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Tizanidine (DS103-282), a centrally acting muscle relaxant, selectively depresses excitation of feline dorsal horn neurones to noxious peripheral stimuli by an action at alpha 2-adrenoceptors.
Neurosci Lett ; 48(2): 197-202, 1984 Jul 27.
Article en En | MEDLINE | ID: mdl-6090998
The effects of microiontophoretic ejection of tizanidine were compared with those of adrenoceptor agonists on responses of single laminae IV and V neurones to noxious and innocuous cutaneous stimuli. Tizanidine, noradrenaline and clonidine depressed neuronal responses to noxious but not innocuous stimuli. Spontaneous activity was also depressed by these three substances. By contrast, beta- and alpha 1-adrenoceptor agonists had no consistent effect on neuronal responses to cutaneous stimuli. The selective actions of tizanidine, noradrenaline and clonidine were reversibly antagonized by the alpha 2-adrenoceptor antagonist RX781094 but not by WB4101 (alpha 1 antagonist). The binding of an alpha 2-adrenoceptor ligand to rat brain membranes was preferentially displaced by tizanidine. These results indicate an interaction of tizanidine with central alpha 2-adrenoceptors.
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dolor / Médula Espinal / Receptores Adrenérgicos alfa / Clonidina / Relajantes Musculares Centrales Límite: Animals Idioma: En Revista: Neurosci Lett Año: 1984 Tipo del documento: Article Pais de publicación: Irlanda
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Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dolor / Médula Espinal / Receptores Adrenérgicos alfa / Clonidina / Relajantes Musculares Centrales Límite: Animals Idioma: En Revista: Neurosci Lett Año: 1984 Tipo del documento: Article Pais de publicación: Irlanda