7). AChE reactivators (also known as oximes) are generally used for the reactivation of an inhibited enzyme.Methods: Two new AChE reactivators-K033 and K027-were tested for their in vitro reactivation of sarin-inhibited pig-brain AChE. Their reactivation potencies were compared with the commercially available AChE reactivators, pralidoxime, obidoxime, and HI-6.Results: Of the oximes tested, the newly developed … Show more

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Cited by 6 publications
(5 citation statements)
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“…Tables –). Although reactivation constants from previous studies differ depending on the AChE source and species, it became apparent that K027 is an effective reactivator of AChE inhibited by various OPs. Indeed, herein K027 showed the fastest nucleophilic displacement rates k +2 , higher than 1 min –1 in the cases of sarin-, cyclosarin-, and VX-inhibited AChE, which resulted in a high degree of enzymatic activity shortly upon the start of reactivation. Its overall reactivation rates ( k r ) would be even more efficient if the affinities of phosphylated AChE (1/ K OX ) for K027 were not as low (cf.…”
Section: Results and Discussionmentioning
confidence: 99%
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“…Tables –). Although reactivation constants from previous studies differ depending on the AChE source and species, it became apparent that K027 is an effective reactivator of AChE inhibited by various OPs. Indeed, herein K027 showed the fastest nucleophilic displacement rates k +2 , higher than 1 min –1 in the cases of sarin-, cyclosarin-, and VX-inhibited AChE, which resulted in a high degree of enzymatic activity shortly upon the start of reactivation. Its overall reactivation rates ( k r ) would be even more efficient if the affinities of phosphylated AChE (1/ K OX ) for K027 were not as low (cf.…”
Section: Results and Discussionmentioning
confidence: 99%
“…38 The halogenated aldoximes were then treated with monoquaternary pyridinium amides (15−17), which were prepared as previously described, 39 resulting in the final mono-or dichlorinated pyridinium oximes (7−12). The final step took at least 12 h for compounds with a double bond in the linker (9,12) and several days for compounds with a fully saturated linker (7,8,10,11). The yields were found to be better for compounds with an unsaturated linker (9,12), whereas compounds with a saturated linkage (7,8,10,11) were obtained in generally lower yields, especially when two chlorine moieties were present.…”
Section: ■ Results and Discussionmentioning
confidence: 99%
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“…The use of an animal model, such as swine, that adequately simulates the structure and physiology of humans, provides a readily available source of mesenchymal stem cells for research, and allows for improvements in therapeutic protocols [18][19][20]. Pigs have been used as a large animal model for studying human clinical therapies as diverse as heart surgery [18], genetic disorders [21], and drug testing [22]. In addition, pigs have ample subcutaneous fat which is similar to that in humans.…”
Section: Introductionmentioning
confidence: 99%