Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Eliprodil

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Eliprodil
Clinical data
ATC code
  • None
Identifiers
  • 1-(4-Chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
CAS Number
PubChemCID
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.162.249Edit this at Wikidata
Chemical and physical data
FormulaC20H23ClFNO
Molar mass347.86 g·mol−1
3D model (JSmol)
  • C1CN(CCC1CC2=CC=C(C=C2)F)CC(C3=CC=C(C=C3)Cl)O
  • InChI=1S/C20H23ClFNO/c21-18-5-3-17(4-6-18)20(24)14-23-11-9-16(10-12-23)13-15-1-7-19(22)8-2-15/h1-8,16,20,24H,9-14H2 checkY
  • Key:GGUSQTSTQSHJAH-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

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]

References

[edit]
  1. ^The Pharma Letter. 2 December 1996Synthelabo's Eliprodil Fails In Stroke Trials
  2. ^De Keyser J, Sulter G, Luiten PG (December 1999)."Clinical trials with neuroprotective drugs in acute ischaemic stroke: are we doing the right thing?".Trends in Neurosciences.22 (12):535–40.doi:10.1016/s0166-2236(99)01463-0.PMID 10542428.S2CID 16302841.
  3. ^abLee JM, Zipfel GJ, Choi DW (June 1999). "The changing landscape of ischaemic brain injury mechanisms".Nature.399 (6738 Suppl): A7-14.doi:10.1038/399a007.PMID 10392575.S2CID 10086931.
  4. ^Ikonomidou C, Turski L (October 2002). "Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury?".The Lancet. Neurology.1 (6):383–6.doi:10.1016/s1474-4422(02)00164-3.PMID 12849400.S2CID 31477519.
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor
σ1
σ2
Unsorted
Stub icon

Thisdrug article relating to thenervous system is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Eliprodil&oldid=1244531182"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp