Protein Information

Name cholinesterases
Synonyms Acylcholine acylhydrolase; BCHE; BCHE protein; Butyrylcholine esterase; Butyrylcholinesterase; CHE1; Choline esterase II; Cholinesterase…

Compound Information

Name trichlorfon
CAS

Reference List

PubMed Abstract RScore(About this table)
18825528 Pohanka M, Jun D, Kuca K: In vitro reactivation of trichlorfon-inhibited butyrylcholinesterase using HI-6, obidoxime, pralidoxime and K048. J Enzyme Inhib Med Chem. 2008 Sep 29:1.
249(3,3,4,4) Details
7325477 Gingerich DA, Mia AS: Clinical toxicosis and erythrocyte cholinesterase inhibition of trichlorfon combined with mebendazole in horses. Am J Vet Res. 1981 Sep;42(9):1645-50.
162(2,2,2,2) Details
18968024 Wan K, Chovelon JM, Jaffrezic-Renault N: Enzyme-octadecylamine Langmuir-Blodgett membranes for ENFET biosensors. Talanta. 2000 Jul 31;52(4):663-70.

Langmuir-Blodgett (LB) films containing butyrylcholinesterase (BuChE) are fabricated to realise an enzymatic field effect transistor (ENFET) for the detection of organophosphorus pesticides in water.
Trichlorfon as a common pesticide is examined in our work.
3(0,0,0,3) Details
10507245 Heinig R, Sachse R: The effect of food and time of administration on the pharmacokinetic and pharmacodynamic profile of metrifonate. Int J Clin Pharmacol Ther. 1999 Sep;37(9):456-64.


OBJECTIVE: Metrifonate--via its pharmacologically active metabolite DDVP--is an inhibitor of cholinesterase effective in the treatment of Alzheimer's disease.
3(0,0,0,3) Details
6733596 Slott V, Ecobichon DJ: An acute and subacute neurotoxicity assessment of trichlorfon. . Can J Physiol Pharmacol. 1984 May;62(5):513-8.

In the acute studies, both DFP and trichlorfon markedly inhibited tissue cholinesterase activities but only DFP elicited a significant inhibition of NTE.
82(1,1,1,2) Details
3601008 Hallak M, Giacobini E: A comparison of the effects of two inhibitors on brain cholinesterase. . Neuropharmacology. 1987 Jun;26(6):521-30.

9(0,0,0,9) Details
405055 Zinkl JG, Henny CJ, DeWeese LR: Brain cholinesterase activities of birds from forests sprayed with trichlorfon (Dylox) and carbaryl (Sevin-4-oil). Bull Environ Contam Toxicol. 1977 Apr;17(4):379-86.
7(0,0,1,2) Details
9875697 Astroff AB, Freshwater KJ, Eigenberg DA: Comparative organophosphate-induced effects observed in adult and neonatal Sprague-Dawley rats during the conduct of multigeneration toxicity studies. Reprod Toxicol. 1998 Nov-Dec;12(6):619-45.

Five organophosphates: tribufos, oxydemeton-methyl, fenamiphos, coumaphos, and trichlorfon were evaluated for their potential to produce reproductive and neonatal toxicity following continuous dietary exposure during multigenerational reproduction toxicity studies in the Sprague-Dawley rat.
Significant inhibition of parental cholinesterase activities (plasma, erythrocyte, and brain) was similarly observed in both generations with all test compounds, with at least the highest concentrations.
3(0,0,0,3) Details
9726626 Giovannini MG, Scali C, Bartolini L, Schmidt B, Pepeu G: Effect of subchronic treatment with metrifonate and tacrine on brain cholinergic function in aged F344 rats. Eur J Pharmacol. 1998 Jul 31;354(1):17-24.


A 75% inhibition of cholinesterase activity was found 18 h after the last metrifonate administration, while only a 15% inhibition was detectable 18 h after the last tacrine administration.
3(0,0,0,3) Details
2073711 Aden-Abdi Y, Villen T, Ericsson O, Gustafsson LL, Dahl-Puustinen ML: Metrifonate in healthy volunteers: interrelationship between pharmacokinetic properties, cholinesterase inhibition and side-effects. Pharmacol Toxicol. 1991 Feb;68(2):137-9.

3(0,0,0,3) Details
11590700 Yavo B, Brunetti IL, da Fonseca LM, Catalani LH, Campa A: Selective activity of butyrylcholinesterase in serum by a chemiluminescent assay. Luminescence. 2001 Sep-Oct;16(5):299-304.

Addition of aliesterase inhibitors, such as fluoride ion and trichlorfon or the cholinesterase inhibitor eserine, totally prevents light emission.
33(0,1,1,3) Details
8068758 Plumlee KH, Richardson ER, Gardner IA, Galey FD: Effect of time and storage temperature on cholinesterase activity in blood from normal and organophosphorus insecticide-treated horses. J Vet Diagn Invest. 1994 Apr;6(2):247-9.

Six horses were treated with 16 g of trichlorfon per os, 6 horses were treated with 15 g of dichlorvos per os, and 10 horses were untreated controls.
6(0,0,0,6) Details
1115426 Silvestri R, Himes JA, Edds GT: Repeated oral administration of coumaphos in sheep: effects on erythrocyte acetylcholinesterase and other constituents. Am J Vet Res. 1975 Mar;36(3):283-7.

Treatment of sheep with an intravenous injection of the organophosphorous compound trichlorfon, insufficient to produce a significant effect on erythrocyte cholinesterase activity, produced additive effects with those of coumaphos.
6(0,0,1,1) Details
19372080 Wu ML, Deng JF: Acute hemolysis caused by incidental trichlorfon exposure. J Chin Med Assoc. 2009 Apr;72(4):214-8.

Trichlorfon (o-o-dimethyl-2,2,2-trichloro-hydroxyethylphosphate), an organophosphate, has a moderately potent anticholinesterase activity.
6(0,0,1,1) Details
3524957 Aquilonius SM, Hartvig P: Clinical pharmacokinetics of cholinesterase inhibitors. . Clin Pharmacokinet. 1986 May-Jun;11(3):236-49.

5(0,0,0,5) Details
18968581 Reybier K, Zairi S, Jaffrezic-Renault N, Fahys B: The use of polyethyleneimine for fabrication of potentiometric cholinesterase biosensors. Talanta. 2002 Apr 8;56(6):1015-20.

The BuChE-electrode was tested as biochemical sensor for detection of an organophosphorus pesticide, trichlorfon in liquid, the detection being based on the enzyme inhibition.
33(0,1,1,3) Details
16119488 Roberts DM, Fraser JF, Buckley NA, Venkatesh B: Experiences of anticholinesterase pesticide poisonings in an Australian tertiary hospital. Anaesth Intensive Care. 2005 Aug;33(4):469-76.

Two cases of intermediate syndrome were attributed to fenthion and diazinon, and one case of delayed polyneuropathy to trichlorfon.
5(0,0,0,5) Details
10096702 Williams BR: Metrifonate: a new agent for the treatment of Alzheimer's disease. Eksp Med Morfol. 1979;18(1):31-5.


The pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of metrifonate, a long-acting cholinesterase inhibitor, are discussed.
5(0,0,0,5) Details
10743648 Gimenez-Pardo C, Ros Moreno RM, De Armas-Serra C, Rodriguez-Caabeiro F: Presence of cholinesterases in Echinococcus granulosus protoscolices. Parasite. 2000 Mar;7(1):47-50.

