Receptor interaction profile and CNS general pharmacology of metrifonate and its transformation product dichlorvos in rodents

Drug Development Research

Volumn 38, Issue 1, 1996, Pages 31-42

  Hinz, Volker C ^a   Blokland, Arjan ^a   Van Der Staay, Franz Josef ^a   Gebert, Irmingard ^a   Schuurman, Teunis ^b   Schmidt, Bernard H ^a  

^a MEDA Manufacturing GmbH   (Germany)

^b WAGENINGEN UNIVERSITY   (Netherlands)

Author keywords

Cholinergic symptoms; Dichlorvos; General CNS pharmacology; Metrifonate

Indexed keywords

DICHLORVOS; METRIFONATE; MUSCARINIC RECEPTOR; NICOTINIC RECEPTOR;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BEHAVIOR; CELL MEMBRANE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; CONVULSION; DIARRHEA; DRUG RECEPTOR BINDING; IN VITRO STUDY; INDUCED HYPOTHERMIA; MALE; MOUSE; NONHUMAN; ORAL DRUG ADMINISTRATION; RAT; REARING; SALIVATION; TREMOR;

EID: 0029778404     PISSN: 02724391     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1098-2299(199605)38:1<31::AID-DDR4>3.0.CO;2-M     Document Type: Article

References (54)

