39230-30-3Relevant academic research and scientific papers
Synthesis and pharmacological characterization of two novel, brain penetrating P2X7 antagonists
Letavic, Michael A.,Lord, Brian,Bischoff, Francois,Hawryluk, Natalie A.,Pieters, Serge,Rech, Jason C.,Sales, Zachary,Velter, Adriana I.,Ao, Hong,Bonaventure, Pascal,Contreras, Victor,Jiang, Xiaohui,Morton, Kirsten L.,Scott, Brian,Wang, Qi,Wickenden, Alan D.,Carruthers, Nicholas I.,Bhattacharya, Anindya
supporting information, p. 419 - 422 (2013/06/26)
The synthesis and preclinical characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to
Discovery of a novel series of selective HCN1 blockers
McClure, Kelly J.,Maher, Michael,Wu, Nancy,Chaplan, Sandra R.,Eckert III, William A.,Lee, Dong H.,Wickenden, Alan D.,Hermann, Michelle,Allison, Brett,Hawryluk, Natalie,Breitenbucher, J. Guy,Grice, Cheryl A.
scheme or table, p. 5197 - 5201 (2011/10/02)
The discovery of a series of novel, potent, and selective blockers of the cyclic nucleotide-modulated channel HCN1 is disclosed. Here we report an SAR study around a series of selective blockers of the HCN1 channel. Utilization of a high-throughput VIPR assay led to the identification of a novel series of 2,2-disubstituted indane derivatives, which had moderate selectivity and potency at HCN1. Optimization of this hit led to the identification of the potent, 1,1-disubstituted cyclohexane HCN1 blocker, 2-ethoxy-N-((1-(4- isopropylpiperazin-1-yl)cyclohexyl)methyl)benzamide. The work leading to the discovery of this compound is described herein.