4(0,0,0,4) Details
9543465 Crismon ML: Pharmacokinetics and drug interactions of cholinesterase inhibitors administered in Alzheimer's disease. Bioelectrochemistry. 2002 Jan;55(1-2):75-7.

4(0,0,0,4) Details
11789125 Schreiter Gasser U, Gasser T: [A comparison of cholinesterase inhibitors and ginkgo extract in treatment of Alzheimer dementia]. Acta Vet Scand. 1988;29(1):51-5.

4(0,0,0,4) Details
9329715 Lahiri DK, Farlow MR, Nurnberger JI Jr, Greig NH: Effects of cholinesterase inhibitors on the secretion of beta-amyloid precursor protein in cell cultures. Ann N Y Acad Sci. 1997 Sep 26;826:416-21.

4(0,0,0,4) Details
2810476 Hildebrand SV, Hill T 3rd, Holland M: The effect of the organophosphate trichlorfon on the neuromuscular blocking activity of atracurium in halothane-anesthetized horses. J Vet Pharmacol Ther. 1989 Sep;12(3):277-82.

To determine whether cholinesterase inhibition by an organophosphate would influence atracurium's neuromuscular blockade, six horses were anesthetized and paralyzed with atracurium (total of five injections per horse) on experimental Day 1, then were given trichlorfon (64 mg/kg per os) 6 days later.
32(0,1,1,2) Details
9865625 Wakakura M, Utsunomiya-Kawasaki I, Ishikawa S: Rapid increase in cytosolic calcium ion concentration mediated by acetylcholine receptors in cultured retinal neurons and Muller cells. Bull World Health Organ. 1990;68(6):731-6.

Intracellular calcium ion concentration ([Ca2+] i) following the administration of acetylcholine, a cholinesterase inhibitor (trichlorfon), nicotine or muscarinic agonist with or without a receptor antagonist was monitored using the calcium ion indicator, fura-2.
32(0,1,1,2) Details
8981616 Kronforst-Collins MA, Moriearty PL, Ralph M, Becker RE, Schmidt B, Thompson LT, Disterhoft JF: Metrifonate treatment enhances acquisition of eyeblink conditioning in aging rabbits. Pharmacol Biochem Behav. 1997 Jan;56(1):103-10.


In response, a therapeutic approach to Alzheimer's disease has been to attempt to compensate for the decrease in central cholinergic function by potentiating the activity of the remaining intact cholinergic cells with cholinesterase inhibitors.
4(0,0,0,4) Details
11234910 Mega MS, Cummings JL, O'Connor SM, Dinov ID, Reback E, Felix J, Masterman DL, Phelps ME, Small GW, Toga AW: Cognitive and metabolic responses to metrifonate therapy in Alzheimer disease. Acta Physiol Pharmacol Bulg. 1981;7(2):38-42.


OBJECTIVE: The objective of this study was to identify the relation between the cognitive benefit seen with the cholinesterase inhibitor metrifonate and changes in brain metabolism as visualized with [18F]-fluorodeoxyglucose positron emission tomography (FDG-PET).
4(0,0,0,4) Details
2725846 Hallak M, Giacobini E: Physostigmine, tacrine and metrifonate: the effect of multiple doses on acetylcholine metabolism in rat brain. Neuropharmacology. 1989 Mar;28(3):199-206.


The effects of two consecutive intramuscular doses of three cholinesterase inhibitors (physostigmine, tetrahydroaminoacridine and metrifonate) were compared in rats.
4(0,0,0,4) Details
8175053 Miyata M, Namba T, Horiuchi K, Aoki S, Ishikawa S: Aggravation of experimental allergic conjunctivitis by environmental chemical and physical factors. Fortschr Med Orig. 2001 Nov 29;119(3-4):135-8.

The effects of trichlorfon (DEP, Dipterex, anticholinesterase pesticide) and paraquat dichloride (Gramoxon, inhibitor of superoxide dismutase) on passive anaphylactic reaction in guinea pig conjunctiva using Japanese cedar pollen were quantitatively studied.
31(0,1,1,1) Details
10794385 Sheets LP: A consideration of age-dependent differences in susceptibility to organophosphorus and pyrethroid insecticides. Neurotoxicology. 2000 Feb-Apr;21(1-2):57-63.

The first involves multi-generation reproduction studies with rats that were treated with OP insecticides (coumaphos, fenamiphos, tribufos, trichlorfon, or oxydemeton-methyl) through the diet and examined for effects, including cholinesterase (ChE) inhibition.
31(0,1,1,1) Details
9139240 Hinz V, Grewig S, Schmidt BH: Metrifonate and dichlorvos: effects of a single oral administration on cholinesterase activity in rat brain and blood. Folia Med Cracov. 1993;34(1-4):129-38.

10(0,0,0,10) Details
7344408 Machemer L: Chronic toxicity of metrifonate. 1-96.

The toxicological profile of trichlorfon in the chronic toxicity study consists, on the one hand, in a depression of cholinesterase activity whereby the different animal species differed in their sensitivity.
9(0,0,1,4) Details
1236006 Khinkova L, Kaloianova F, Dimov S, Atsev E: [Comparative study of the changes in the EEG and cholinesterase activity in experimental Dipterex poisoning]. Arch Invest Med. 1984 Oct-Dec;15(4):349-61.

4(0,0,0,4) Details
1209993 Kr'stev E: [Study of the activity of erythrocyte cholinesterase in healthy and dipterex-poisoned sheep and cattle]. Vet Med Nauki. 1975;12(1):10-5.

4(0,0,0,4) Details
8804059 Bjorklund M, Jakala P, Schmidt B, Riekkinen M, Koivisto E, Riekkinen P Jr: An indirect cholinesterase inhibitor, metrifonate, increases neocortical EEG arousal in rats. Exp Neurol. 2002 Feb;173(2):196-204.

3(0,0,0,3) Details
14535624 Rakonczay Z: Potencies and selectivities of inhibitors of acetylcholinesterase and its molecular forms in normal and Alzheimer's disease brain. Acta Biol Hung. 2003;54(2):183-9.


Eight inhibitors of acetylcholinesterase (AChE), tacrine, bis-tacrine, donepezil, rivastigmine, galantamine, heptyl-physostigmine, TAK-147 and metrifonate, were compared with regard to their effects on AChE and butyrylcholinesterase (BuChE) in normal human brain cortex.
3(0,0,0,3) Details
7344415 Reiner E: Esterases in schistosomes: reaction with substrates and inhibitors. . Acta Pharmacol Toxicol. 1981;49 Suppl 5:72-8.


Studies were made (at 37 degrees, pH 7.6) on the interaction of some organophosphorus compounds and carboxylic acid esters with cholinesterases (EC 3.1.1.7 and EC 3.1.1.8) and A-esterases (EC 3.1.1.2) in homogenates of Schistosoma mansoni (adults and cercariae) and Schistosoma haematobium (adults).
3(0,0,0,3) Details
9139239 Hinz VC, Grewig S, Schmidt BH: Metrifonate induces cholinesterase inhibition exclusively via slow release of dichlorvos. Neurochem Res. 1996 Mar;21(3):331-7.

