Literature DB >> 6667068

Anticonvulsant activity of milacemide.

W van Dorsser, D Barris, A Cordi, J Roba.   

Abstract

The anticonvulsant activity of a new drug, milacemide (2-(pentylamino)-acetamide), has been studied in animal models of convulsions like those induced by bicuculline, pentylenetetrazol, picrotoxin, strychnine, inhibitors of GABA synthesis as 3-mercaptopropionic acid, allylglycine, isoniazid and thiosemicarbazide and electroshock. Milacemide is particularly effective in inhibiting the convulsions induced by bicuculline. The ED50 is 5.7 mg/kg by oral route and the activity lasts for more than 48 hr. It is less active against pentylenetetrazol and only marginally active against electroshock. It has not be found active against the other types of convulsions. Milacemide has a low toxicity (LD50: 2585 mg/kg in the mouse) and alters the behaviour of mouse, rat and monkey, only at high doses (greater than or equal to 1000 mg/kg). Milacemide seems to be specially free of sedative potential.

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Year:  1983        PMID: 6667068

Source DB:  PubMed          Journal:  Arch Int Pharmacodyn Ther        ISSN: 0003-9780


  8 in total

1.  Effect of milacemide on extracellular and tissue concentrations of dopamine and 5-hydroxytryptamine in rat frontal cortex.

Authors:  J Semba; M Doheny; P N Patsalos; G Sarna; G Curzon
Journal:  Br J Pharmacol       Date:  1992-01       Impact factor: 8.739

Review 2.  Anticonvulsant drug action and regional neurotransmitter amino acid changes.

Authors:  A G Chapman; G P Hart
Journal:  J Neural Transm       Date:  1988       Impact factor: 3.575

Review 3.  A review of the in vitro and in vivo neurochemical characterization of the NMDA/PCP/glycine/ion channel receptor macrocomplex.

Authors:  P L Wood; T S Rao; S Iyengar; T Lanthorn; J Monahan; A Cordi; E Sun; M Vazquez; N Gray; P Contreras
Journal:  Neurochem Res       Date:  1990-02       Impact factor: 3.996

4.  Microionophoretic study with milacemide, a glycine precursor, on mammalian central nervous system cells.

Authors:  J M Godfraind
Journal:  Br J Pharmacol       Date:  1990-05       Impact factor: 8.739

Review 5.  Safinamide.

Authors:  Ruggero G Fariello
Journal:  Neurotherapeutics       Date:  2007-01       Impact factor: 7.620

6.  Antiepileptic drug pharmacokinetics and neuropharmacokinetics in individual rats by repetitive withdrawal of blood and cerebrospinal fluid: milacemide.

Authors:  J Semba; G Curzon; P N Patsalos
Journal:  Br J Pharmacol       Date:  1993-04       Impact factor: 8.739

7.  A microdialysis study of glycinamide, glycine and other amino acid neurotransmitters in rat frontal cortex and hippocampus after the administration of milacemide, a glycine pro-drug.

Authors:  M H Doheny; S Nagaki; P N Patsalos
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1996-07       Impact factor: 3.000

8.  Fasting for 24 h reveals liver microsteatosis after continuous i.v. infusion of milacemide in the rat.

Authors:  J L Rakotoamboa; M Masson; B Palate; J Carleer; J Roba
Journal:  Arch Toxicol       Date:  1994       Impact factor: 5.153

  8 in total

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