Author/Authors :
Robert G. Gentles، نويسنده , , Katherine Grant-Young، نويسنده , , Shuanghua Hu، نويسنده , , Yazhong Huang، نويسنده , , Michael A. Poss، نويسنده , , Charles Andres، نويسنده , , Tracey Fiedler، نويسنده , , Ronald Knox، نويسنده , , Nicholas Lodge، نويسنده , , C. David Weaver، نويسنده , , David G. Harden، نويسنده ,
Abstract :
An initial SAR study on a series of apamin-displacing 2-aminothiazole KCa2 channel blockers is described. Potent inhibitors such as N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (13) are disclosed, and for select members of the series, the relationship between the observed activity in a thallium flux, a binding and a whole-cell electrophysiology assay is presented.
Keywords :
2-Aminothiazole , Small conductance potassium channel , Potassium channel blockers , Apamin
