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Start Over Author "Zhang, Xu-Feng" Journal bioorganic & medicinal chemistry letters Publisher elsevier b.v.
1 results on '"Zhang, Xu-Feng"'

1. The discovery of a new class of large-conductance Ca2+-activated K+ channel opener targeted for overactive bladder: synthesis and structure–activity relationships of 2-amino-4-azaindoles

Author

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, and Sullivan, James P.

Subjects
*CALCIUM channels, *AMINES
Abstract

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 muscle tissue strips obtained from Landrace pig bladders. The preliminary SAR data indicate the importance of steric bulk around the 2-amino substituent. [Copyright &y& Elsevier]

Published
2003
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