3(0,0,0,3) Details
8768721 van der Staay FJ, Hinz VC, Schmidt BH: Effects of metrifonate, its transformation product dichlorvos, and other organophosphorus and reference cholinesterase inhibitors on Morris water escape behavior in young-adult rats. J Pharmacol Exp Ther. 1996 Aug;278(2):697-708.

2(0,0,0,2) Details
1711162 Soininen H, Unni L, Shillcutt S: Effect of acute and chronic cholinesterase inhibition on biogenic amines in rat brain. Neurochem Res. 1990 Dec;15(12):1185-90.

2(0,0,0,2) Details
11420082 Ikonen S, Tanila H: Effects of metrifonate on the hippocampal theta rhythm of freely moving intact and MS-lesioned mice. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):165-72.


Spatial learning can be improved in medial septal (MS)-lesioned mice by metrifonate, a cholinesterase inhibitor.
2(0,0,0,2) Details
10599054 Moriearty PL, Seubert P, Galasko D, Markwell S, Unni L, Vicari S, Becker RE: Effects of time and cholinesterase inhibitor treatment on multiple cerebrospinal fluid parameters in Alzheimer's disease. Methods Find Exp Clin Pharmacol. 1999 Oct;21(8):549-54.

2(0,0,0,2) Details
10478948 Dachir S, Schmidt BH, Levy A: Kinetics of brain cholinesterase inhibition following metrifonate administration. Neurochem Res. 1999 Aug;24(8):1075-80.

2(0,0,0,2) Details
7184787 Nordgren I: Quantitation of metrifonate and dichlorvos in blood and tissues by gas chromatography-mass spectrometry. Fundam Appl Toxicol. 1981 Mar-Apr;1(2):230-7.


The results were compared to erythrocyte and plasma cholinesterase determinations.
2(0,0,0,2) Details
15163438 Bouger PC, Spowart-Manning L, Ferrara A, Schmidt BH, van der Staay FJ: Effects of acute and repeated administration of a cholinesterase inhibitor on timing behaviour. Eur Neuropsychopharmacol. 2004 Aug;14(4):285-94.

2(0,0,0,2) Details
11822883 Liu L, Ikonen S, Heikkinen T, Tapiola T, van Groen T, Tanila H: The effects of long-term treatment with metrifonate, a cholinesterase inhibitor, on cholinergic activity, amyloid pathology, and cognitive function in APP and PS1 doubly transgenic mice. Tsitologiia. 1985 Jun;27(6):633-8.

2(0,0,0,2) Details
235931 Reiner E, Krauthacker B, Simeon V, Skrinjaric-Spoljar M: Mechanism of inhibition in vitro of mammalian acetylcholinesterase and cholinesterase in solutions of 0,0-dimethyl 2,2,2-trichloro-1-hydroxyethyl phosphonate (Trichlorphon). Biochem Pharmacol. 1975 Mar 15;24(6):717-22.

1(0,0,0,1) Details
4656609 Bueding E, Liu CL, Rogers SH: Inhibition by metrifonate and dichlorvos of cholinesterases in schistosomes. Br J Pharmacol. 1972 Nov;46(3):480-7.

1(0,0,0,1) Details
15888665 Quistad GB, Klintenberg R, Casida JE: Blood acylpeptide hydrolase activity is a sensitive marker for exposure to some organophosphate toxicants. Toxicol Sci. 2005 Aug;86(2):291-9. Epub 2005 May 11.

Mouse blood and brain APH and blood butyrylcholinesterase (BChE) are of similar sensitivity to DFP in vitro and in vivo (ip and vapor exposure), but APH inhibition is much more persistent in vivo (still > 80% inhibition after 4 days).
The inhibitory potency of OP pesticides in vivo in mice varies from APH selective (dichlorvos, naled, and trichlorfon), to APH and BChE selective (profenofos and tribufos), to ChE selective or nonselective (many commercial insecticides).
1(0,0,0,1) Details
703701 Sokhanenkova TL, Lineva VA: [Change in the cholinesterase properties of the head portion of the housefly (Musca domestica L., 1758) in its development of resistance to DDT and chlorophos] Med Parazitol. 1978 Sep-Oct;47(5):92-5.

1(0,0,0,1) Details
3621504 Ren HN, Luo KJ, Cheng BZ: [Effects of various anti-hookworm drugs on the cholinesterase activity of Necator americanus, Ancylostoma duodenale, Ancylostoma caninum and Nippostrongylus braziliensis] Zhongguo Ji Sheng Chong Xue Yu Ji Sheng Chong Bing Za Zhi. 1987;5(1):13-7.

1(0,0,0,1) Details
2379248 Kassa J: [Use of peritoneal dialysis as a therapeutic method in poisoning by Neguvon]. Cesk Farm. 1990 Feb;39(1):7-10.


A closer examination of the effect of the individual components of the dialysate for Neguvon poisoning revealed that approximately 60% of the effect of treatment is due to albumin, 40% to butyrylcholinesterase in the administered plasma.
2(0,0,0,2) Details
5147622 Selivanova AS, Molodykh ZhV: [Effect of chlorophos analogs on the cholinesterase of chick ascaridia and swine ascarids. Med Parazitol. 1971 Nov-Dec;40(6):674-6.

2(0,0,0,2) Details
8107298 Yamanaka S, Yoshida M, Yamamura Y, Nishimura M, Takaesu Y: [A study on acute organophosphorus poisoning--changes in the activity and isoenzyme patterns of serum cholinesterase in human poisoning]. Nippon Eiseigaku Zasshi. 1993 Dec;48(5):955-65.

Fenitrothion, Malathion, Isoxathion, Pyridaphenthion and Trichlorfon, and studied on the changes in the activity and isoenzyme patterns of serum ChE after ingestion.
2(0,0,0,2) Details
1206768 Davis A: Clinically available antischistosomal drugs. J Toxicol Environ Health. 1975 Nov;1(2):191-201.


Metrifonate, a cholinesterase-inhibiting organophosphorus compound, is effective only against S. hematobium.
1(0,0,0,1) Details
8784247 Bassant MH, Jazat-Poindessous F, Lamour Y: Effects of metrifonate, a cholinesterase inhibitor, on local cerebral glucose utilization in young and aged rats. J Cereb Blood Flow Metab. 1996 Sep;16(5):1014-25.

2(0,0,0,2) Details
11419566 Cummings JL, Nadel A, Masterman D, Cyrus PA: Efficacy of metrifonate in improving the psychiatric and behavioral disturbances of patients with Alzheimer's disease. J Geriatr Psychiatry Neurol. 2001 Summer;14(2):101-8.


This study was a retrospective analysis of pooled NPI data from two double-blind, placebo-controlled, multicenter 26-week studies of metrifonate that had achieved similar levels of cholinesterase inhibition.
1(0,0,0,1) Details
5150100 Gaultier M, Pebay-Peyroula F, Lecorsier A: [Drop in blood cholinesterase in the course of treatment of onchocerciasis by an organophosphorus compound (Metrifonate)] Eur J Toxicol. 1971 Sep-Oct;4(5):429-31.

1(0,0,0,1) Details
1564112 Unni LK, Hannant ME, Becker RE: High-performance liquid chromatographic method using ultraviolet detection for measuring metrifonate and dichlorvos levels in human plasma. J Chromatogr. 1992 Jan 3;573(1):99-103.


