Anticholinesterase agents

Anticholinesterases are drugs that inhibit or inactivate acetylcholinesterase, causing the accumulation of acetylcholine at the cholinergic receptors. 

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Dialkylphosphorochloridates, (R0)2P(=0)C1, react with trialkyl phosphate esters to give organic pyrophosphates. Organopyrophosphates are anticholinesterase agents and should be handled with great caution (16). Atropine sulfate is a specific antidote. 

A. Goodman and H. Martens, Studies on the Use of Ulectric Tel Acetylcholinesterasefor Anticholinesterase Agent Detection, Edgewood Arsenal Report No. 

Taylor P (1990) Anticholinesterase agents. In Gilman AG, Rail TW, Nies AS, Taylor P (eds) The pharmacological basis of therapeutics. Pergamon Press, New York, pp 131-149... 

Individuals with hereditary low plasma cholinesterase levels (Kalow 1956 Lehman and Ryan 1956) and those with paroxysmal nocturnal hemoglobinuria, which is related to abnormally low levels of erythrocyte acetylcholinesterase (Auditore and Hartmann 1959), would have increased susceptibility to the effects of anticholinesterase agents such as methyl parathion. Repeated measurements of plasma cholinesterase activity (in the absence of organophosphate exposure) can be used to identify individuals with genetically determined low plasma cholinesterase. 

Gordon CJ. 1994. Thermoregulation in laboratory mammals and humans exposed to anticholinesterase agents. Neurotoxicol Teratol 16 427-453. 

Murphy SD, DuBois KP. 1958. The influence of various factors on the enzymatic conversion of organic thiophosphates to anticholinesterase agents. J Pharmacol Exp 124 194-202. 

Taylor P. 1985. Anticholinesterase agents. Chapter 6. In Gilman AG, Goodman LS, Rail TW, et al., eds. Goodman and Gilman s the pharmacological basis of therapeutics. 7th ed.. New York, NY MacMillan Publishing Co. 110-129. ... 

Hohnstedt, B. (1963). Structure-activity relationships of the organophosphorous anticholinesterase agents. In G.B. Keolle (Ed.) Chohnesterases and Antichohnesterase Agents. Handbuch der Experimentelle Phamacologie 15,428 85. 

GB is a lethal anticholinesterase agent. Its toxic hazard is high for inhalation, ingestion, and eye/skin exposure. Due to its high volatility, it is mainly an... 

Famoxon is about 100 times more effective than famphur in controlling houseflies (Musca spp.), which confirms the generalization that the corresponding oxons are the most effective anticholinesterase agents and are, in fact, the actual toxicants (O Brien et al. 1965). 

Albuquerque EX, Akaike A, Shaw KP, Rickett DL. The interaction of anticholinesterase agents with the acetylcholine receptor-channel complex. Fundam. Appl. Toxicol. 4 S27-S33, 1984. 

EFFECTS OF OVEREXPOSURE GA is an anticholinesterase agent similar in action to GB. Although only about half as toxic as GB by inhalation, GA in low concentrations is more irritating to the eyes than GB. 

Catalysis of the C-alkylation of 5-methyoxy-l,3-dimethyloxindole with chloroacetonitrile by A-(3,4-dichlorobenzyl)cinchoninium or quininium chloride leads in good yield to the (5)-3-alkylatcd derivative (78% ee), which provides an efficient stereospecific route to the anticholinesterase agent, (-)-physostigmine [9]. Other analogous alkylation reactions have been reported [10]. 

H. M. Greenblatt, H. Dvir, 1. Sdman, J. L. Sussman Acetylcholinesterase a multifaceted target for structure-based drug design of anticholinesterase agents for the treatment of Alzheimer s disease. J Mol Neurosci 2003, 20, 369-383. 

Toxicology. Carbaryl is a short-acting anticholinesterase agent with the important characteristic of rapid reversibility of inhibition of the enzyme. 

Toxieology. Chlorpyrifos is an anticholinesterase agent, but it has only moderate capacity to reduce red blood cell... 

Koelle GB (ed) Cholinesterases and anticholinesterase agents. Handbuch der Experi-menteUen Pharmakologie, Vol 15, pp 989-1027. Berlin, Springer-Verlag, 1963... 

Koelle GB Anticholinesterase agents. In Goodman LS, Gilman A (eds) The Pharma-cological Basis of Therapeutics, 5th ed, pp 456-466. New York, Macmillan, 1975... 

Complete symptomatic recovery usually occurs within a week increased susceptibility to the effects of anticholinesterase agents persists for up to several weeks after exposure. Daily exposure to concentrations that are insufficient to produce symptoms after a single exposure may result in the onset of symptoms. Continued daily exposure may be followed by increasingly severe effects. 

Uses. As a flame retardant, a preignition additive for gasoline, an antifoam agent, a plasticizer and stabilizer, a textile conditioner, and an antistatic agent used experimentally to mimic the physical and spectroscopic (but not biological) properties of anticholinesterase agents... 

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