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 oxime K027 achieved the highest reactivation potency (100%; concentration of the oxime -10(-2) M). However, oxime HI-6 (33%) and obidoxime (23%) seem to be the best AChE reactivators for human relevant doses (10(-4) M and lower). CONCLUSION: For human relevant doses, newly developed oximes (K027 and K033) do not surpass the reactivation potency of the most promising oxime, HI-6.

• MeSH
• Acetylcholinesterase metabolism   MeSH
• Antidotes pharmacology   MeSH
• Cholinesterase Inhibitors toxicity   MeSH
• Brain drug effects   enzymology   MeSH
• Obidoxime Chloride pharmacology   MeSH
• Oximes pharmacology   MeSH
• Pralidoxime Compounds pharmacology   MeSH
• Swine MeSH
• Pyridinium Compounds pharmacology   MeSH
• Cholinesterase Reactivators pharmacology   MeSH
• Sarin toxicity   MeSH
• In Vitro Techniques MeSH
• Research Design MeSH
• Dose-Response Relationship, Drug MeSH
• Animals MeSH
• Check Tag
• Animals MeSH
• Publication type
• Journal Article MeSH
• Research Support, Non-U.S. Gov't MeSH
• Comparative Study MeSH
• Names of Substances
• 1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide MeSH Browser
• 1,4-bis(2-hydroxyiminomethylpyridinium)butane MeSH Browser
• Acetylcholinesterase MeSH
• Antidotes MeSH
• asoxime chloride MeSH Browser
• Cholinesterase Inhibitors MeSH
• Obidoxime Chloride MeSH
• Oximes MeSH
• pralidoxime MeSH Browser
• Pralidoxime Compounds MeSH
• Pyridinium Compounds MeSH
• Cholinesterase Reactivators MeSH
• Sarin MeSH