A bis-(-)-nor-meptazinol derivative in which the two meptazinol rings are linked by a nonamethylene spacer is a novel acetylcholinesterase inhibitor that inhibits both catalytic activity and Abeta peptide aggregation. The crystal structure of its complex with Torpedo californica acetylcholinesterase was determined to 2.7 A resolution. The ligand spans the active-site gorge, with one nor-meptazi...

Amaryllidaceae are known as ornamental plants, furthermore some species of this family contain galanthamine, an acetylcholinesterase inhibitor approved for the treatment of Alzheimer ́s disease, and other alkaloids with interesting pharmacological activity. The chemical composition of alkaloids from Zephyranthes grandiflora Lindl. was analyzed by GC/MS. Seven known compounds, belonging to five s...

Amaryllidaceae are known as ornamental plants, furthermore some species of this family contain galanthamine, an acetylcholinesterase inhibitor approved for the treatment of Alzheimer ́s disease, and other alkaloids with interesting pharmacological activity. The chemical composition of alkaloids from Zephyranthes grandifl ora Lindl. was analyzed by GC/MS. Seven known compounds, belonging to fi ve...

Galanthamine, an acetylcholinesterase inhibitor marketed as a hydrobromide salt (Razadyne®, Reminyl®) for the treatment of Alzheimer's disease (AD), is obtained from Amaryllidaceae plants, especially those belonging to the genera Leucojum, Narcissus, Lycoris and Ungernia. The growing demand for galanthamine has prompted searches for new sources of this compound, as well as other bioactive alkal...

The reversible inhibition of acetylcholinesterase (AChE) by 4,4'-bipyridine (BP) was measured with acetylthiocholine as substrate. The enzyme/inhibitor dissociation constant for binding of BP to the catalytic site was Ka = 1.0 mM and the non-competitive dissociation constant for binding to an allosteric site was K, = = 9.0 mM. BP protected AChE against phosphylation by sarin, soman, tabun and V...