1091598-83-2Relevant academic research and scientific papers
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine KCa channel blockers
Gentles, Robert G.,Hu, Shuanghua,Huang, Yazhong,Grant-Young, Katherine,Poss, Michael A.,Andres, Charles,Fiedler, Tracey,Knox, Ronald,Lodge, Nicholas,Weaver, C. David,Harden, David G.
scheme or table, p. 5694 - 5697 (2009/08/07)
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.
