Literature DB >> 1686756

The non-N-methyl-D-aspartate receptor antagonists, GYKI 52466 and NBQX are anticonvulsant in two animal models of reflex epilepsy.

S E Smith1, N Dürmüller, B S Meldrum.   

Abstract

The effect of i.p. or i.v. administration of the non-N-methyl-D-aspartate antagonists, GYKI 52466 (1-(4-aminophenyl)-4-methyl-7,8-methylendioxy-5H-2,3-benzodiazepin e.HCl, molecular weight 330) and NBQX (2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo(F)-quinoxaline, molecular weight 342) on sound-induced seizures in rats and photically induced myoclonus in baboons was studied. In both species an anticonvulsant effect occurred 15-60 min after administration of GYKI 52466 or NBQX. The ED50 value for clonic seizure suppression for GYKI 52466 at 30 min was 39 (rats, i.p.) and at 15 min was 13 (Papio papio, i.v.) mumol kg-1 and for NBQX at 30 min was 40 (rats, i.p.) and at 15 min approximately 10 (Papio papio, i.v.) mumol kg-1. Side effects were not observed in rats; apparent side effects in baboons probably arose from drug formulation. The anticonvulsant actions of GYKI 52466 and NBQX suggest a possible role for non-NMDA antagonists in the therapy of epilepsy.

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Year:  1991        PMID: 1686756     DOI: 10.1016/0014-2999(91)90342-n

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN: 0014-2999            Impact factor:   4.432


  17 in total

1.  Behavioural and neurochemical interactions of the AMPA antagonist GYKI 52466 and the non-competitive NMDA antagonist dizocilpine in rats.

Authors:  M Bubser; T Tzschentke; W Hauber
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2.  Neuroprotection by glutamate receptor antagonists against seizure-induced excitotoxic cell death in the aging brain.

Authors:  P Elyse Schauwecker
Journal:  Exp Neurol       Date:  2010-03-29       Impact factor: 5.330

3.  AMPA antagonists differ from NMDA antagonists in their effects on operant DRL and delayed matching to position tasks.

Authors:  D N Stephens; B J Cole
Journal:  Psychopharmacology (Berl)       Date:  1996-08       Impact factor: 4.530

4.  Mechanism of Inhibition of the GluA2 AMPA Receptor Channel Opening: the Role of 4-Methyl versus 4-Carbonyl Group on the Diazepine Ring of 2,3-Benzodiazepine Derivatives.

Authors:  Mark Ritz; Congzhou Wang; Nicola Micale; Roberta Ettari; Li Niu
Journal:  ACS Chem Neurosci       Date:  2011-05-12       Impact factor: 4.418

5.  Interactions of 2,3-benzodiazepines and cyclothiazide at AMPA receptors: patch clamp recordings in cultured neurones and area CA1 in hippocampal slices.

Authors:  G Rammes; D Swandulla; G L Collingridge; S Hartmann; C G Parsons
Journal:  Br J Pharmacol       Date:  1996-03       Impact factor: 8.739

6.  Mechanism and site of inhibition of AMPA receptors: pairing a thiadiazole with a 2,3-benzodiazepine scaffold.

Authors:  Congzhou Wang; Yan Han; Andrew Wu; Sándor Sólyom; Li Niu
Journal:  ACS Chem Neurosci       Date:  2013-12-17       Impact factor: 4.418

7.  Investigation of the involvement of opioid receptors in the action of anticonvulsants.

Authors:  H C Jackson; D J Nutt
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

8.  Pharmacological Preconditioning with GYKI 52466: A Prophylactic Approach to Neuroprotection.

Authors:  Chelsea S Goulton; Anna R Patten; John R Kerr; D Steven Kerr
Journal:  Front Neurosci       Date:  2010-08-03       Impact factor: 4.677

Review 9.  AMPA receptors as a molecular target in epilepsy therapy.

Authors:  M A Rogawski
Journal:  Acta Neurol Scand Suppl       Date:  2013

10.  Treatment of early and late kainic acid-induced status epilepticus with the noncompetitive AMPA receptor antagonist GYKI 52466.

Authors:  Brita Fritsch; Jeffrey J Stott; Joy Joelle Donofrio; Michael A Rogawski
Journal:  Epilepsia       Date:  2009-07-20       Impact factor: 5.864

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