In Vitro Effects of (+)MK-801 (dizocilpine) and Memantine on β-Amyloid Peptides Linked to Alzheimer's Disease.

ABSTRACT: An in vitro effect of (+)MK-801 (dizocilpine), an inhibitor of the glutamate/NMDA and nicotinic acetylcholine receptors, on the Aβ[1-42] and Aβ[1-40] peptides is described and compared to that of memantine. Memantine has been approved by the U.S. Food and Drug Administration for the treatment of mild-moderate Alzheimer's disease. Both compounds accelerated the formation of a β-sheet structure by Aβ[1-42], (+)MK-801 more rapidly than memantine, as observed in a thioflavin T fluorescence assay. The acceleration was followed by a decrease in the fluorescence signal that was not observed when the ligand was absent. Nuclear magnetic resonance spectra of the soluble peptides in the presence and absence of (+)MK-801 demonstrated that the monomeric form did not bind (+)MK-801 and that in th

SUBMITTER: Coombs SE 

PROVIDER: S-EPMC8126891 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature