Eliprodil

drugbox
IUPAC_name = 1-(4-chlorophenyl)-2- [4- [(4-fluorophenyl)methyl] piperidin-1-yl] ethanol

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CAS_number = 119431-25-3
synonyms = Eliprodil
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PubChem = 60703
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C = 20 | H = 23 | Cl = 1 | F = 1 | N = 1 | O = 1
molecular_weight = 347.854 g/mol
smiles = C1CN(CCC1CC2=CC=C(C=C2)F)CC(C3=CC=C(C=C3)Cl)O
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Eliprodil (SL-82.0715) is a drug which acts as an NMDA antagonist, binding to the polyamine modulatory site. [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] It has neuroprotective and anticonvulsant effects in animal studies, [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] but does not support self administration or substitute for phencyclidine, [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] and does not produce sedation or amnesia. [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] It was researched for the treatment of stroke [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] and epilepsy [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] but human trials failed to show clear beneficial effects. [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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