Protection of cholinesterase against

Koelle, G.B. (1946). Protection of cholinesterase against irreversible inactivation by DFP in vitro. J. Pharmacol. Exp. Ther. 88 323-7. 

Protection in vitro of cholinesterases against organo-phosphorus compounds... 

Scalfe, J.F. Protection of human red cell cholinesterase against inhibition by tabun and 0,O-diethyl-S-2-diethyl-aminoethyl phosphorothiolate. Can. J. Biochem. Physiol. 38 301-303, 1960. 

The protective activity of IV against lethal Intoxication by OF compounds has been thought to be exerted principally by promoting reactivation of Inhibited cholinesterase. IV has been found to... 

Schaumann OO found that pretreatment of mice with 2-PAM 1 reduced inhibition of acetylcholinesterase in brain by paraoxon much more effectively than those by DFP and 217-A0. The finding of some protection against all three OP compounds could depend on direct reaction between the last two inhibitors and the oxime, with a reduction in inhibition of the enzyme. A similar consideration applies to the report by Bisa et al. that IV protected serum and brain cholinesterase from inhibition by paraoxon administered later at twice the LD5O. Although the same intraperitoneal dose of IV (7 mg) was found to protect the cholinesterase of rat serum and brain only incompletely from inhibition by DFP at 5 times the LD50, that of serum recovered its normal activity by 20 h after the dose of DFP, whereas that of brain required 26 h for recovery. 

In vitro, addition of IV and DFP simultaneously to red-cell cholinesterase protected the enzyme against Inhibition by DFP to a greater extent than the reactivation that the same concentration of the oxime (10 3 m) was capable of effecting after exposure of the enzyme to the same concentrations of DFP (1-3 x 10 g/ml). 

Maxwell, D.M., Saxena, A., Gordon, R.K., Doctor, B.P. (1999). Improvements in scavenger protection against organophos-phorus agents by modification of cholinesterases. Chem. Biol. Interact. 119-20 419-28. 

Wolfe, A.D., Blick, D.W., Murphy, M.R., Miller, S.A., Gentry, M.K., Hartgraves, S.L., Doctor, B.P. (1992). Use of cholinesterases as pretreatment drugs for the protection of rhesus monkeys against soman toxicity. Toxicol. Appl. Pharmacol. 117 189-93. 

Doctor, B. P., Blick, D. W., Caranto, G., Castro, C. A., Gentry, M. K., Larison, R., et al. (1993). Cholinesterases as scavengers for organophosphorus compounds Protection of primate performance against soman toxicity. Chemico-Biological Interactions, 87, 285-293. 

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