Document Report Card

ID: ALA1149147

Journal: J Med Chem

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

Authors: McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.

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.

CiteXplore: 15056006

DOI: 10.1021/jm030483s