NR2B selective NMDA glutamate receptor antagonist which appears to target the "polyamine site" on the NMDA receptor, setting it apart from other NR2B receptor antagonists. Possesses neuroprotective effects in models of ischemia, but prolongs the QT interval in patients; currently under investigation for acute and chronic pain.
The discovery that glutamate's activity at the N-methyl-D-aspartate (NMDA) receptor is positively modulated by glycine and polyamines has led to a new pharmacological strategy that NMDA receptor-mediated events could be antagonized indirectly at the strychnine-insensitive glycine co-agonist site (glycine(B) receptor)
Pharmacology, biochemistry, and behavior, 65(4), 611-620 (2000-04-15)
Current perspectives on the clinical use of NMDA receptor antagonists infer repeated administration schedules for the management of different pathological states. The development of tolerance and cross-tolerance between different NMDA receptor antagonists may be an important factor contributing to the
Pharmaceutical development and technology, 11(1), 87-91 (2006-03-21)
Measurement of drug release of a sparingly soluble drug by conventional methods proceeds very slowly without the aid of surfactants. Two preliminary automated methods were developed that increase sensitivity and accelerate such studies by working at very small reservoir volumes.
Statistics in medicine, 17(24), 2835-2847 (1999-01-28)
Between 1993 and 1996, a total of 452 patients were entered into a randomized trial evaluating eliprodil (a non-competitive NMDA receptor antagonist) in patients suffering from severe head injury. The primary efficacy analysis concerned the Glasgow Outcome Score (GOS), six
The N-methyl-D-aspartate (NMDA) subtype of glutamate receptor is one pathway through which excessive influx of calcium has been suggested to trigger ischemia-induced delayed neuronal death. NMDA receptors are heterooligomeric complexes comprised of both NR1 and NR2A-D subunits, in various combinations.
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