[The anticonvulsive effect of 4,4-bis(hydroxymethyl)-2-phenyl-2-oxazoline].

Abstract

INTRODUCTION:

Certain compounds belonging to the family of the 2-aryl oxazolines have been reported to act on the central nervous system with a number of different effects and applications, which make them useful as depressants, anaesthetics, anticonvulsants, and so on.

AIMS:

Our aim was to study the possible effect of 4,4-bis(hydroxymethyl)-2-phenyl-2-oxazoline (OX), obtained by chemical synthesis using microwaves, in two experimental models of epilepsy.

MATERIALS AND METHODS:

Two models were used: one involving (repeated stimulation) electroconvulsive shock in mice and the other consisted in inducing audiogenic seizures in Mongolian gerbils. Recordings were performed of the potentials in the dentate gyrus (DG) generated in response to electrical stimulation of the entorhinal cortex in anaesthetised gerbils, using the stereotactic technique.

RESULTS:

A 150 mg/kg dose of OX lowered the number of electrical pulses required to induce the tonic seizures triggered by the electroshock, as well as their duration. This same dose blocked the seizures induced by audiogenic stimuli in the gerbils and significantly reduced their severity (degrees of seizures) and occurrence. OX diminished, in a dose-dependent manner, the amplitude of the excitatory post-synaptic potential and that of the population spike, triggered by stimulating the entorhinal cortex in the DG.

CONCLUSIONS:

OX acts as an antiepileptic agent and its mechanism of action could be related to the inhibiting effect it exerts on the entorhinal cortex-DG synapses in the hippocampus.

• Authors: M Díaz-Molina, M N Sánchez-Rodríguez, M Bu, H Pérez-Saad
• Journal: Revista de neurologia (Rev Neurol) 2005 Jun 1-15 Vol. 40 Issue 11 Pg. 652-5 ISSN: 0210-0010 [Print] Spain
• Vernacular Title: Efecto anticonvulsionante de la 2-fenil-4,4-bis (hidroximetil)-2-oxazolina.
• PMID: 15948066 (Publication Type: Comparative Study, English Abstract, Journal Article)

Chemical References

• 4,4-bis(hydroxymethyl)-2-phenyl-2-oxazoline
• Anticonvulsants
• Oxazoles
• Diazepam

Topics

• Animals
• Anticonvulsants (administration & dosage, chemical synthesis, pharmacology, therapeutic use)
• Dentate Gyrus (drug effects, physiopathology)
• Diazepam (therapeutic use)
• Dose-Response Relationship, Drug
• Drug Evaluation, Preclinical
• Electroshock
• Entorhinal Cortex (drug effects, physiopathology)
• Epilepsy, Reflex (drug therapy, genetics)
• Gerbillinae
• Mice
• Mice, Inbred Strains
• Oxazoles (administration & dosage, chemical synthesis, pharmacology, therapeutic use)
• Perforant Pathway (drug effects, physiology)
• Seizures (drug therapy, etiology, genetics)