Reactivation potency of new group of acetylcholinesterase reactivators and their comparison with currently available oximes.
In this work, in vitro potency of novel serie of monoquaternary pyridinium oximes to reactivate cyclosarin-inhibited acetylcholinesterase (AChE) was tested. Currently available oximes (pralidoxime, obidoxime, trimedoxime, HI-6 and BI-6) were used as oximes for comparison. As resulted, none of tested new reactivators was able to reactivate AChE inhibited by cyclosarin. Also pralidoxime, obidoxime and trimedoxime did not reach good reactivation results. Only oximes HI-6 and BI-6 achieved sufficient reactivation potency. From obtained results, it can be deduced, that only reactivators with oxime group in position two are able to reactivate cyclosarin-inhibited AChE.
Kuca
Kamil
K
University of Defence in Brno, Faculty of Military Health Sciences in Hradec Králové, Czech Republic. kucakam@pmfhk.cz
Pícha
Jan
J
Jun
Daniel
D
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D002801:Cholinesterase Reactivators / Q000737:chemistry / Q000494:pharmacology*; D066298:In Vitro Techniques; D009943:Organophosphorus Compounds / Q000494:pharmacology; D010091:Oximes / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats
D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D009943:Organophosphorus Compounds; D010091:Oximes; D000110:Acetylcholinesterase; C053914:cyclohexyl methylphosphonofluoridate