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Pharmacol Res ; 26(2): 131-41, 1992 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-1409254

RESUMEN

The neuropsychopharmacological profile of a new centrally acting skeletal muscle relaxant, 2,4-dihydro[1,2,4]triazolo[3,4-c][1,4]benzothiazine-1-one (IDPH-791), an analogue of triazolobenzothiazine, has been described and compared to mephenesin, a well known centrally-acting muscle relaxant. IDPH-791 was found to be safer and of longer duration of action than mephenesin in all the tests conducted in this study. Both IDPH-791 and mephenesin caused ataxia, decrease in spontaneous activity and inhibition of pinnal reflex. IDPH-791 was 1.5 to 2.0 times more potent in exhibiting motor inco-ordination and anticonvulsant activity than mephenesin in mice and rats. IDPH-791 was twice as active in inhibiting various spinal polysynaptic reflexes, crossed extensor, flexor, and linguomandibular reflexes; however, both did not affect the typical monosynaptic reflex, patellar reflex. IDPH-791 and mephenesin did not have sedative activity. Although mephenesin exhibited haemolytic activity, IDPH-791 was devoid of this activity. It is concluded that IDPH-791 is a safe and effective centrally-acting muscle relaxant having a longer duration of action than mephenesin. IDPH-791 is also devoid of sedative and haemolytic activity.


Asunto(s)
Encéfalo/efectos de los fármacos , Actividad Motora/efectos de los fármacos , Relajantes Musculares Centrales/farmacología , Relajación Muscular/efectos de los fármacos , Tiazinas/farmacología , Triazoles/farmacología , Administración Oral , Animales , Hipnosis , Inyecciones Intraperitoneales , Dosificación Letal Mediana , Mefenesina/administración & dosificación , Mefenesina/farmacología , Mefenesina/toxicidad , Ratones , Relajantes Musculares Centrales/administración & dosificación , Relajantes Musculares Centrales/toxicidad , Parálisis/inducido químicamente , Conejos , Ratas , Ratas Wistar , Convulsiones/prevención & control
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