We report high-performance liquid chromatographic methods using ultraviolet detection, developed for the first time in our laboratory with sensitivity to detect clinically significant concentrations of metrifonate (MTF), an experimental drug for Alzheimer disease, and its active anticholinesterase metabolite, dichlorvos (DDVP).
1(0,0,0,1) Details
8051989 Unni LK, Womack C, Hannant ME, Becker RE: Pharmacokinetics and pharmacodynamics of metrifonate in humans. Methods Find Exp Clin Pharmacol. 1994 May;16(4):285-9.


We studied the pharmacokinetics and pharmacodynamics [red blood cell (RBC) cholinesterase (ChE) inhibition] of metrifonate (MTF) and its active anti-ChE metabolite, dichlorvos (DDVP) in Alzheimer's disease (AD) patients and normal controls after oral MTF.
1(0,0,0,1) Details
9449438 Dachir S, Schmidt B, Levy A: Effects of metrifonate on radial arm maze acquisition in middle-aged rats. Brain Res. 1997 Nov 28;777(1-2):251-4.


The efficacy of metrifonate, a well-tolerated cholinesterase (ChE) inhibitor, in attenuating the normal aging- and corticosterone-induced impairments of radial maze performance of rats was compared.
1(0,0,0,1) Details
7247612 Trujillo-Valdes VM, Gonzalez-Barranco D, Orozco-Bohne R, Villanueva-Diaz G, Sandoval-Islas ME: Experimental treatment of cysticercosis with metrifonate. Arch Invest Med. 1981;12(1):15-28.


The results obtained after treatment demonstrated the effectivity in cerebral ocular and musculocutaneous cysticercosis, corroborated by clinical evaluations like: neurological, ophtalmological and psychiatric examinations; routine laboratory tests; special examinations like indirect immunofluorescence and hemagglutination, immunoglobulin quantitation and cholinesterase activity and by special cabinet studies like electroencephalogram, retinal fluorangiography, axial computerized tomography.
1(0,0,0,1) Details
813485 Richter D, Runde H: [Effect of organophosphorus compounds on esterases in rat intestine- a comparing histochemical and biochemical investigation (author's transl)]. Acta Histochem. 1975;54(1):56-65.


They differ in cholinesterases.
1(0,0,0,1) Details
9595961 Knopman DS: Metrifonate for Alzheimer's disease: is the next cholinesterase inhibitor better? Neurology. 1998 May;50(5):1203-5.

1(0,0,0,1) Details
11402526 : Evaluation of certain veterinary drug residues in food. World Health Organ Tech Rep Ser. 2001;900:i-vi

The first part of the report considers the interpretation of data on inhibition of cholinesterase activity and recommendations arising from an informal meeting on harmonization with the Joint FAO/WHO Meeting on Pesticide Residues.
A summary follows of the Committee's evaluations of toxicological and residue data on a variety of veterinary drugs: one anthelminthic agent (ivermectin); four antimicrobial agents (flumequine, lincomycin, oxytetracycline and tilmicosin); six insecticides (cyhalothrin, cypermethrin, alpha-cypermethrin, dicyclanil, permethrin and metrifonate (trichlorfon)); and one production aid (melengestrol acetate).
1(0,0,0,1) Details
9122369 Riekkinen P Jr, Schmidt B, Jakala P, Koivisto E, Bjorklund M: Chronic nimodipine and acute metrifonate treatment decreases age-related cortical high voltage spindles in rats. Psychopharmacology. 1997 Jan;129(1):91-5.


The threshold dose of metrifonate, a cholinesterase inhibitor, for suppression of HVSs was lower in nimodipine compared to placebo treated aged rats (30 mg/kg versus 60 mg/kg; p.o.).
1(0,0,0,1) Details
8570013 Mori F, Cuadra G, Giacobini E: Metrifonate effects on acetylcholine and biogenic amines in rat cortex. Neurochem Res. 1995 Sep;20(9):1081-8.


The effect of systemic and local administration of metrifonate (MTF), a long-acting cholinesterase inhibitor (ChEl) on extracellular levels of acetylcholine (ACh), norepinephrine (NE), dopamine (DA) and serotonin (5-HT) was investigated in the rat cortex by using transcortical microdialysis.
1(0,0,0,1) Details
2628016 Priputina LS, Predtechenskii MB, Levkovich IuI: [Cerebral blood flow function during altered cholinergic mediation] . Fiziol Zh SSSR Im I M Sechenova. 1989 Nov;75(11):1589-95.


The study of cerebral blood flow was performed with the aid of hydrogen clearance technique and the cinema-television method in alteration of cholinergic transmission by means of phosphorus-organic inhibitors of cholinesterase and a cholinolytic agent in unanesthetized rats.
1(0,0,0,1) Details
10867446 Farlow MR, Cyrus PA: Metrifonate therapy in Alzheimer's disease: a pooled analysis of four randomized, double-blind, placebo-controlled trials. Dement Geriatr Cogn Disord. 2000 Jul-Aug;11(4):202-11.


Metrifonate is the first cholinesterase inhibitor consistently shown under prospective, placebo-controlled conditions to improve significantly behavior in addition to cognition, function in activities of daily living and global functional status of patients with mild to moderate AD.
1(0,0,0,1) Details
6283788 Le Quesne PM, Maxwell IC: Effect of metrifonate on neuromuscular transmission. Acta Pharmacol Toxicol. 1981;49 Suppl 5:99-104.


The least detectable effect of acute cholinesterase inhibition (produced by edrophonium) in a normal subject is described.
1(0,0,0,1) Details
10024365 Oh MM, Power JM, Thompson LT, Moriearty PL, Disterhoft JF: Metrifonate increases neuronal excitability in CA1 pyramidal neurons from both young and aging rabbit hippocampus. J Neurosci. 1999 Mar 1;19(5):1814-23.


The effects of metrifonate, a second generation cholinesterase inhibitor, were examined on CA1 pyramidal neurons from hippocampal slices of young and aging rabbits using current-clamp, intracellular recording techniques.
1(0,0,0,1) Details
6535521 Martinez-Zedillo G, Gonzalez-Barranco D, Rebolledo-Camacho P, Lara-Nunez MA: Kinetic aspects of Taenia solium metacestode cholinesterases and their inhibition with DDVP and neostigmine. Neuropsychiatry Neuropsychol Behav Neurol. 2001 Jan;14(1):63-8.

1(0,0,0,1) Details
624050 James MF, Jewsbury JM: Schistosomiasis, metriphonate, cholinesterase, and suxamethonium. Br Med J. 1978 Feb 18;1(6110):442.

1(0,0,0,1) Details
4024256 Tomilin NV, Kuznetsov VG, Kubarskaia LG, Mashanskii VF: [Ultrastructural changes in the muscle fibers of the rat diaphragm and the dynamics of intracellular calcium redistribution as affected by an anticholinesterase substance--chlorophos]. J Clin Psychiatry. 1996;57 Suppl 14:30-6.

1(0,0,0,1) Details
9088864 Itoh A, Nitta A, Katono Y, Usui M, Naruhashi K, Iida R, Hasegawa T, Nabeshima T: Effects of metrifonate on memory impairment and cholinergic dysfunction in rats. Eur J Pharmacol. 1997 Mar 12;322(1):11-9.


