Referenced in: none

Automatically associated channels: Kv11.1

Title: NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.

Authors: John A McCauley, Cory R Theberge, Joseph J Romano, Susan B Billings, Kenneth D Anderson, David A Claremon, Roger M Freidinger, Rodney A Bednar, Scott D Mosser, Stanley L Gaul, Thomas M Connolly, Cindra L Condra, Menghang Xia, Michael E Cunningham, Bohumil Bednar, Gary L Stump, Joseph J Lynch, Alison Macaulay, Keith A Wafford, Kenneth S Koblan, Nigel J Liverton

Journal, date & volume: J. Med. Chem., 2004 Apr 8 , 47, 2089-96

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/15056006

Abstract
Two classes of 5-substituted benzimidazoles were identified as potent antagonists of the NR2B subtype of the N-methyl-d-aspartate (NMDA) receptor. Selected compounds show very good selectivity versus the NR2A, NR2C, and NR2D subtypes of the NMDA receptor as well as versus hERG-channel activity and alpha(1)-adrenergic binding. Benzimidazole 37a shows excellent activity in the carrageenan-induced mechanical hyperalgesia assay in rats as well as good pharmacokinetic behavior in dogs.