A comparison of the decarbamoylation rates of physostigmine-inhibited plasma and red cell cholinesterases of man with other species
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Cited by (19)
Human plasma-derived butyrylcholinesterase is behaviorally safe and effective in cynomolgus macaques (Macaca fascicularis)challenged with soman
2019, Chemico-Biological InteractionsCitation Excerpt :In mice, the behavioral safety of a large dose of HuBChE alone, physostigmine alone, and HuBChE pretreatment followed by physostigmine challenge was evaluated by Clark et al. [11]. Physostigmine (also known as eserine) is often used as a surrogate challenge agent for OP nerve agents or insecticides because it is a reversible carbamate cholinesterase inhibitor with high potency and a well-described pharmacokinetic and toxicity profile [5,20,46,47,50]. Clark et al. exposed mice to 2000 U of HuBChE by intraperitoneal injection followed by an assessment of acoustic startle reflex (ASR) and prepulse inhibition (PPI) and demonstrated that a 600-fold increase in circulating blood BChE activity did not alter ASR or PPI behavior.
Efficacy of antidotes and their combinations in the treatment of acute carbamate poisoning in rats
2018, ToxicologyCitation Excerpt :Although the mechanisms of antidotal action of HI-6 and d-tubocurarine differ, the fact that both the antidotes lack significant penetration into brain gives the plausible explanation why they are more effective against peripherally active carbamate pyridostigmine and suggests that the neuromuscular transmission is the function that they protect in case of AChE inhibition. In vitro studies have shown that physostigmine and pyridostigmine have high carbamylation and decarbamylation constants in various types of cholinesterases – AChE and butyrylcholinesterase from various animal species, including humans (Wetherell and French, 1991; Stojan and Zorko, 1997). Novel carbamates aimed at treatment of Alzheimer’s disease, including the already approved rivastigmine, have higher constants of carbamylation and lower decarbamylation constants than the older carbamates physostigmine and pyridostigmine (Stojan and Zorko, 1997; Groner et al., 2007).
Reversal of cardiac vagal effects of physostigmine by adjunctive muscarinic blockade
2016, NeuroToxicologyCitation Excerpt :Therefore, at least with higher concentrations of physostigmine, near maximal inhibition is likely to be achieved within 10-min of drug perfusion – as used in the present study. In previous work, the rate of reactivation of acetylcholinesterase (i.e. decarbomoylation) was substantially slower than the rate of inactivation, with a time course of several hours (Wetherell and French, 1991). A such, a non-cumulative concentration-response, starting at the highest concentration of physostigmine, would not be possible within a suitable timeframe for experiments in isolated hearts.
Characterization of human serum butyrylcholinesterase in rhesus monkeys: Behavioral and physiological effects
2012, Neurotoxicology and TeratologyCitation Excerpt :Further, a significant increase in choice reaction time was observed following exposure to physostigmine. Physostigmine in rhesus monkeys is fairly well characterized and the decarbamylation rates of physostigmine-inhibited ChEs are believed to be similar to that observed in humans, with a peak physiological effect obtained within 30 min and a typical half-life of ChE inhibition approximating 60 min (Asthana et al., 1995; Wetherell and French, 1991). With respect to behavioral evaluation in particular, the performance-impairing effects of physostigmine in rhesus monkeys have been shown using a variety of cognitive–behavioral tasks, including attention and short-term memory tasks analogous to the present task (Frederick et al., 1995; Penetar and McDonough, 1983) and behavioral performance generally (Frederick et al., 1995) at doses comparable to the one used here.
In vitro kinetic interactions of pyridostigmine, physostigmine and soman with erythrocyte and muscle acetylcholinesterase from different species
2011, Toxicology LettersCitation Excerpt :Although significant differences between species were calculated (Table 2), the maximum difference of the decarbamylation half-time was only 20% with pyridostigmine. Physostigmine-inhibited guinea pig AChE decarbamylated substantially slower compared to the other species, a fact which was observed already by Wetherell and French (1991) using a different methodology. The dynamic model for the real-time determination of membrane-bound AChE activity was originally developed for use with human erythrocytes (Eckert et al., 2006a).
Effects of oximes on rate of decarbamylation of human red blood cell AChE measured with two different methods
2008, Biochemical PharmacologyCitation Excerpt :A prerequisite of our approach to determine the decarbamylation kinetics of AChE is the strict obedience of a first-order reaction. Although such a behavior may be anticipated on theoretical grounds, it has been repeatedly confirmed experimentally [9,14–16]. This behavior enables the kinetic analysis of the more advanced part of the reaction curve when excess carbamate was already effectively removed both in the dynamic and the static system; in fact, fitting procedures to the data points showed clear first-order reactions with goodness of fit, R2 > 0.999 and 0.980, respectively.