Referenced in: none

Automatically associated channels: Kv11.1

Title: Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.

Authors: Charles J McIntyre, John A McCauley, Bohumil Bednar, Rodney A Bednar, John W Butcher, David A Claremon, Michael E Cunningham, Roger M Freidinger, Stanley L Gaul, Carl F Homnick, Ken S Koblan, Scott D Mosser, Joseph J Romano, Nigel J Liverton

Journal, date & volume: Bioorg. Med. Chem. Lett., 2009 Sep 1 , 19, 5132-5

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/19648007

Abstract
A novel series of annulated tricyclic compounds was synthesized and evaluated as NMDA/NR2B antagonists. Structure-activity development was directed towards in vitro optimization of NR2B activity and selectivity over the hERG K(+) channel. Preferred compounds were subsequently evaluated for selectivity in an alpha(1)-adrenergic receptor binding counter-screen and a cell-based assay of NR2B activity.