Synthesis and Studies on Anticonvulsant and Antidepressant Activities of 5-Alkoxy-tetrazolo[1,5-a]quinolines

• Published in: Bulletin of the Korean Chemical Society Vol. 31; no. 2; pp. 447 - 452
• Main Authors: Deng, Xian-Qing, Wei, Cheng-Xi, Song, Ming-Xia, Chai, Kyu-Yun, Sun, Zhi-Gang, Quan, Zhe-Shan
• Format: Journal Article
• Language: Korean
• Published: 2010
• Subjects: Antidepressant; Forced swimming test; Synthesis; Tetrazolo[1,5-a]quinoline; Anticonvulsant
• ISSN: 0253-2964; 1229-5949

A series of 5-alkoxy-tetrazolo[1,5-a]quinolines were synthesized to evaluate their anticonvulsant and antidepressant effects. Anticonvulsant effects and neurotoxicity of the compounds when injected intraperitoneally to mice were determined by a maximal electroshock (MES) test and a rotarod test, respectively. Only three of the synthesized compounds (4a, 4b, 4c) displayed anticonvulsant activity at a dose of 300 mg/kg. Most of the compounds significantly reduced immobility times during the forced swimming test (FST) at a dose of 100 mg/kg, indicative of antidepressant activity. Among the compounds, 5-(2-fluorobenzyloxy)tetrazolo[1,5-a]quinoline (4k) reduced immobility time by 66.85% at 30 mg/kg compared with the same dose of Fluoxetine, which reduced immobility time by 52.30%. According to the results of the 5-Hydroxytryptophan induced head-twitch test and yohimbine toxicity potentiation test, the noradrenergic system seems not to be involved in the antidepressant-like effect of compound 4k while the serotonergic system seems a little to be involved.