Eliprodil

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Eliprodil
Systematic (IUPAC) name
1-(4-chlorophenyl)-2-[4-[(4-fluorophenyl)methyl]piperidin-1-yl]ethanol
Identifiers
CAS number 119431-25-3
ATC code  ?
PubChem 60703
Chemical data
Formula C20H23ClFNO 
Mol. mass 347.854 g/mol
SMILES eMolecules & PubChem
Synonyms Eliprodil
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.

?

Legal status
Routes  ?

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 stroke5 and epilepsy6 but human trials failed to show clear beneficial effects.7


References

  1. ^ Dereń-Wesołek A, Maj J. Central effects of SL 82.0715, an antagonist of polyamine site of the NMDA receptor complex. Polish Journal of Pharmacology. 1993 Sep-Dec;45(5-6):467-80. PMID 7912135
  2. ^ Toulmond S, Serrano A, Benavides J, Scatton B. Prevention by eliprodil (SL 82.0715) of traumatic brain damage in the rat. Existence of a large (18 h) therapeutic window. Brain Research. 1993 Aug 20;620(1):32-41. PMID 8402196
  3. ^ Balster RL, Nicholson KL, Sanger DJ. Evaluation of the reinforcing effects of eliprodil in rhesus monkeys and its discriminative stimulus effects in rats. Drug and Alcohol Dependence. 1994 Jun;35(3):211-6. PMID 7956750
  4. ^ Patat A, Molinier P, Hergueta T, Brohier S, Zieleniuk I, Danjou P, Warot D, Puech A. Lack of amnestic, psychotomimetic or impairing effect on psychomotor performance of eliprodil, a new NMDA antagonist. International Clinical Psychopharmacology. 1994 Sep;9(3):155-62. PMID 7814824
  5. ^ Reyes M, Reyes A, Opitz T, Kapin MA, Stanton PK. Eliprodil, a non-competitive, NR2B-selective NMDA antagonist, protects pyramidal neurons in hippocampal slices from hypoxic/ischemic damage. Brain Research. 1998 Jan 26;782(1-2):212-8. PMID 9519265
  6. ^ Kohl BK, Dannhardt G. The NMDA receptor complex: a promising target for novel antiepileptic strategies. Current Medicinal Chemistry. 2001 Sep;8(11):1275-89. PMID 11562266
  7. ^ Ikonomidou C, Turski L. Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? Lancet Neurology. 2002 Oct;1(6):383-6. PMID 12849400


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  • This page was last modified on 20 July 2008, at 07:50.

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