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Synthesis and In Vitro Evaluation of Novel Dopamine Receptor D2 3,4-dihydroquinolin-2(1H)-one Derivatives Related to Aripiprazole
R. Juza, K. Stefkova, W. Dehaen, A. Randakova, T. Petrasek, I. Vojtechova, T. Kobrlova, L. Pulkrabkova, L. Muckova, M. Mecava, L. Prchal, E. Mezeiova, K. Musilek, O. Soukup, J. Korabecny
Language English Country Switzerland
Document type Journal Article, Research Support, Non-U.S. Gov't
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PubMed
34572475
DOI
10.3390/biom11091262
Knihovny.cz E-resources
- MeSH
- Aripiprazole chemical synthesis pharmacology MeSH
- Cell Death MeSH
- Central Nervous System drug effects MeSH
- Quinolones chemical synthesis chemistry pharmacology MeSH
- CHO Cells MeSH
- Cricetulus MeSH
- Blood-Brain Barrier drug effects pathology MeSH
- Ligands MeSH
- Models, Molecular MeSH
- Drug Design MeSH
- Receptors, Dopamine D2 chemistry metabolism MeSH
- Binding Sites MeSH
- Animals MeSH
- Check Tag
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
In this pilot study, a series of new 3,4-dihydroquinolin-2(1H)-one derivatives as potential dopamine receptor D2 (D2R) modulators were synthesized and evaluated in vitro. The preliminary structure-activity relationship disclosed that compound 5e exhibited the highest D2R affinity among the newly synthesized compounds. In addition, 5e showed a very low cytotoxic profile and a high probability to cross the blood-brain barrier, which is important considering the observed affinity. However, molecular modelling simulation revealed completely different binding mode of 5e compared to USC-D301, which might be the culprit of the reduced affinity of 5e toward D2R in comparison with USC-D301.
Institute of Physiology Czech Academy of Sciences Videnska 1083 142 20 Prague Czech Republic
National Institute of Mental Health Topolova 748 250 67 Klecany Czech Republic
References provided by Crossref.org
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