The basal forebrain lesion decreased the cholinesterase activity in the cerebral cortex, and metrifonate (100 mg/kg) further reduced the cholinesterase activity.
1(0,0,0,1) Details
12649296 Samochocki M, Hoffle A, Fehrenbacher A, Jostock R, Ludwig J, Christner C, Radina M, Zerlin M, Ullmer C, Pereira EF, Lubbert H, Albuquerque EX, Maelicke A: Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors. J Pharmacol Exp Ther. 2003 Jun;305(3):1024-36. Epub 2003 Mar 20.


These studies support our previous proposal that the therapeutic action of galantamine is mainly produced by its sensitizing action on nAChRs rather than by general cholinergic enhancement due to cholinesterase inhibition.
1(0,0,0,1) Details
9877077 Poindessous-Jazat F, Schmidt BH, Bassant MH: Effect of subchronic metrifonate treatment on cerebral glucose metabolism in young and aged rats. Eur J Pharmacol. 1998 Dec 11;363(1):17-28.


The effects of subchronic administration of metrifonate, a long-lasting cholinesterase inhibitor, on local cerebral glucose utilization were assessed in 3- and 27-month old Sprague-Dawley rats, using the autoradiographic [14C] 2-deoxyglucose technique.
1(0,0,0,1) Details
6614577 Splisteser H, Muller B, Zerenlcham N, Hornawsky G, Betke P, Gossing S: [Effectiveness, tolerance, and residue formation of trichlorbon 6%-"new" in controlling hypodermyiasis in cattle in the Mongolian People's Republic]. Angew Parasitol. 1983 May;24(2):86-94.


The inhibition of the activity of cholinesterase was moderate but longer lasting than with other preparations.
1(0,0,0,1) Details
436709 Dzhirkolova T, Dishovski Kh, Rusev G: [Changes in the transverse striated musculature during treatment with the pesticide, Neguvon, and TMB-4 reactivator]. Acta Med Okayama. 1975 Jun;29(3):233-6.


The reaktivator of cholinesterase TMB-4 (20 mg/kg) recovered the contractile capability of myofibres even on the third day after treatment, but superprecipitation of myosin B-after the twentieth day.
1(0,0,0,1) Details
9376763 Elaeva NL, Predtechenskii MB, Kul'bitskii GN, Babaina EV, Trefilov VV: [The pharmacokinetic interaction of cholinolytics and cholinesterase reactivators as a reflection of the modulation of their binding in blood plasma and in brain tissue]. Eksp Klin Farmakol. 1997 Jul-Aug;60(4):64-7.

1(0,0,0,1) Details
5167527 Selivanova AS, Molodykh ZhV: [Effect of some chlorophos analogs on cholinesterase of chicken and swine ascaridia] Med Parazitol. 1971 Sep-Oct;40(5):534-7.

1(0,0,0,1) Details
9388884 Sun D, Zhou H, Huang J: [Twenty-years health surveillance of workers in dipterex packaging] . Zhonghua Yu Fang Yi Xue Za Zhi. 1996 Sep;30(5):273-5.


Data of health surveillance from 1970 to 1989 for the workers employed in dipterex packaging were collected and statistically analyzed with a microcomputer by scoring their whole blood choline esterase activities and symptoms and signs.
1(0,0,0,1) Details
12425964 Honorato de Oliveira G, Moreira V, Ribeiro Goes SP: Organophosphate induced delayed neuropathy in genetically dissimilar chickens: studies with tri-ortho-cresyl phosphate (TOCP) and trichlorfon. Toxicol Lett. 2002 Dec 15;136(2):143-50.

Measurements of plasma cholinesterase (pl.ChE), brain cholinesterase (Br.ChE) and brain Neuropathy Target Esterase (Br.NTE) were made in three different lineages of chickens.
1(0,0,0,1) Details
127517 Okuyama A, Arima T, Goto Y, Imai M, Haraoka S: [A case of hypocholinesterasemia induced by trichlorfon] . Probl Khig. 1975;1:39-44.

Laboratory examination performed on the admission disclosed a serum cholinesterase activity of 0.3deltapH per hour.
1(0,0,0,1) Details
3718886 Hu XH, Lu YP, Xue SZ, Ling YX, Gu XQ: Toxicity of dipterex: a field study. Br J Ind Med. 1986 Jun;43(6):414-9.


The findings suggest that both airborne dipterex and dermal contamination contribute to the inhibition of blood cholinesterase (ChE) and that cases of poisoning in hot seasons can be attributed mainly to dermal absorption.
1(0,0,0,1) Details
9720485 Tariot PN: Evaluating response to metrifonate. J Clin Psychiatry. 1998;59 Suppl 9:33-7.


In combination, these pharmacologic characteristics lead to a reduced side effect profile in comparison with several other cholinesterase inhibitors.
1(0,0,0,1) Details
9383522 Kronforst-Collins MA, Moriearty PL, Schmidt B, Disterhoft JF: Metrifonate improves associative learning and retention in aging rabbits. Behav Neurosci. 1997 Oct;111(5):1031-40.


In response, a therapeutic approach to AD has been to attempt to compensate for the decrease in central cholinergic function by potentiating the activity of the remaining intact cholinergic cells with cholinesterase (ChE) inhibitors.
1(0,0,0,1) Details
3524328 Seibert BP, Newcomb KM, Michael BF: Critical test and safety evaluations of an oral paste preparation of mebendazole and trichlorfon in horses. Am J Vet Res. 1986 Jun;47(6):1347-50.

Transient clinical signs of organophosphate toxicosis (primarily the passage of loose feces) and prolonged inhibition of erythrocyte cholinesterase activity were evident within 1 hour after drug treatment.
1(0,0,0,1) Details
10365643 Dingemanse J, Halabi A, Kleinbloesem CH, Heinig R, Blume H: Pharmacokinetics and pharmacodynamics of the acetylcholinesterase inhibitor metrifonate in patients with renal impairment. Ther Drug Monit. 1999 Jun;21(3):310-6.


Inhibition of acetylcholinesterase activity in erythrocytes and butyrylcholinesterase in plasma were also measured.
1(0,0,0,1) Details
9543466 Jann MW: Preclinical pharmacology of metrifonate. Pharmacotherapy. 1998 Mar-Apr;18(2 Pt 2):55-67; discussion 79-82.


Metrifonate is converted by a nonenzymatic process to the long-acting cholinesterase inhibitor 2,2-dichlorovinyl dimethyl phosphate (DDVP).
1(0,0,0,1) Details
4667852 Liniuchev NM, Mima IuP, Sergeev VV: [Effect of phenobarbital on the toxicity and anticholinesterase activity of chlorophos] Gig Sanit. 1972 Oct;37(10):106-7.

1(0,0,0,1) Details
12111444 Scali C, Casamenti F, Bellucci A, Costagli C, Schmidt B, Pepeu G: Effect of subchronic administration of metrifonate, rivastigmine and donepezil on brain acetylcholine in aged F344 rats. J Neural Transm. 2002 Jul;109(7-8):1067-80.


