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A comparison of the efficacy of a new asymmetric bispyridinium oxime BI-6 with presently used oximes and H oximes against sarin by in vitro and in vivo methods

P.O. Box 35/T, Purkyné Military Medical Academy, 500 01 Hradec Králové, Czech Republic

J Cabal

Purkyné Military Medical Academy, Hradec Králové, Czech Republic

1. 1 The reactivating and therapeutic efficacy of a new acetylcholinesterase reactivator, designated BI-6 (1-/2-hydroxyiminomethylpyridinium/-4-/carbamoylpyridinium/-2-butene dibromide), against organophosphate sarin was compared with presently used oximes (pralidoxime, obidoxime, methoxime) and H oximes (HI-6, HLö-7) by in vitro and in vivo methods.
   
2. 2 Our results confirm that the new oxime BI-6 is a significantly more efficacious acetylcholinesterase reactivator than currently available pralidoxime and obidoxime but not as effective as H oximes (HI-6, HLö-7) in vitro as well as in vivo. In addition, the oxime BI-6 is able to protect supralethal sarin poisoned rats at human-relevant doses.
   
3. 3 Our data also suggest that the potency of oximes tested to reactivate sarin-inhibited acetylcholinesterase in vitro closely corresponds to their reactivating efficacy in vivo and their ability to protect rats poisoned with supralethal doses of sarin.
   

Key Words: sarin • pralidoxime • obidoxime • methoxime • HI-6 • HLö-7

Human & Experimental Toxicology, Vol. 18, No. 9, 560-565 (1999)
DOI: 10.1191/096032799678845106


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