Physostigmine, tacrine and metrifonate: the effect of multiple doses on acetylcholine metabolism in rat brain - PubMed (original) (raw)
Physostigmine, tacrine and metrifonate: the effect of multiple doses on acetylcholine metabolism in rat brain
M Hallak et al. Neuropharmacology. 1989 Mar.
Abstract
The effects of two consecutive intramuscular doses of three cholinesterase inhibitors (physostigmine, tetrahydroaminoacridine and metrifonate) were compared in rats. The results revealed major differences in biochemical effects on the brain of the rat including the extent and duration of inhibition of cholinesterase, inhibition of release of acetylcholine and increase in levels of acetylcholine. Side effects were also markedly different in the time of appearance, duration and severity. These results suggest that there are significant differences in the mechanisms of action of various cholinesterase inhibitors. Since all three cholinesterase inhibitors are currently used in the experimental treatment of Alzheimer's disease, these findings have potential implications for the symptomatic therapy of these patients.
Similar articles
- Metrifonate and tacrine: a comparative study on their effect on acetylcholine dynamics in mouse brain.
Nordgren I, Karlén B, Kimland M. Nordgren I, et al. Pharmacol Toxicol. 1992 Sep;71(3 Pt 1):236-40. doi: 10.1111/j.1600-0773.1992.tb00553.x. Pharmacol Toxicol. 1992. PMID: 1438050 - Effect of subchronic treatment with metrifonate and tacrine on brain cholinergic function in aged F344 rats.
Giovannini MG, Scali C, Bartolini L, Schmidt B, Pepeu G. Giovannini MG, et al. Eur J Pharmacol. 1998 Jul 31;354(1):17-24. doi: 10.1016/s0014-2999(98)00429-4. Eur J Pharmacol. 1998. PMID: 9726626 - Metrifonate induces cholinesterase inhibition exclusively via slow release of dichlorvos.
Hinz VC, Grewig S, Schmidt BH. Hinz VC, et al. Neurochem Res. 1996 Mar;21(3):331-7. doi: 10.1007/BF02531649. Neurochem Res. 1996. PMID: 9139239 - Mechanism of action of cholinesterase inhibitors in Alzheimer's disease.
Håkansson L. Håkansson L. Acta Neurol Scand Suppl. 1993;149:7-9. doi: 10.1111/j.1600-0404.1993.tb04245.x. Acta Neurol Scand Suppl. 1993. PMID: 7907455 Review. - Multiple actions of THA on cholinergic neurotransmission in Alzheimer brains.
Nordberg A, Nilsson-Håkansson L, Adem A, Lai Z, Winblad B. Nordberg A, et al. Prog Clin Biol Res. 1989;317:1169-78. Prog Clin Biol Res. 1989. PMID: 2557636 Review.
Cited by
- Reversal effect of DM-9384 on scopolamine-induced acetylcholine depletion in certain regions of the mouse brain.
Abe E. Abe E. Psychopharmacology (Berl). 1991;105(3):310-6. doi: 10.1007/BF02244423. Psychopharmacology (Berl). 1991. PMID: 1798828 - Differential binding of bispyridinium oxime drugs with acetylcholinesterase.
Kesharwani MK, Ganguly B, Das A, Bandyopadhyay T. Kesharwani MK, et al. Acta Pharmacol Sin. 2010 Mar;31(3):313-28. doi: 10.1038/aps.2009.193. Epub 2010 Feb 8. Acta Pharmacol Sin. 2010. PMID: 20140002 Free PMC article. - Why do so many drugs for Alzheimer's disease fail in development? Time for new methods and new practices?
Becker RE, Greig NH, Giacobini E. Becker RE, et al. J Alzheimers Dis. 2008 Oct;15(2):303-25. doi: 10.3233/jad-2008-15213. J Alzheimers Dis. 2008. PMID: 18953116 Free PMC article. Review. - Energetics of Ortho-7 (oxime drug) translocation through the active-site gorge of tabun conjugated acetylcholinesterase.
Sinha V, Ganguly B, Bandyopadhyay T. Sinha V, et al. PLoS One. 2012;7(7):e40188. doi: 10.1371/journal.pone.0040188. Epub 2012 Jul 11. PLoS One. 2012. PMID: 22808117 Free PMC article.