Eighteen h after the last administration, cholinesterase inhibition was 85, 52 and 39% after metrifonate, rivastigmine and donepezil, respectively, and was accompanied by 988, 590 and 75% increase in cortical acetylcholine level.
1(0,0,0,1) Details
7358304 Sholokhov VM, Kizhaev EV, Verin DM: [Micro express method of measuring pH for determining blood cholinesterase activity] Gig Sanit. 1980 Feb;(2):60-1.

1(0,0,0,1) Details
9690734 Hinz VC, Kolb J, Schmidt BH: Effects of subchronic administration of metrifonate on cholinergic neurotransmission in rats. Neurochem Res. 1998 Jul;23(7):931-8.


The effects of subchronic oral administration of metrifonate, a long-acting cholinesterase (ChE) inhibitor, on cholinergic neurotransmission were assessed in young adult male Wistar rats.
1(0,0,0,1) Details
6194775 Kravtsova GB: [Morpho-functional changes in the liver after exposure to cholinesterase inhibitors]. Arkh Anat Gistol Embriol. 1983 Jul;85(7):55-62.

1(0,0,0,1) Details
10025821 Sandson TA: Metrifonate for Alzheimer's disease: is the next cholinesterase inhibitor better? Gen Pharmacol. 1983;14(6):689-91.

1(0,0,0,1) Details
4809600 Bello TR, Amborski GF, Torbert BJ: Effects of organic phosphorus anthelmintics on blood cholinesterase values in horses and ponies. Am J Vet Res. 1974 Jan;35(1):73-8.

1(0,0,0,1) Details
2396286 Dagaev VN, Iskandarov AI, Luzhnikov EA, Gorin EE, Lisovikh ZhA, El'kov AN: [Expert criteria of the degree of severity of the chemical trauma in acute poisonings by organophosphate insecticides]. Sud Med Ekspert. 1990 Apr-Jun;33(2):28-30.


Standard diagrams were plotted which help to assess the life threatening values of the given compounds depending on the initial blood poison level or recorded decrease in enzyme cholinesterase activity.
1(0,0,0,1) Details
9543464 Cummings JL: Metrifonate: overview of safety and efficacy. Pharmacotherapy. 1998 Mar-Apr;18(2 Pt 2):43-6; discussion 79-82.


Metrifonate is a cholinesterase inhibitor with a long-lasting inhibition that raises brain acetylcholine levels.
1(0,0,0,1) Details
8065512 Mehl A, Schanke TM, Johnsen BA, Fonnum F: The effect of trichlorfon and other organophosphates on prenatal brain development in the guinea pig. Neurochem Res. 1994 May;19(5):569-74.

0(0,0,0,0) Details
46730 Silvestri R, Himes JA, Edds GT: Repeated oral administration of coumaphos in sheep: interactions of coumaphos with bishydroxycoumarin, trichlorfon, and phenobarbital sodium. Am J Vet Res. 1975 Mar;36(3):289-92.

0(0,0,0,0) Details
363095 Holmstedt B, Nordgren I, Sandoz M, Sundwall A: Metrifonate. Arch Toxicol. 1978 Oct 13;41(1):3-29.


The organophosphorus compound 0,0-dimethyl-(1-hydroxy-2,2,2-trichloroethyl)-phosphonate was introduced as an insecticide, trichlorfon, in 1952 (Lorenz et al., 1955) and as a drug, metrifonate, in the treatment of schistosomiasis in 1960 (Lebrun and Cerf, 1960).
0(0,0,0,0) Details
18968123 Gogol EV, Evtugyn GA, Marty JL, Budnikov HC, Winter VG: Amperometric biosensors based on nafion coated screen-printed electrodes for the determination of cholinesterase inhibitors. Talanta. 2000 Nov 1;53(2):379-89.

The detection limits were found to be 3.5x10 (-7) M for trichlorfon and 1.5x10 (-7) M for coumaphos.
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8688164 Ghindilis AL, Morzunova TG, Barmin AV, Kurochkin IN: Potentiometric biosensors for cholinesterase inhibitor analysis based on mediatorless bioelectrocatalysis. Biosens Bioelectron. 1996;11(9):873-80.

The detection limit for trichlorfon analysis is 2 x 10 (-13) M.
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15992092 Ringman JM, Cummings JL: Metrifonate (Trichlorfon): a review of the pharmacology, pharmacokinetics and clinical experience with a new acetylcholinesterase inhibitor for Alzheimer's disease. Expert Opin Investig Drugs. 1999 Apr;8(4):463-71.

Metrifonate is a cholinesterase inhibitor, effective in the treatment of both the cognitive and behavioural symptoms of Alzheimer's disease (AD).
2(0,0,0,2) Details
10791297 Unni L, Vicari S, Moriearty P, Schaefer F, Becker R: The recovery of cerebrospinal fluid acetylcholinesterase activity in Alzheimer's disease patients after treatment with metrifonate. Methods Find Exp Clin Pharmacol. 2000 Jan-Feb;22(1):57-61.


We investigated the relationship between peripheral and central cholinesterase (ChE) inhibition levels after chronic treatment of Alzheimer's disease (AD) patients with metrifonate (MTF).
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6662350 Matkovics B, Szabo L, Ivan J, Gaal I: Some further data on the effects of two organophosphate pesticides on the oxidative metabolism in the liver. Am J Health Syst Pharm. 1999 Mar 1;56(5):427-32.


Sumithion is the most active cholinesterase inhibitor.
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9720483 Peskind ER: Pharmacologic approaches to cognitive deficits in Alzheimer's disease. J Clin Psychiatry. 1998;59 Suppl 9:22-7.


Two cholinesterase inhibitors are available for Alzheimer's disease, and others most likely will soon be available.
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8231460 Moriearty PL, Thornton SL, Becker RE: Transdermal patch delivery of acetylcholinesterase inhibitors. . Neurology. 1999 Feb;52(3):675-6.


Transdermal delivery of cholinesterase inhibitors (ChEI) for treatment of dementia would have advantages associated with continuous dosing and enhanced compliance, but feasibility depends on achieving desired levels of central nervous system enzyme inhibition.
2(0,0,0,2) Details
3202059 Buchmann K, Mellergaard S: Histochemical demonstration of the inhibitory effect of Nuvan and Neguvon on cholinesterase activity in Pseudodactylogyrus anguillae (Monogenea). Acta Pharmacol Toxicol. 1981;49 Suppl 5:15-28.

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9163564 Scali C, Giovannini MG, Bartolini L, Prosperi C, Hinz V, Schmidt B, Pepeu G: Effect of metrifonate on extracellular brain acetylcholine and object recognition in aged rats. Eur J Pharmacol. 1997 May 1;325(2-3):173-80.


In old rats, metrifonate (80 mg/kg p.o.) brought about 85% inhibition of cholinesterase activity in the cortex and hippocampus, a 4-fold increase in extracellular acetylcholine levels in the cortex only, and restored object recognition.
1(0,0,0,1) Details
6380243 Gyrd-Hansen N, Kraul I: Obidoxime reactivation of organophosphate-inhibited cholinesterase activity in pigs. Acta Vet Scand. 1984;25(1):86-95.

1(0,0,0,1) Details
12116861 Ros-Moreno RM, De Armas-Serra C, Gimenez-Pardo C, Rodriguez-Caabeiro F: Comparison of cholinesterase activities in the excretion-secretion products of Trichinella pseudospiralis and Trichinella spiralis muscle larvae. Parasite. 2002 Jun;9(2):153-9.

