2012
DOI: 10.1111/j.1447-0594.2011.00827.x
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3‐(2,4‐Dimethoxybenzylidene)‐anabaseine: A promising candidate drug for Alzheimer's disease?

Abstract: 3-(2,4-dimethoxybenzylidene)-anabaseine is an analog of the paralytic alkaloid, anabaseine, from the ribbon worms Amphiporus sp., that shows numerous properties, in particular an agonist activity on alpha 7 nicotinic acetylcholine receptors. This article reviews these properties and explains to what extent they could be valuable to control symptomatology and/or neurodegeneration in Alzheimer's disease.

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Cited by 21 publications
(8 citation statements)
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“…They are composed of different combinations of five subunits (α, β, γ, δ and ε) that form cysteine-loop ligand-gated cation channels permeable to Na + and K + and, to variable amounts of Ca 2+ . In the brain, the most abundant subunits are homomeric α7 subtype and the heteromeric α4β2 subtype, which are highly expressed in brain regions that develop AD neuropathology [ 68 , 69 , 70 ]. The binding of an agonist to a α7 nAChR leads to conformational changes and, consequently, the opening of the channel allowing the passage of ions.…”
Section: Marine Natural Productsmentioning
confidence: 99%
See 1 more Smart Citation
“…They are composed of different combinations of five subunits (α, β, γ, δ and ε) that form cysteine-loop ligand-gated cation channels permeable to Na + and K + and, to variable amounts of Ca 2+ . In the brain, the most abundant subunits are homomeric α7 subtype and the heteromeric α4β2 subtype, which are highly expressed in brain regions that develop AD neuropathology [ 68 , 69 , 70 ]. The binding of an agonist to a α7 nAChR leads to conformational changes and, consequently, the opening of the channel allowing the passage of ions.…”
Section: Marine Natural Productsmentioning
confidence: 99%
“…Following activation, the channel rearranges resulting in a loss of biological response [ 71 ]. The nAChR is a target for AD, because Aβ binds to these receptors, especially to the α7 subtype, and can alter the normal functionalization of the receptor leading to the initialization of Aβ [ 68 ].…”
Section: Marine Natural Productsmentioning
confidence: 99%
“…It was also shown to improve memory-related behaviour in Sprague–Dawley rats [50]. DMXBA in Alzheimer’s has been reviewed by Zawieja et al [51], and Kem et al reviewed studies on the use of anabaseine and DMXBA against memory loss and schizophrenia [46]. A comprehensive paper by Rangel and Falkenberg discussed the recent status of clinical trials with regard to compounds of marine origin and their derivatives in the pharmaceutical pipeline [52].…”
Section: Ribbon Worm Toxinsmentioning
confidence: 99%
“…76 Additionally, GTS-21 is a selective agonist of the a7 nicotinic receptor, showed promising characteristics during Phase II clinical trial. 77 Fig. 2 and Table S2 † show cholinergic inhibitors in clinical trials.…”
Section: Cholinergic Drugsmentioning
confidence: 99%