Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor …

…, JF Daanen, KB Ryther, JT Wasicak, JF Kincaid…

文献索引：Holladay, Mark W.; Bai, Hao; Li, Yihong; Lin, Nan-Horng; Daanen, Jerome F.; Ryther, Keith B.; Wasicak, James T.; Kincaid, John F.; He, Yun; Hettinger, Anne-Marie; Huang, Peggy; Anderson, David J.; Bannon, Anthony W.; Buckley, Michael J.; Campbell, Jeffrey E.; Donnelly-Roberts, Diana L.; Gunther, Karen L.; Kim, David J. B.; Kuntzweiler, Theresa A.; Sullivan, James P.; Decker, Michael W.; Arneric, Stephen P. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 19 p. 2797 - 2802

全文：HTML全文

被引用次数: 58

摘要

Analogs of A-98593 (1) and its enantiomer ABT-594 (2) with diverse substituents on the pyridine ring were prepared and tested for affinity to nicotinic acetylcholine receptor binding sites in rat brain and for analgesic activity in the mouse hot plate assay. Numerous types of modifications were consistent with high affinity for [3H] cytisine binding sites. By contrast, only selected modifications resulted in retention of analgesic potency in the same range ...