himbacine has been researched along with Alzheimer-Disease* in 2 studies
2 other study(ies) available for himbacine and Alzheimer-Disease
| Article | Year |
|---|---|
Synthesis and muscarinic M(2) subtype antagonistic activity of enantiomeric pairs of 3-demethylhimbacine (3-norhimbacine) and its C(4)-epimer.
In the course of our studies of the structure-activity relationships of himbacine 1, a potent antagonist of the M(2) subtype of muscarinic receptor, the four title compounds, 2, ent-2, 3, and ent-3, were synthesized with a highly stereoselective intermolecular Diels-Alder reaction of tetrahydroisobenzofuran 4 with achiral furan-2(5H)-one 5 as a key step, followed by simultaneous optical resolution and epimer separation of the racemic intermediates. Among these compounds, 3-demethylhimbacine (3-norhimbacine) 2, bearing an absolute configuration corresponding to that of 1, was found to show more potent muscarinic M(2) subtype receptor binding activity than natural 1. Topics: Alkaloids; Alzheimer Disease; Animals; Brain Stem; Cerebral Cortex; Furans; Muscarinic Antagonists; Naphthalenes; Parasympatholytics; Piperidines; Radioligand Assay; Rats; Receptor, Muscarinic M2; Receptors, Muscarinic; Stereoisomerism; Structure-Activity Relationship | 2002 |
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
In our search for M2-selective muscarinic receptor antagonists, we synthesized 1,3-disubstituted indenes. The effects of different basic moieties with regard to binding and selectivity towards the five distinct muscarinic receptor subtypes were investigated. The results show that the quinuclidine series afforded the most promising compounds in terms of both receptor affinity and M2-subtype selectivity. Topics: Alzheimer Disease; Humans; In Vitro Techniques; Ligands; Quinuclidines; Radiopharmaceuticals; Receptor, Muscarinic M2; Receptors, Muscarinic; Tomography, Emission-Computed | 2001 |