3(0,0,0,3) Details
11001599 Mega MS, Dinov ID, Lee L, O'Connor SM, Masterman DM, Wilen B, Mishkin F, Toga AW, Cummings JL: Orbital and dorsolateral frontal perfusion defect associated with behavioral response to cholinesterase inhibitor therapy in Alzheimer's disease. J Neuropsychiatry Clin Neurosci. 2000 Spring;12(2):209-18.

3(0,0,0,3) Details
9080632 Yamashita M, Yamashita M, Tanaka J, Ando Y: Human mortality in organophosphate poisonings. Vet Hum Toxicol. 1997 Apr;39(2):84-5.

Fenitrothion, malathion, dichlorvos, trichlorfon and fenitrothion/malathion were the most frequent chemicals involved.
About 3/4 of the severely serum cholinesterase-depressed cases needed ventilators.
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18484526 Cui YM, Ao MZ, Li W, Yu LJ: Effect of glabridin from Glycyrrhiza glabra on learning and memory in mice. Planta Med. 2008 Mar;74(4):377-80.


Glabridin was isolated from the roots of Glycyrrhiza glabra and its effects on cognitive functions and cholinesterase activity were investigated in mice.
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11193171 Giacobini E: Cholinesterase inhibitors stabilize Alzheimer's disease. Ann N Y Acad Sci. 2000;920:321-7.

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16458491 Disterhoft JF, Oh MM: Pharmacological and molecular enhancement of learning in aging and Alzheimer's disease. J Physiol Paris. 2006 Mar-May;99(2-3):180-92. Epub 2006 Feb 3.


The studies reviewed here include those using nimodipine, an L-type calcium current blocker that tends to cross the blood-brain barrier; metrifonate, a cholinesterase inhibitor; CI1017, a muscarinic cholinergic agonist; and galantamine, a combined cholinesterase inhibitor and nicotinic agonist.
1(0,0,0,1) Details
9062677 Itoh A, Nitta A, Hirose M, Hasegawa T, Nabeshima T: Effects of metrifonate on impairment of learning and dysfunction of cholinergic neuronal system in basal forebrain-lesioned rats. Behav Brain Res. 1997 Feb;83(1-2):165-7.


Several studies have indicated the possibility of using cholinesterase (ChE) inhibitors as therapeutic drugs for Alzheimer's disease.
1(0,0,0,1) Details
9016911 Jakala P, Riekkinen M, Bjorklund M, Koivisto E, Schmidt B, Riekkinen P Jr: Effects of combined nimodipine and metrifonate on rat cognition and cortical EEG. Neurochem Res. 1996 Mar;21(3):339-45.


The present study investigated if short-term treatment with an L-type Ca2+-channel inhibitor, nimodipine, can stimulate cognitive functioning and cortical electroencephalograph (EEG) arousal, and potentiate the effect of a cholinesterase inhibitor, metrifonate.
1(0,0,0,1) Details
3206954 Menzikova OV: [The cholinesterase properties of Daphnia magna] . Zh Evol Biokhim Fiziol. 1988 Jul-Aug;24(4):596-8.

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10584768 Ringman JM, Cummings JL: Metrifonate: update on a new antidementia agent. J Clin Psychiatry. 1999 Nov;60(11):776-82.


OBJECTIVE: To review preclinical and clinical studies of metrifonate, a cholinesterase inhibitor relevant to the treatment of Alzheimer's disease.
3(0,0,0,3) Details
9718230 Schmidt BH, Heinig R: The pharmacological basis for metrifonate's favourable tolerability in the treatment of Alzheimer's disease. Dement Geriatr Cogn Disord. 1998;9 Suppl 2:15-9.


Metrifonate, through its pharmacologically active metabolite 2,2-dichlorovinyl dimethylphosphate (DDVP), is a long-acting cholinesterase inhibitor for the symptomatic treatment of mild-to-moderate Alzheimer's disease.
3(0,0,0,3) Details
15582113 Spowart-Manning L, van der Staay FJ: Spatial discrimination deficits by excitotoxic lesions in the Morris water escape task. Behav Brain Res. 2005 Jan 30;156(2):269-76.


The effects of the cholinesterase inhibitors (ChEI) metrifonate and donepezil were assessed on spatial performance of rats with bilateral lesions of the entorhinal cortex (EC), which is thought to model early changes in the brains of patients suffering from Alzheimer's disease.
2(0,0,0,2) Details
7344416 Nordgren I, Bengtsson E, Holmstedt B, Pettersson BM: Levels of metrifonate and dichlorvos in plasma and erythrocytes during treatment of schistosomiasis with Bilarcil. Acta Pharmacol Toxicol. 1981;49 Suppl 5:79-86.


Cholinesterase activity in plasma reaches zero levels within 15 min. and remains inhibited for more than eight hours.
2(0,0,0,2) Details
9731544 Schneider LS: New therapeutic approaches to cognitive impairment. J Clin Psychiatry. 1998;59 Suppl 11:8-13.


Clinical pharmacologic approaches toward improvement of cognitive symptoms are discussed, with an emphasis on cholinergic approaches, since they currently appear most promising and since several cholinesterase inhibitors may soon be available for prescribing.
2(0,0,0,2) Details
1852719 Abdi YA, Villen T: Pharmacokinetics of metrifonate and its rearrangement product dichlorvos in whole blood. J Neurophysiol. 2001 Jan;85(1):319-22.


Cholinesterases were also determined in blood haemolyzed with water.
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6281697 Maxwell IC, Le Quesne PM, Ekue JM, Biles JE: Effect on neuromuscular transmission of repeated administration of an organophosphorus compound, metrifonate, during treatment of children with urinary schistosomiasis. Neurotoxicology. 1981 Dec;2(4):687-701.


Mean erythrocyte cholinesterase activity was 52-75% of pretreatment value in different groups when examined electrophysiologically.
1(0,0,0,1) Details
1813075 Nhachi CF, Murambiwa W, Kasilo OJ, Gwanzura L, Mason P: Effect of a single oral dose of metrifonate on human plasma cholinesterase levels. Bull Environ Contam Toxicol. 1991 Nov;47(5):641-5.

1(0,0,0,1) Details
17150236 Mehl A, Schanke TM, Torvik A, Fonnum F: The effect of trichlorfon and methylazoxymethanol on the development of guinea pig cerebellum. Toxicol Appl Pharmacol. 2007 Mar;219(2-3):128-35. Epub 2006 Nov 1.

There was a significant reduction in choline esterase, choline acetyltransferase and glutamate decarboxylase activities in the cerebellum.
1(0,0,0,1) Details
3434 Kutsenko SA: [Heightened anticholinesterase activity of chlorophos in its interaction with the TMB-4 reactivator in vitro]. Graefes Arch Clin Exp Ophthalmol. 1998 Dec;236(12):934-9.

3(0,0,0,3) Details
15474645 van der Staay FJ, Bouger PC: Effects of the cholinesterase inhibitors donepezil and metrifonate on scopolamine-induced impairments in the spatial cone field orientation task in rats. Behav Brain Res. 2005 Jan 6;156(1):1-10.

