THE ANTICHOLINESTERASE ACTIVITY OF MEFLOQUINE
Abstract
SUMMARY: 1. The characteristics of the inhibition of electric eel acetylcholinesterase (AChE) and horse serum butyrylcholinesterase (BChE) by the antimalarial agents mefloquine, chloroquine, amodiaquine and amopyroquine were determined. 2. The antimalarials were found to be non‐competitive inhibitors of both AChE and BChE. In both enzyme systems, inhibitory potencies were in the order amodiaquine > amopyroquine > chloroquine > mefloquine. 3. The low inhibitory potency of mefloquine may account in part for the appearance of gastrointestinal and central nervous system disturbances only at high doses of the drug.
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Mefloquine has demonstrated AChE and butyrylcholinesterase (BChE) inhibitory activities attributable to its quinoline ring.
“To note, other studies about mefloquine potential in AD, have demonstrated its AChE and butyrylcholinesterase (BChE) inhibitory activities, attributable to its quinoline ring, a well-known ChE pharmacophoric function.72”
From From combinations to multitarget-directed ligands: A continuum in Alzheimer’s disease polypharmacology (2021) · cites this paper as [72]
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Juszczak, G. R., & Swiergiel, A. H. (2009) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2008.12.014 · Cited by 211 · see citing works
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- Authors
- Lim, L. Y., & Go, M. L.
- Affiliations
- National University of Singapore (SG)
- Corresponding author
- Go, M. L.
- ORCID
- Venue
- Clinical and Experimental Pharmacology and Physiology
- Publisher
- Wiley
- Published
- 1985-10
- Volume
- 12
- Issue
- 5
- Pages
- 527-531
- ISSN
- 0305-1870 (ISSN-L)
- 1440-1681
- OpenAlex
- W1992370441
- Cited by
- 33
- References
- 16
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 2 · 2022: 1 · 2021: 3 · 2020: 3 · 2019: 1 · 2018: 1 · 2015: 1 · 2013: 4
- FWCI
- 0.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Clinical and Experimental Pharmacology and Physiology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Pharmacology › Cholinesterase and Neurodegenerative Diseases
- Life Sciences › Agricultural and Biological Sciences › Plant Science › Pesticide Exposure and Toxicity
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Enzyme function and inhibition
- Keywords
- mefloquine, anticholinesterase activity, acetylcholinesterase, butyrylcholinesterase, non-competitive inhibition, chloroquine, amodiaquine, antimalarial drugs, gastrointestinal adverse effects, central nervous system adverse effects
- MeSH terms
- Amodiaquine, Animals, Antimalarials, Butyrylcholinesterase, Chloroquine, Cholinesterase Inhibitors, Cholinesterases, Horses, Kinetics, Quinolines, Structure-Activity Relationship, Mefloquine
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