2-(Arylmethyl)-3-substituted quinuclidines as selective α7 nicotinic receptor ligands

…, TY Phillips, A Seamans, JD Schmitt, TA Hauser…

文献索引：Mazurov, Anatoly; Klucik, Jozef; Miao, Lan; Phillips, Teresa Y.; Seamans, Angela; Schmitt, Jeffrey D.; Hauser, Terry A.; Johnson Jr., Raymond T.; Miller, Craig Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 8 p. 2073 - 2077

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被引用次数: 42

摘要

A series of 2-(arylmethyl)-3-substituted quinuclidines was developed as α7 neuronal nicotinic acetylcholine receptor (nAChR) agonists based on a putative pharmacophore model. The series is highly selective for the α7 over other nAChRs (eg, the α4β2 of the CNS, and the muscle and ganglionic subtypes) and is functionally tunable at α7. One member of the series,(+)-N-(1-azabicyclo [2.2. 2] oct-3-yl) benzo [b] furan-2-carboxamide (+)-8l), has ...