The discovery of a new class of large-conductance Ca 2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure–activity relationships of …

…, TK White, M Gopalakrishnan, MJ Coghlan…

文献索引：Turner, Sean C.; Carroll, William A.; White, Tammie K.; Gopalakrishnan, Murali; Coghlan, Michael J.; Shieh, Char-Chang; Zhang, Xu-Feng; Parihar, Ashutosh S.; Buckner, Steven A.; Milicic, Ivan; Sullivan, James P. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 12 p. 2003 - 2007

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被引用次数: 30

摘要

2-Amino-4-azaindoles have been identified as a structurally novel class of BKCa channel openers. Their synthesis from 2-chloro-3-nitropyridine is described together with their in vitro properties assessed by 86Rb+ efflux and whole-cell patch-clamp assays using HEK293 cells stably transfected with the BKCa α subunit. In vitro functional characterization of BKCa channel opening activity was also assessed by measurement of relaxation of smooth ...