1333413-75-4Relevant academic research and scientific papers
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (σ) receptor ligands
Banister, Samuel D.,Yoo, David T.,Chua, Sook Wern,Cui, Jinquan,MacH, Robert H.,Kassiou, Michael
, p. 5289 - 5292 (2011/10/03)
A series of racemic N-arylalkyl-2-azaadamantan-1-ols (9-15) and the corresponding deoxygenated, achiral N-arylalkyl-2-azaadamantanes (23-29) were synthesized and screened in competition binding assays against a panel of CNS targets. Adamantyl hemiaminals 9-15 displayed generally low affinity for both σ1 (Ki values = 294-1950 nM) and σ2 receptors (Ki values = 201-1020 nM), and negligible affinity for 42 other CNS proteins. Deoxygenation of 9-15 to give the corresponding achiral azaadamantanes 23-29 greatly improved affinity for σ1 (K i values = 8.3-239 nM) and σ2 receptors (K i values = 34-312 nM).
