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.
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This compound was developed by Sanofi Aventis. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
Dopamine (DA) receptor blockade induces catalepsy in rats which increases in strength upon retesting. This increase in catalepsy represents a form of sensitization which has been shown to be completely context dependent. Sensitization of catalepsy therefore represents a good model
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.
The British journal of ophthalmology, 83(2), 236-240 (1999-07-09)
This study characterised the pharmacology of [3H]-ifenprodil binding to the polyamine binding sites (PBS) on the N-methyl-D-aspartate (NMDA) receptor channel complex on human retinas. These data were correlated with the known neuroprotective effects of ifenprodil and eliprodil. Specific binding of
European journal of pharmacology, 362(2-3), 103-110 (1999-01-05)
Effects of noncompetitive and competitive NMDA receptor antagonists have been repeatedly characterized using place conditioning models. The present study aimed to characterize the effects in mice of another NMDA receptor antagonist acting at polyamine binding site, eliprodil. Five-day conditioning with
Naunyn-Schmiedeberg's archives of pharmacology, 366(2), 117-122 (2002-07-18)
The exact site(s) and the molecular mechanism(s) by which ethanol inhibits the activity of NMDA receptors in the brain have so far not been identified although the involvement of several NMDA receptor modulatory sites activated by glycine, Mg2+, Zn2+, polyamines
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