Chemistry:Eliprodil
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| Formula | C20H23ClFNO |
| Molar mass | 347.86 g·mol−1 |
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Eliprodil (codenamed SL-82.0715) is an NMDA 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 acute ischemic stroke in 1996, sponsored by Synthélabo Recherche.[1][2][3]
NMDA receptors are a key component in mediating glutamate-induced excitotoxicity, and it is believed that NMDA antagonists would be neuroprotective after a stroke or other traumatic 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 of AMPA 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]
References
- ↑ The Pharma Letter. 2 December 1996 Synthelabo's Eliprodil Fails In Stroke Trials
- ↑ "Clinical trials with neuroprotective drugs in acute ischaemic stroke: are we doing the right thing?". Trends in Neurosciences 22 (12): 535–40. December 1999. doi:10.1016/s0166-2236(99)01463-0. PMID 10542428. https://www.rug.nl/research/portal/en/publications/clinical-trials-with-neuroprotective-drugs-in-acute-ischaemic-stroke(7deb2c8f-aa7e-4685-8dc2-2d41a70da739).html.
- ↑ 3.0 3.1 "The changing landscape of ischaemic brain injury mechanisms". Nature 399 (6738 Suppl): A7-14. June 1999. doi:10.1038/399a007. PMID 10392575.
- ↑ "Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury?". The Lancet. Neurology 1 (6): 383–6. October 2002. doi:10.1016/s1474-4422(02)00164-3. PMID 12849400.
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