Synthesis and evaluation of xanomeline analogs—Probing the wash-resistant phenomenon at the M 1 muscarinic acetylcholine receptor

…, MKO Grant, EE El-Fakahany, DM Ferguson

文献索引：Kane, Brian E.; Grant, Marianne K.O.; El-Fakahany, Esam E.; Ferguson, David M. Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 3 p. 1376 - 1392

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被引用次数: 29

摘要

A series of xanomeline analogs were synthesized and evaluated for binding at the M1 muscarinic acetylcholine receptor (M1 receptor). Specifically, compounds that substitute the O-hexyl chain of xanomeline with polar, ionizable, or conformationally restricted moieties were assessed for their ability to bind to the M1 receptor in a wash-resistant manner (persistent binding). From our screen, several novel ligands that persistently bind to the ...