2. Academic Validation
  3. NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles

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

  • J Med Chem. 2004 Apr 8;47(8):2089-96. doi: 10.1021/jm030483s.
John A McCauley 1,  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
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. john_mccauley@merck.com
PMID: 15056006 DOI: 10.1021/jm030483s
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.

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