Alpha 2-antagonistic effect of N-carbamoyl-2-(2,6-dichlorophenyl) acetamidine hydrochloride (LON-954).
The effect of N-carbamoyl-2-(2,6-dichlorophenyl) acetamidine hydrochloride (LON-954) on alpha 2-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 alpha 2-antagonist both centrally and peripherally.
D000317:Adrenergic alpha-Antagonists; D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D003000:Clonidine / Q000494:pharmacology; D018492:Dopamine Antagonists; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D051379:Mice; D009130:Muscle, Smooth / Q000187:drug effects*; D009197:Myenteric Plexus / Q000187:drug effects; D010433:Pentylenetetrazole / Q000494:pharmacology; D051381:Rats; D012640:Seizures / Q000139:chemically induced; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology; D014649:Vas Deferens / Q000187:drug effects; D015016:Yohimbine / Q000494:pharmacology
D000317:Adrenergic alpha-Antagonists; D018492:Dopamine Antagonists; D015016:Yohimbine; C014908:LON 954; D014508:Urea; D003000:Clonidine; D010433:Pentylenetetrazole