Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the α3β4 nicotinic acetylcholine receptor (nAChR)

…, J Chewning, N Fedorov, K Tallapragada…

文献索引：Kombo, David C.; Hauser, Terry A.; Grinevich, Vladimir P.; Melvin, Matthew S.; Strachan, Jon-Paul; Sidach, Serguei S.; Chewning, Joseph; Fedorov, Nikolai; Tallapragada, Kartik; Breining, Scott R.; Miller, Craig H. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1450 - 1455

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被引用次数: 5

摘要

We have carried out a pharmacological evaluation of arylmethylene quinuclidine derivatives interactions with human α3β4 nAChRs subtype, using cell-based receptor binding, calcium- influx, electrophysiological patch-clamp assays and molecular modeling techniques. We have found that the compounds bind competitively to the α3β4 receptor with micromolar affinities and some of the compounds behave as non-competitive antagonists ( ...