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Updated: Aug 24, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
1,5-Diarylsubstituted 1,2,3-triazoles as potassium channel activators. VI
Giuliana Biagi1, Vincenzo Calderone, Irene Giorgi
1Dipartimento di Scienze Farmaceutiche, via Bonanno 6, 56126 Pisa, Italy.
Abstract:
As part of our program toward designing potassium channel openers, synthesis of a novel series of 1,5-diphenylsubstituted 1,2,3-triazoles, as potential activators of the large-conductance calcium-activated potassium channels (BK), as well as their vasorelaxant activity are presented. The functional effect of these potential structurally novel BK-openers on vascular contractile function were studied in vitro, using isolated rat aortic rings pre-contracted with KCl 20 mM. Among the target compounds, only 16 showed appreciable effectiveness, exhibiting an efficacy parameter (57%) lower than that of NS1619 and a comparable potency index (pIC50: 5.58).
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