Мы используем файлы cookie.
Продолжая использовать сайт, вы даете свое согласие на работу с этими файлами.
Abandoned drugs
Eliprodil
Другие языки:

    Eliprodil

    Подписчиков: 0, рейтинг: 0
    Eliprodil
    Eliprodil.svg
    Clinical data
    ATC code
    • None
    Identifiers
    • 1-(4-Chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    ChEBI
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.162.249
    Chemical and physical data
    Formula C20H23ClFNO
    Molar mass 347.86 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 (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.

    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. 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.


    Новое сообщение