RESUMO
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...(AU)
Assuntos
Anticonvulsivantes/uso terapêutico , Epilepsia Reflexa/tratamento farmacológico , OxazóisRESUMO
Introducción. Algunos compuestos de la familia de las 2- aril-oxazolinas se han descrito como sustancias activas sobre el sistema nervioso central, con efectos y aplicaciones diversas, comodepresores, anestésicos, anticonvulsionantes, etc. Objetivo. Estudiar el posible efecto de la 2-fenil-4,4-bis (hidroximetil)-2-oxazolina (OX)obtenida por síntesis química bajo microondas en dos modelos deepilepsia experimental. Materiales y métodos. Se emplearon el modelode choque electroconvulsivo por estimulación repetitivaen ratones y el de crisis audiogénica en el gerbo mongol. Se incluyó el registro de los potenciales del giro dentado (GD) en respuesta a la estimulación eléctrica de la corteza entorrinal en el gerbo anestesiado mediante la técnica estereotáctica. Resultados. La dosis de 150 mg/kg de OX redujo el número de pulsos eléctricos necesarios parainducir la crisis tónica producida por el choque eléctrico, así comosu duración. Esta misma dosis bloqueó las crisis inducidas por el estímulo audiogénico en el gerbo y disminuyó significativamente su gravedad (grados de crisis) y aparición. La OX redujo, en forma dependiente de la dosis, la amplitud del potencial postsináptico excitatorio y de la espiga de población, provocada por la estimulación dela corteza entorrinal en el GD. Conclusiones. La OX posee un efectoantiepiléptico cuyo mecanismo podría estar relacionado con su acción inhibitoria sobre la sinapsis corteza entorrinal-GD en el hipocampo(AU)
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 consistedin 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 stereotactictechnique. 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-dependentmanner, 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(AU)
Assuntos
Animais , Camundongos , Anticonvulsivantes/administração & dosagem , Anticonvulsivantes/farmacologia , Anticonvulsivantes/uso terapêutico , Epilepsia Reflexa/tratamento farmacológico , Epilepsia Reflexa/genética , Oxazóis/administração & dosagem , Oxazóis/farmacologia , Oxazóis/uso terapêuticoRESUMO
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.