1450729-98-2Relevant academic research and scientific papers
Compound, composition, and method of activating GIRK potassium channel and use of same for treating conditions of interest
-
Page/Page column 31; 32; 34, (2015/07/07)
The present invention provides small molecule activators of GIRK potassium channels and methods for use thereof.
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators
Ramos-Hunter, Susan J.,Engers, Darren W.,Kaufmann, Kristian,Du, Yu,Lindsley, Craig W.,Weaver, C. David,Sulikowski, Gary A.
, p. 5195 - 5198 (2013/09/12)
This Letter describes a novel series of GIRK activators identified through an HTS campaign. The HTS lead was a potent and efficacious dual GIRK1/2 and GIRK1/4 activator. Further chemical optimization through both iterative parallel synthesis and fragment library efforts identified dual GIRK1/2 and GIRK1/4 activators as well as the first examples of selective GIRK1/4 activators. Importantly, these compounds were inactive on GIRK2 and other non-GIRK1 containing GIRK channels, and SAR proved shallow.
