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). Z9 30

1,5-Diarylsubstituted 1,2,3-triazoles as potential potassium channels activators. VI.

CALDERONE, VINCENZO;GIORGI, IRENE;MARTELLI, ALMA;
2004-01-01

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). Z9 30
Biagi, G; Calderone, Vincenzo; Giorgi, Irene; Livi, O; Martinotti, E; Martelli, Alma; Nardi, A.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/181638
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