Investigation of the pharmacological activity of two acetylenic triazoline derivatives

Al Tememi, Ghazi F.; Arif, Inaam S.; Al Ghrary, Nidhal F.; Muhi Eldeen, Zuhair

Progress In Neuro-Psychopharmacology and Biological Psychiatry. : 263-272


DOI: 10.1016/0278-5846(94)00007-5
Accession: 008913460

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The pharmacological activity of two acetylenic triazolines: 4,5-diaryl-1-(4-(2,6-dimethylpiperdino-2-butynyl)-1,2,4-triazoline-5-one (comp.I) and 4,5-diaryl-1-(4-(piperidino-2-butynyl)-1,2,4-triazoline-5-one (comp.II) was evaluated as oxotremorine analogues in mice and rats. The test compounds stimulated the central nervous system at high doses (80 mg/Kg or higher) manifested as: increased locomotor activity, antagonism of pentobarbitone-induced sleeping and potentiation of strychnine toxicity and lethality in mice. These compounds did not affect the oxotremorine-induced tremor,salivation and diarrhea in mice. In addition, the compounds failed to antagonize the carbachol- induced lacrimal secretion or the pilocarpine-induced salivation in male Wistar rats. These results indicate that acetylenic triazoline failed to block the centrally-mediated effects of the parent compound oxotremorine or to modify the glandular hypersecretion of cholinergic drugs in rodents.