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1438050 Nordgren I, Karlen B, Kimland M: Metrifonate and tacrine: a comparative study on their effect on acetylcholine dynamics in mouse brain. Pharmacol Toxicol. 1992 Sep;71(3 Pt 1):236-40.


Tetrahydroaminoacridine (THA) and metrifonate are cholinesterase inhibitors used in the treatment of Alzheimer's disease.
2(0,0,0,2) Details
2597761 Predtechenskii MB, Elaeva NL, Smirnova ZI: [Modification of selective adsorption of muscarinic antagonists in cerebral membranes during chlorophos poisoning]. Farmakol Toksikol. 1976 Jan-Feb;39(1):35-9.


Cholinesterase reactivator dipyroxime was shown to induce normalization of the cyclosyl specific binding kinetics.
2(0,0,0,2) Details
473212 Reiner E, Plestina R: Regeneration of cholinesterase activities in humans and rats after inhibition by O,O-dimethyl-2,2-dichlorovinyl phosphate. Toxicol Appl Pharmacol. 1979 Jul;49(3):451-4.

1(0,0,0,1) Details
534330 Badiugin IS, Titova NN, Khamitova RIa, Makarov NIa: [Clinical aspects of domestic poisonings and the pathogenesis of intoxication from anticholinesterase organophosphorus compounds] Voen Med Zh. 1979 Nov;(11):37-40.

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4538536 Davis RP, Bailey DR: Effect of metrifonate on blood cholinesterases in children during the treatment of schistosomiasis. Bull World Health Organ. 1972;46(6):747-59.

1(0,0,0,1) Details
7281216 Ejezie GC, Ade-Serrano MA: Schistosoma haematobium in Ajara community of Badagry. Trop Geogr Med. 1981 Jun;33(2):181-4.


Metrifonate, an organophosphorus cholinesterase inhibitor, which has been shown to be effective in the treatment of urinary schistosomiasis was administered orally to 145 school children aged 6-15 years at a dose of 10 mg/kg body weight in 3 doses at 14-day intervals.
1(0,0,0,1) Details
9718229 Kaufer D: Beyond the cholinergic hypothesis: the effect of metrifonate and other cholinesterase inhibitors on neuropsychiatric symptoms in Alzheimer's disease. Dement Geriatr Cogn Disord. 1998;9 Suppl 2:8-14.

1(0,0,0,1) Details
11786345 Ivanov AN, Lukachova LV, Evtugyn GA, Karyakina EE, Kiseleva SG, Budnikov HC, Orlov AV, Karpacheva GP, Karyakin AA: Polyaniline-modified cholinesterase sensor for pesticide determination. Neuroreport. 1996 Apr 10;7(5):1097-101.

The detection limits found (coumaphos, 0.002, trichlorfon, 0.04, aldicarb, 0.03, methiocarb, 0.08 mg l (-1)) make it possible to detect the pollutants in the waters on the level of limited threshold levels without sample preconcentration.
2(0,0,0,2) Details
14521865 Disterhoft JF, Matthew Oh M: Modulation of cholinergic transmission enhances excitability of hippocampal pyramidal neurons and ameliorates learning impairments in aging animals. Neurobiol Learn Mem. 2003 Nov;80(3):223-33.


Four cholinesterase inhibitors have been approved by the US Food and Drug Administration for treating behavioral symptoms of Alzheimer's disease.
2(0,0,0,2) Details
11311445 Rakonczay Z, Papp H: Effects of chronic metrifonate treatment on cholinergic enzymes and the blood-brain barrier. Neurochem Int. 2001 Jul;39(1):19-24.


After an acute (4 h) treatment with an irreversible cholinesterase inhibitor organophosphate, metrifonate (100 mg/kg i.p.), the activities of both acetyl- and butyrylcholinesterase were inhibited (66.0-70.7% of the control level) in the rat brain cortex and hippocampus.
2(0,0,0,2) Details
9024334 Schneider LS: New therapeutic approaches to Alzheimer's disease. Biull Eksp Biol Med. 1989 Oct;108(10):459-61.


Cholinergic agents are currently the most promising treatment, and several cholinesterase inhibitors will soon be available for prescription.
2(0,0,0,2) Details
16625573 Lopez-Arrieta JM, Schneider L: Metrifonate for Alzheimer's disease. Cochrane Database Syst Rev. 2006 Apr 19;(2):CD003155.


BACKGROUND: Metrifonate is a long-acting irreversible cholinesterase inhibitor, originally used to treat schistosomiasis.
2(0,0,0,2) Details
9024678 Sheets LP, Hamilton BF, Sangha GK, Thyssen JH: Subchronic neurotoxicity screening studies with six organophosphate insecticides: an assessment of behavior and morphology relative to cholinesterase inhibition. Fundam Appl Toxicol. 1997 Jan;35(1):101-19.

Sulprofos, disulfoton, azinphos-methyl, methamidophos, trichlorfon, and tebupirimphos were screened for neurotoxic potential, in accordance with U.S.
2(0,0,0,2) Details
7344403 Bloom A: Studies of the mode of action of metrifonate and DDVP in schistosomes - cholinesterase activity and the hepatic shift. Acta Pharmacol Toxicol. 1981;49 Suppl 5:109-13.

1(0,0,0,1) Details
16822217 Dhingra D, Parle M, Kulkarni SK: Comparative brain cholinesterase-inhibiting activity of Glycyrrhiza glabra, Myristica fragrans, ascorbic acid, and metrifonate in mice. J Med Food. 2006 Summer;9(2):281-3.

1(0,0,0,1) Details
5140307 Karlog O, Rasmussen F, Skafte B: [The cholinesterase activity of red blood cells and plasma after cutaneous or oral application of metrifonatum NFN in pigs] Nord Vet Med. 1971 Mar;23(3):170-5.

1(0,0,0,1) Details
7250022 Dishovski K, Panova I, Uzunov P: [Effect of the organophosphorus compound neguvon on the dopamine content in the rat brain]. Eksp Med Morfol. 1981;20(2):62-6.


The reactivator of cholinesterase TMB-4 and H-choline blocker tropacine prevented this effect.
1(0,0,0,1) Details
11152731 Power JM, Oh MM, Disterhoft JF: Metrifonate decreases sI (AHP) in CA1 pyramidal neurons in vitro. Eur J Pharmacol. 1996 Dec 30;318(2-3):239-50.


Metrifonate, a cholinesterase inhibitor, has been shown to enhance learning in aging rabbits and rats, and to alleviate the cognitive deficits observed in Alzheimer's disease patients.
1(0,0,0,1) Details
2047580 Udom CE, Smith TJ: Hypolipidemic effect of metrifonate and the relationship to serum cholinesterase inhibition. Res Commun Chem Pathol Pharmacol. 1991 Mar;71(3):387-90.

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829002 Benes J, Proksova M, Hrusovsky J: [Treatment with antidotes in sheep perorally intoxicated] . Vet Med. 1976 Dec;21(12):737-46.


In a model of sheep perorally intoxicated with a 200.0 mg kg-1 trichlorphon dose, the effectivity of the worked out therapeutical procedure was confirmed; the procedure consisted in the administration of an anticholinergic (20.0 mg of 1.1% atropine s. c. pro toto) and cholinesterase reactivator (30.0 mg of 10% trimedoxime kg-1 i. m.) mixture 4 hours after the administration of the noxious agent.
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