Journal
BIOORGANIC CHEMISTRY
Volume 97, Issue -, Pages -Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2020.103662
Keywords
Long-chain arylpiperazines; Depression; 5-HT1A receptor ligands; Schizophrenia; Multi-target ligands
Funding
- Polish National Science Centre [2013/09/B/NZ7/00748]
- Medical University of Warsaw [FW26/PM1/17/17]
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A series of novel 4-butyl-arylpiperazine-3-(1H-indol-3-yl)pyrrolidine-2,5-dione derivatives were synthesized and evaluated for their 5-HT1A/D-2 receptor affinity and serotonin reuptake inhibition. The compounds exhibited high affinity for the 5-HT1A receptor, (especially 4d K-i = 0.4 nM) which depended on the substitution pattern at the phenylpiperazine moiety. From this series screen, compound 4c emerged with promising mixed receptor profiles for the 5-HT1A/D-2 receptors and the serotonin transporter (K-i = 1.3 nM, 182 nM and 64 nM, respectively).
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