New dual ligands for the D2 and 5-HT1A receptors from the group of 1,8-naphthyl derivatives of LCAP |
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| Authors: | Przemysław Zaręba Jolanta Jaśkowska Paweł Śliwa Grzegorz Satała |
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| Affiliation: | 1. Faculty of Chemical Engineering and Technology, Institute of Organic Chemistry and Technology, Cracow University of Technology, 24 Warszawska Street, Cracow 31-155, Poland;2. Department of Medicinal Chemistry, Institute of Pharmacology – Polish Academy of Sciences, 12 Sm?tna Street, Cracow 31-343, Poland |
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| Abstract: | More than 300 million people are suffering from depression, one of the civilization diseases in the 21st century. Serotonin 5-HT1AR and dopamine D2R play an important role in the treatment and pathogenesis of depression. Moreover, in recent years, the efficacy of dual 5-HT1A/D2 receptors ligands has been demonstrated in the fight against depression. In this work the new bulky arylpiperazine derivatives (LCAP) were synthesized in microwave radiation field. The affinities for the selected serotonin (5-HT1A,5-HT2A,5-HT6,5-HT7) and dopamine (D2) receptors have been evaluated in vitro. Compounds 5.3a, 5.4, 5.1c, 5.3d, 5.2a are promising dual 5-HT1AR/D2R ligands. The SAR analysis were additionally supported with molecular docking studies. |
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| Keywords: | Corresponding author. Serotonin receptors Depression Molecular modelling Microwave-assisted |
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