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NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2004 Apr 08; Vol. 47 (8), pp. 2089-96. - Publication Year :
- 2004
-
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.
- Subjects :
- Analgesics pharmacokinetics
Analgesics pharmacology
Animals
Benzimidazoles pharmacokinetics
Benzimidazoles pharmacology
Brain metabolism
Calcium metabolism
Carrageenan
Cell Line
Dogs
Female
Humans
Hyperalgesia blood
Hyperalgesia chemically induced
Hyperalgesia drug therapy
In Vitro Techniques
Male
Patch-Clamp Techniques
Rats
Rats, Sprague-Dawley
Receptors, N-Methyl-D-Aspartate physiology
Structure-Activity Relationship
Analgesics chemical synthesis
Benzimidazoles chemical synthesis
Receptors, N-Methyl-D-Aspartate antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 47
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 15056006
- Full Text :
- https://doi.org/10.1021/jm030483s