Investigation of the pharmacological activity of two acetylenic triazoline derivatives

• Published in: Progress in neuro-psychopharmacology & biological psychiatry 1995, Vol.19 (2), p.263-272
• Main Authors: Al-Tememi, Ghazi F., Arif, Inaam S., Al-Ghrary, Nidhal F., Muhi-Eldeen, Zuhair
• Format: Article
• Language: English
• Subjects: acetylenic compounds; Biological and medical sciences; Cholinergic system; Medical sciences; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; oxotremorine analogues; Pharmacology. Drug treatments; triazoline
• ISSN: 0278-5846; 1878-4216
• DOI: 10.1016/0278-5846(94)00007-5

1. 1. 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. 2. 2. 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. 3. 3. These compounds did not affect the oxotremorine-induced tremor, salivation and diarrhea in mice. 4. 4. In addition, the compounds failed to antagonize the carbacholinduced lacrimal secretion or the pilocarpine-induced salivation in male Wistar rats. 5. 5. 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.