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| ECHA InfoCard | 100.162.249 |
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| Formula | C20H23ClFNO |
| Molar mass | 347.86 g·mol−1 |
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Eliprodil (codenamedSL-82.0715) is anNMDA antagonist drug candidate which selectively inhibits the NR2B (GLUN2B) subtype NMDA receptor at submicromolar concentrations. Eliprodil failed a Phase III clinical trial for the treatment of acuteischemic stroke in 1996, sponsored by Synthélabo Recherche.[1][2][3]
NMDA receptors are a key component in mediating glutamate-inducedexcitotoxicity, and it is believed thatNMDA antagonists would beneuroprotective after a stroke or othertraumatic brain injury.[4] After a traumatic brain injury, neurons become deprived of glucose and oxygen. These neurons quickly lose ATP and become depolarized, which releases glutamate. The extracellular buildup of glutamate triggers the overstimulation ofAMPA and NMDA receptors. This, in turn, causes an influx of Na+ and Ca2+. Therefore, when NMDA receptors are activated, there is an increase in intracellular Ca2+ concentration. High Ca2+ causes fatal metabolic consequences, including neuronal cell death.[3]
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