Author/Authors :
Robert G. Gentles، نويسنده , , Shuanghua Hu، نويسنده , , Yazhong Huang، نويسنده , , Katherine Grant-Young، 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 exploratory SAR study on a series of potent, non-apamin-displacing 4-(aminomethylaryl)pyrazolopyrimidine KCa channel blockers is described and their selectivity against KCa channel subtypes is reported. The most potent analog, 5-chloro-N-(thiophen-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine (24) displayed sub-micromolar activity in both a thallium flux and whole-cell electrophysiology assay and did not displace apamin in a competitive binding study.
Keywords :
Small conductance potassium channel , Pyrrazolopyrimidine , Non-apamin displacing , Apamin
