Synthesis, Antidepressant Evaluation and Docking Studies of Long-Chain Alkylnitroquipazines as Serotonin Transporter Inhibitors (pages 695–706)
Mari Gabrielsen, Karol Wołosewicz, Anna Zawadzka, Jerzy Kossakowski, Gabriel Nowak, Małgorzata Wolak, Katarzyna Stachowicz, Agata Siwek, Aina W. Ravna, Irina Kufareva, Lech Kozerski, Elżbieta Bednarek, Jerzy Sitkowski, Wojciech Bocian, Ruben Abagyan, Andrzej J. Bojarski, Ingebrigt Sylte and Zdzisław Chilmonczyk
Version of Record online: 11 APR 2013 | DOI: 10.1111/cbdd.12116
Twelve alkyl analogues 6-nitroquipazine (6-NQ) were synthesised and tested for their binding to the serotonin transporter protein (SERT) using in vitro radioligand competition binding assays and molecular docking. The putative antidepressant activity of the binders with the highest SERT binding affinities was also studied by the forced swim and locomotor activity mouse tests. The results showed that several of the 6-NQ analogues are high-affinity SERT inhibitors and that three of the analogues have moderate antidepressant activity.