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Eliprodil

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Title: Eliprodil  
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Eliprodil

Eliprodil
Systematic (IUPAC) name
1-(4-chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
Clinical data
Legal status
?
Identifiers
CAS number  N
ATC code None
PubChem
ChemSpider  YesY
UNII  YesY
ChEMBL  YesY
Synonyms Eliprodil
Chemical data
Formula C20H23ClFNO 
Mol. mass 347.854 g/mol
 N   

Eliprodil (SL-82.0715) is a drug which acts as an NMDA antagonist, binding to the polyamine modulatory site.[1] It has neuroprotective and anticonvulsant effects in animal studies,[2] but does not support self-administration or substitute for phencyclidine,[3] and does not produce sedation or amnesia.[4] It was researched for the treatment of stroke[5] and epilepsy[6] but human trials failed to show clear beneficial effects.[7]

References

  1. ^ Dereń-Wesołek, A; Maj, J (1993). "Central effects of SL 82.0715, an antagonist of polyamine site of the NMDA receptor complex". Polish journal of pharmacology 45 (5–6): 467–80.  
  2. ^ Toulmond, S; Serrano, A; Benavides, J; Scatton, B (1993). "Prevention by eliprodil (SL 82.0715) of traumatic brain damage in the rat. Existence of a large (18 h) therapeutic window". Brain Research 620 (1): 32–41.  
  3. ^ Balster, RL; Nicholson, KL; Sanger, DJ (1994). "Evaluation of the reinforcing effects of eliprodil in rhesus monkeys and its discriminative stimulus effects in rats". Drug and alcohol dependence 35 (3): 211–6.  
  4. ^ Patat, A; Molinier, P; Hergueta, T; Brohier, S; Zieleniuk, I; Danjou, P; Warot, D; Puech, A (1994). "Lack of amnestic, psychotomimetic or impairing effect on psychomotor performance of eliprodil, a new NMDA antagonist". International clinical psychopharmacology 9 (3): 155–62.  
  5. ^ Reyes, M; Reyes, A; Opitz, T; Kapin, MA; Stanton, PK (1998). "Eliprodil, a non-competitive, NR2B-selective NMDA antagonist, protects pyramidal neurons in hippocampal slices from hypoxic/ischemic damage". Brain Research 782 (1–2): 212–8.  
  6. ^ Kohl, BK; Dannhardt, G (2001). "The NMDA receptor complex: a promising target for novel antiepileptic strategies". Current medicinal chemistry 8 (11): 1275–89.  
  7. ^ Ikonomidou, C; Turski, L (2002). "Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury?". Lancet neurology 1 (6): 383–6.  


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