Novel Benzo[b]thiophene Derivatives as New Potential Antidepressants with Rapid Onset of Action

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• 作者：Luis Berrade ; Ba虂rbara Aisa ; Mari虂a J. Ramirez ; Silvia Galiano ; Salvatore Guccione ; Lise Roma虂n Moltzau ; Finn Olav Levy ; Ferdinando Nicoletti ; Giuseppe Battaglia ; Gemma Molinaro ; Ignacio Aldana ; Antonio Monge ; Silvia Perez-Silanes
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：April 28, 2011
• 年：2011
• 卷：54
• 期：8
• 页码：3086-3090
• 全文大小：780K
• 年卷期：v.54,no.8(April 28, 2011)
• ISSN：1520-4804

文摘

We report benzo[b]thiophene derivatives synthesized according to a dual strategy. 8j, 9c, and 9e with affinity values toward 5-HT₇R and 5-HTT were selected to probe their antidepressant activity in vivo using the forced swimming text (FST). The results showed significant antidepressant activity after chronic treatment. 9c was effective in reducing the immobility time in FST even after acute treatment. These findings identify these compounds as a new class of antidepressants with a rapid onset of action.