Reactivators, acetylcholinesterase

Kuca, K., Cabal, J., Jim, D., Hrahinova, M. (2007). Potency of five structurally different acetylcholinesterase reactivators to reactivate human brain cholinesterases inhibited by cyclosarin. Clin. Toxicol. (Phila.) 45 512-15. 

Alkondon, M., Rao, K.S., Albuquerque, E.X. (1988). Acetylcholinesterase reactivators modify the functional properties of the nicotinic acetylcholine receptor ion channel. J. Pharmacol. Exp. Ther. 245 543-56. 

Hrabinova, M., Musilek, K., Jun, D., Kuca, K. (2006). New group xylene linker containing acetylcholinesterase reactivators as antidotes against nerve agent cyclosarin. J. Enzyme Inhib. Med. Chem. 21 515-19. 

Kuca, K., Cabal, J., Jun, D., Kassa, K., Bartosova, L., Kunesova, G. (2005c). In vitro reactivation potency of some acetylcholinesterase reactivators against sarin and cyclosarin-induced inhibitions. J. Appl. Toxicol. 25 296-300. 

Pang, Y.P., Kollmeyer, T.M., Hong, F., Lee, J.C., Hammond, P.I., Haugabouk, S.P., Brimijoin, S. (2003). Rational design of alkylene-linked bis-pyridiniumaldoximes as improved acetylcholinesterase reactivators. Chem. Biol. 10 491-502. 

Kuca, K. et al. Strategy for the development of new acetylcholinesterase reactivators—antidotes used for treatment of nerve agent poisonings, Biomed. Pap. Med. Fac. Univ. Palacky Olomouc Czech Repub., 149, 429, 2005. 

Kuca, K., Juna, D. and Musilek, K. Structural requirements of acetylcholinesterase reactivators. Mini Rev. Med. Chem., 6, 269, 2006. 

Kassa, J., and Cabal, J., A comparison of the efficacy of acetylcholinesterase reactivators against cyclohexyl methylphosphonofluoridate (GF agent) by in vitro and in vivo methods, Pharmacol. Toxicol., 84, 41-45. 1999. 

Clement, J.G., Shiloff, J.D., and Gennings, C., Efficacy of the combination of acetylcholinesterase reactivators, HI-6 and obidoxime, against tabun and soman poisoning in mice, J. Chromatogr., 389, 87-94, 1987. 

Clement J., Lockwood, P, and Tomson, A. The acetylcholinesterase reactivator HI-6 comparative study of HI-6 samples from various sources. Arch.Toxicology 62,2-3,220-223,1988. 

Busker RW, Zijlstra JJ, van der Wiel HJ et al. (1991). Organophosphate poisoning a method to test therapeutic effects of oximes other than acetylcholinesterase reactivation in the rat. Toxicology, 69, 331-344. 

Garrigue H, Maurizis JC, Nicolas C et al. (1990). Disposition and metabolism of two acetylcholinesterase reactivators, pyrimidoxime and HI6, in rats submitted to organophosphate poisoning. 

Maurizis JC, Olher M, Nicolas C et al. (1992). In vitro binding of oxime acetylcholinesterase reactivators to proteoglycans synthesized by cultured chondrocytes and fibroblasts. Biochem Pharmacol, 44, 1927-1933. 

Dekleva, A., D. Sket, J. Sketelji, and M. Brzin. 1989. Attenuation of soman- induced lesions of skeletal muscle by acetylcholinesterase reactivating and nonreactivating antidotes. Acta Neu-ropathol. 79(2) 183 -89 cited in Chem. Abstr. CA 112(1) 93434p. 

V-Alkylation of p)ridazine is achieved using alkyl bromides the access via iV-alkylation to new mono-oxime bis-quaternary acetylcholinesterase reactivators used in the treatment of organophosphorous poisoning has been reported (eq 4). The alkylation takes place in DMF at 60 °C and provides the bis-quaternary salt in very good yield (92%). 

In 1990, the Iraqi Army invaded neighboring Kuwait. Subsequently, the United States, at the request of Saudi Arabia, led a coalition to send forces to the area (Smart, 1997). These forces were the largest to operate in a potential chemical environment since World War I. They were provided witii atropine autoinjectors, an acetylcholinesterase reactivator, and a nerve agent pretreatment (p5nidostig-mine bromide). Fortunately, chemical weapons apparently were not used in this conflict, although multiple false alarms were reported. The failure of the Iraqi military... 

Karasova, J.Z., Pohanka, M., Musilek, K., et al., 2010. Passive diffusion of acetylcholinesterase reactivators through the bloodM rain barrier influence of molecular structure. Toxicol. In Vitro 24, 1838-1844. 

Bajgar, J., 2010. Optimal choice of acetylcholinesterase reactivators for antidotal treatment of nerve agent intoxication. Acta Medica (Hradec Kr ove) 53,... 

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