In vitro reactivation of acetylcholinesterase using the oxime K027.
The ability of a new bisquaternary oxime, K027 (1-[4-hydroxyiminomethylpyridinium]-3-[carbamoylpyridinium] propane dibromide), to reactivate the enzyme acetylcholinesterase (AChE) inhibited by the nerve agents Tabun, sarin and VX was evaluated. Its reactivation potency was compared to the AChE reactivators pralidoxime (2-PAM), obidoxime and HI-6; K027 seems a good reactivator of organophosphates-inhibited AChE. Its reactivation potency is lower compared to the other oximes for reactivation of sarin-inhibited AChE, but it is sufficient to significantly increase the activity of sarin-inhibited AChE. Its reactivation ability is comparable to obidoxime for reactivation of VX- and tabun-inhibited AChE and is higher than the reactivation potency of HI-6, for tabun-inhibited AChE. HI-6 is currently regarded the most promising reactivator of organophosphates-inhibited AChE.
Kuca
Kamil
K
Purkyne Military Medical Academy, Department of Toxicology, PO Box 35/T, 500 01 Hradec Králové, Czech Republic.
Kassa
Jirí
J
D000110:Acetylcholinesterase / Q000737:chemistry*; D000818:Animals; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators / Q000737:chemistry*; D004305:Dose-Response Relationship, Drug; D009768:Obidoxime Chloride / Q000737:chemistry; D010755:Organophosphates; D009946:Organothiophosphorus Compounds; D010091:Oximes / Q000737:chemistry*; D011220:Pralidoxime Compounds / Q000737:chemistry; D011726:Pyridinium Compounds / Q000737:chemistry; D012524:Sarin; D013329:Structure-Activity Relationship
D000110:Acetylcholinesterase; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D009768:Obidoxime Chloride; D010755:Organophosphates; D009946:Organothiophosphorus Compounds; D010091:Oximes; D011220:Pralidoxime Compounds; D011726:Pyridinium Compounds; D012524:Sarin; C481758:1-(4-hydroxyiminomethylpyridinium)-3-(carbamoylpyridinium) propane dibromide; C009680:VX-agent; C022870:asoxime chloride; C028797:pralidoxime; C009374:tabun