α2-antagonistic effect of N-carbamoyl-2-(2,6-dichlorophenyl) Acetamidine hydrochloride (cas 124-42-5) (LON-954)

Add time:09/08/2019    Source:sciencedirect.com

The effect of N-carbamoyl-2-(2,6-dichlorophenyl) Acetamidine hydrochloride (cas 124-42-5) (LON-954) on α2-adrenoceptors was studied in in vivo and in vitro preparations. Like yohimbine, LON-954 antagonised the clonidine-induced inhibition of twitch responses in the Auerbach's plexus of guinea pig ileum and rat vas deferens preparations. It also reversed the anti-convulsant effect of clonidine on pentylenetetrazol (PTZ)-induced convulsions in the rat, a property shared by yohimbine. However LON-954 failed to prevent the hypothermic response to clonidine in mice. The dissimilarity in action of LON-954 and yohimbine on clonidine-induced hypothermia could be due to the fact that the anticlonidine effect of yohimbine on hypothermia is mediated through its antiserotonin action. The results indicate that LON-954 acts as an α2-antagonist both centrally and peripherally.

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