Title : Reactivation kinetics of a series of related bispyridinium oximes with organophosphate-inhibited human acetylcholinesterase--Structure-activity relationships.

Pub. Date : 2012 Jun 15

PMID : 22649796






5 Functional Relationships(s)
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1 However, numerous in vitro and in vivo studies demonstrated a limited ability of these oximes to reactivate acetylcholinesterase (AChE) inhibited by different OP pesticides and nerve agents. Oximes acetylcholinesterase (Cartwright blood group) Homo sapiens
2 However, numerous in vitro and in vivo studies demonstrated a limited ability of these oximes to reactivate acetylcholinesterase (AChE) inhibited by different OP pesticides and nerve agents. Oximes acetylcholinesterase (Cartwright blood group) Homo sapiens
3 New oximes were mostly tested for their therapeutic efficacy by using different animal models and for their reactivating potency with AChE from different species. Oximes acetylcholinesterase (Cartwright blood group) Homo sapiens
4 Now, we found it tempting to determine the reactivation kinetics of a series of bispyridinium oximes bearing one or two oxime groups at different positions and having an oxybismethylene or a trimethylene linker under identical conditions with human AChE inhibited by structurally different OP. Oximes acetylcholinesterase (Cartwright blood group) Homo sapiens
5 Hence, these and previous data emphasize the necessity for thorough kinetic investigations of OP-oxime-AChE interactions and underline the difficulty to develop a broad spectrum oxime reactivator which is efficient against structurally different OP inhibitors. Oximes acetylcholinesterase (Cartwright blood group) Homo sapiens