1. Adem A, Jossan SS, Oreland L (1989): Tetrahydroaminoacridine inhibits human and rat brain monoamino oxidase. Neurosci Lett 107:313-317.
2. Averbook BJ, Anderson RJ (1983): Electrophysiological changes associated with chronic administration of organophosphates. Arch Toxicol 52:167-172.
3. Bakry NM, el Rashidy AH, Eldefrawi AT, Eldefrawi ME (1988): Direct actions of organophosphate anticholinesterases on nicotinic and muscarinic acetylcholine receptors. J Biochem Toxicol 3:235-259.
4. Becker RE, Giacobini E (1988): Mechanisms of cholinesterase inhibition in senile dementia of the Alzheimer type: Clinical, pharmacological, and therapeutic aspects. Drug Dev Res 12: 163-195.
5. Becker RE, Colliver J, Elble R, Feldman E, Giacobini E, Kumar V, Markwell S, Moriearty P, Parks R, Shillcutt SD, Unni L, Vicari S, Womack C, Zec RF (1990): Effects of metrifonate, a long-acting cholinesterase inhibitor, in Alzheimer disease: Report of an open trial. Drug Dev Res 19:425-434.
6. Bierer LM, Haroutunian V, Gabriel S, Knott PJ, Carlin LS, Purohit DP, Perl DP, Schmeidler J, Kanof P, Davis KL (1995): Neurochemical correlates of dementia severity in Alzheimer's disease: Relative importance of the cholinergic deficits. J Neurochem 64:749-760.
7. Bigge CF, Drummond JT, Johnson G, Malone T, Probert AWJ, Marcoux FW, Coughenour LL, Brahce LJ (1989): Exploration of phenyl-spaced 2-amino-(5,9)-phosphonoalkanoic acids as comparative N-methyl-D-aspartic acid antagonists. J Med Chem 32: 1580-1590.
8. Blair D, Hoadley EC, Hutson DH (1975): The distribution of dichlorvos in the tissues of mammals after its inhalation or intravenous administration. Toxicol Appl Pharmacol 31:243-253.
9. Blokland A, Hinz V, Schmidt BH (1995): Effects of metrifonate and tacrine in the spatial Morris task and modified Irwin test: Evaluation of the efficacy/safety profile in rats. Drug Dev Res 36: 166-179.
10. Capacio BR, Harris LW, Anderson DR, Lennox WJ, Gales V, Dawson JS (1992): Use of the accelerating rotorod for assessment of motor performance decrement induced by potential anticonvulsive compounds in nerve agent poisoning. Drug Chem Toxicol 15:177-201.
11. Chan PC, Peters AC (1989): Thirteen week subchronic dosed feed study of trichlorfon in Fischer rats and B6C3F1 mice. Proc Am Assoc Cancer Res 30:137-144.
12. Cohen SD, Williams RA, Killinger JM, Freudenthal RI (1985): Comparative sensitivity of bovine and rodent acetylcholinesterase to in-vitro inhibition by organophosphate insecticides. Toxicol Appl Pharmacol 81:452-459.
13. Collerton D (1986): Cholinergic function and intellectual decline in Alzheimer's disease. Neuroscience 19:1-28.
14. Cozanitis DA, Friedmann T, Furst S (1983): Study of the analgesic effects of galanthamine, a cholinesterase inhibitor. Arch Int Pharmacodyn Ther 266:229-238.
15. Davis A (1991): Metrifonate. In Dollery C (ed): Therapeutic Drugs. Edinburgh: Churchill Livingstone, Vol. 2, pp 164-170.
16. Dawson RM, Poretski M (1991): The interaction of tacrine with benzodiazepine and GABA binding sites of guinea pig brain. Neurosci Lett 129:251-253.
17. el Etri MM, Nickell WT, Ennis M, Skau KA, Shipley MT (1992): Brain norepinephrine reductions in soman-intoxicated rats: Association with convulsions and AChE inhibition, time course, and relations to other monoamines. Exp Neurol 118:153-163.
18. Ferguson PW, Medon PJ, Nasri E (1985): Temephos (Abate™) metabolism and toxicity in rats. Arch Environ Contam Toxicol 14:143-147.
19. Friboulet A, Rieger F, Goudou D, Amitai G, Taylor P (1990): Interaction of an organophosphate with a peripheral site on acetylcholinesterase. Biochemistry 29:914-920.
20. Giacobini E (1991): The second generation of cholinesterase inhibitors: Pharmacological aspects. In Becker R, Giacobini E (eds): Cholinergic Basis for Alzheimer Therapy. Boston, Birkhäuser, pp 247-262.
21. Gordon CJ, Fogelson L (1993): Relationship between serum cholinesterase activity and the change in body temperature and motor activity in the rat: A dose-response study of diisopropyl fluorophosphate. Neurotoxicol Teratol 15:21-25.
22. Gottfries GC (1990): Neurochemical aspects of dementia disorders. Dementia 1:56-64.
23. Haggerty GC, Kurtz PJ, Armstrong RD (1986): Duration and intensity of behavioral change after sublethal exposure to soman in rats. Neurobehav Toxicol Teratol 8:695-702.
24. Hallak M, Giacobini E (1989): Physostigmine, tacrine and metrifonate: The effect of multiple doses on acetylcholine metabolism in rat brain. Neuropharmacology 28:199-206.
25. Herink J, Koupilova M, Hrdina V (1989): Effects of tetrahydroaminoacridine (tacrine) derivatives and physostigmine in convulsion induced by pentylenetetrazole. Act Nerv Super Praha 31:303-305.
26. Hinz VC, Grewig S, Schmidt BH (1996): Metrifonate and dichlorvos: Effects of a single oral administration on cholinesterase activity in rat brain and blood. Neurochemical Res 21:339-345.
27. Holmstedt B, Nordgren I, Sandoz M, Sundwall A (1978): Metrifonate: Summary of toxicological and pharmacological information available. Arch Toxicol 41:3-29.
