RESUMEN
A series of new phenylsuccinimide derivatives substituted in the aromatic ring and/or at the nitrogen atom was synthesized and tested for activity against pentetrazole- and electroshock-induced convulsions.
Asunto(s)
Anticonvulsivantes/síntesis química , Succinatos/síntesis química , Animales , Fenómenos Químicos , Química , Electrochoque , Femenino , Ratones , Ratones Endogámicos BALB C , Pentilenotetrazol/antagonistas & inhibidores , Succinatos/farmacología , Succinatos/toxicidadAsunto(s)
Anticonvulsivantes/farmacología , Fenitoína/análogos & derivados , Animales , Anticonvulsivantes/toxicidad , Interacciones Farmacológicas , Electrochoque , Femenino , Hexobarbital/farmacología , Dosificación Letal Mediana , Ratones , Actividad Motora/efectos de los fármacos , Fenitoína/farmacología , Fenitoína/toxicidad , Sueño/efectos de los fármacosRESUMEN
Anticonvulsant properties of two new derivatives, of phenylsuccinimide, N-morpholinomethyl-3-bromophenyl-succinimide(IL-7) and N-amino-3-bromophenylsuccinimide (IL-16), were studied. It was stated that both compounds have similar acute toxicity and act longer than phensuximide. They are especially active in maximal electroshock seizure (MES) test. Their effectiveness against convulsions produced by pentetrazole is less than that of phensuximide. Their effectiveness against procaine and strychnine is similar, only one of tested compounds has very high potency against strychnine. This compound, IL-16, has also a different pattern of effect-time which is probably due to its different pharmacokinetic behaviour.
Asunto(s)
Anticonvulsivantes , Succinimidas/farmacología , Animales , Electrochoque , Femenino , Dosificación Letal Mediana , Ratones , Pentilenotetrazol/antagonistas & inhibidores , Procaína/antagonistas & inhibidores , Estricnina/antagonistas & inhibidores , Succinimidas/toxicidad , Factores de TiempoRESUMEN
The authors report a 49-year-old man in whom continuous left-sided headaches increasing recently in intensity suggested presence of brain tumour. Sudden clinical deterioration on the 7th day of hospital observation was supposed to be due to brain-stem herniation. On autopsy a thrombus was found filling the basilar artery and the proximal parts of the posterior cerebral arteries with foci of softening in the right hemisphere, brain stem and left cerebellar hemisphere. The authors suppose that headaches were of vascular origin.