28. Johnson MK (1981): Delayed neurotoxicity: Do trichlorphon and/or dichlorvos cause delayed neuropathy in man or in test animals? Acta Pharmacol Toxicol 49:87-98.
29. Johnson PS, Michaelis EK (1992): Characterisation of organophosphate interactions at N-methyl-D-aspartate receptors in brain synpatic membranes. Mol Pharmacol 41:750-756.
30. Kamienski FX, Murphy SD (1975): Biphasic effects of methylene-dioxyphenyl synergists on the action of hexobarbital and organophosphate insecticides in mice. Toxicol Appl Pharmacol 18: 883-894.
31. Kronforst-Collins MA, Moriearty PL, Ralph M, Becker RE, Schmidt B, Thompson LT, Disterhoft JF (1996): Metrifonate treatment enhances acquisition of eyeblink conditioning in aging rabbits. Pharmacol Biochem Behav (in press).
32. Lotti, M. (1992): The pathogenesis of organophosphate polyneuropathy. Crit Rev Toxicol 21:465-487.
33. Makela PM, Truman CA, Ford JM, Roberts CJ (1994): Characteristics of plasma protein binding of tacrine hydrochloride: A new drug for Alzheimer's disease. Eur J Clin Pharmacol 47:151-155.
34. Millan MJ (1991): Antagonists at the NMDA recognition site and blockers of the associated ion channel induce spontaneous tail-flicks in the rat. Eur J Pharmacol 203:315-318.
35. Mori F, Cuadra G, Giacobini E (1995): Metrifonate effects on acetylcholine and biogenic amines in rat cortex. Neurochem Res 20:1081-1088.
36. Nabeshima T, Nitta A, Katono Y, Itoh A, Hasegawa T (1995): Effects of metrifonate on impairment of learning and memory induced by scopolamine and basal forebrain lesions in rats. 55th World Congress of Pharmacology and Pharmaceutical Science, Stockholm, August 1995.
37. Natori K, Okazaki Y, Irie T, Katsube J (1990): Pharmacological and biochemical assessment of SM-10888, a novel cholinesterase inhibitor. Jpn J Pharmacol 53:145-155.
38. Naumann K (1989): Acetylcholinesterase inhibitors. BCPC Mono 43:21-41.
39. Nordgren I, Bergstrom M, Holmstedt B, Sandoz M (1978): Transformation and action of metrifonate. Arch Toxicol 41:31-41.
40. Ornstein PL, Schaus JM, Chambers JW, Huser DL, Leander JD, Wong DT, Paschal JW, Jones ND, Deeter JB (1989): Synthesis and pharmacology of a series of 3- and 4-(phosphonoalkyl)pyridine- and -piperidine-2-carboxylic acids. Potent N-methyl-D-aspartate receptor antagonists. J Med Chem 32:827-833.
41. Palmer AM, Steel JE, Lowe SL, Bowen DM (1990): Influence of tetrahydro-9-amino-acridine on excitatory amino acid release. Clin Neuropharmacol 13:58-66.
42. Rajendra W, Oloffs PC, Banister EW (1986): Effects of chronic intake of diazinon on blood and brain monoamines and amino acids. Drug Chem Toxicol 9:117-131.
43. Rao KS, Aracava Y, Rickett DL, Albuquerque EX (1987): Non-competitive blockade of the nicotinic acetylcholine receptor-ion channel complex by an irreversible cholinesterase inhibitor. J Pharmacol Exp Ther 240:337-344.
44. Rausch JL, Janowsky DS, Risch SC, Huey LY (1985): Physostigmine effects on serotonin uptake in human blood platelets. Eur J Pharmacol 109:91-96.
45. Reiner E, Krauthacker B, Simeon V, Škrinjaric-Špoliar M (1975): Mechanism of inhibition in-vitro of mammalian acetylcolinesterase and cholinesterase in solutions of O,O-dimethyl 2,2,2-trichloro-1-hydroxyethyl phosphonate (Trichlorphon). Biochem Pharmacol 24:717-722.
46. Romano JAJ, Landauer MR (1986): Effects of the organophosphorus compound, O-ethyl-N-dimethyl-phosphoramidocyanidate (tabun), on flavor aversion, locomotor activity, and rotarod performance in rats. Fundam Appl Toxicol 6:62-68.
47. Rupniak NM, Tye SJ, Brazell C, Heald A, Iversen SD, Pagella PG (1992): Reversal of cognitive impairment by heptyl physostigmine, a long-lasting cholinesterase inhibitor, in primates. J Neurol Sci 107:246-249.
48. Silveira CL, Eldefrawi AT, Eldefrawi ME (1990): Putative M2 muscarinic receptors of rat heart have high affinity for organophosphorus anticholinesterases. Toxicol Appl Pharmacol 103: 474-481.
49. Soininen HS, Unni L, Shillcutt S (1990): Effect of acute and chronic cholinesterase inhibition on biogenic amines in rat brain. Neurochem Res 15:1185-1190.
50. Somani SM, Unni LK, McFadden DL (1987): Drug interaction for plasma protein binding: Physostigmine and other drugs. Int J Clin Ther Toxico. 25:412-416.
51. van der Staay FJ, Hinz VC, Schmidt BH (1996): Effects of metrifonate on escape and avoidance learning in young and aged rats. Behav Pharmacol 7:56-64.
52. Vazquez ML, Garland DJ, Sun ET, Cler JA, Mick SJ, Hood WF, Monahan JB, Iyengar S, Rao TS (1992): Characterization of 3-carboxy-5-phosphono-1,2,3,4-tetrahydroisoquinoline (SC-48981), a potent competitive n-methyl-d-aspartate (NMDA) receptor antagonist, in-vitro and in-vivo. Neurosci Lett 135:149-152.
53. Wanibushi F, Nishida T, Hidaka K, Koshiya K, Tsukamoto S, Usuda S (1994): Characterization of a novel muscarinic receptor agonist, YM796: Comparison with cholinesterase inhibitors in in-vivo pharmacological studies. Eur J Pharmacol 265:151-158.
54. Ward TR, Ferris DJ, Tilson HA, Mundy WR (1993): Correlation of the anticholinesterase activity of a series of organophosphates with their ability to compete with agonist binding to muscarinic receptors. Toxicol Appl Pharmacol 122:300-307.