Back to Search
Start Over
Design, Synthesis and Biological Investigation of Flavone Derivatives as Potential Multi-Receptor Atypical Antipsychotics.
- Source :
- Molecules; Sep2020, Vol. 25 Issue 18, p4107, 1p
- Publication Year :
- 2020
-
Abstract
- The design of a series of novel flavone derivatives was synthesized as potential broad-spectrum antipsychotics by using multi-receptor affinity strategy between dopamine receptors and serotonin receptors. Among them, 7-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl) piperidin- 1-yl) butoxy)-2,2-dimethylchroman-4-one (6j) exhibited a promising preclinical profile. Compound 6j not only showed high affinity for dopamine D<subscript>2</subscript>, D<subscript>3</subscript>, and serotonin 5-HT<subscript>1A</subscript>, 5-HT<subscript>2A</subscript> receptors, but was also endowed with low to moderate activities on 5-HT<subscript>2C</subscript>, α<subscript>1</subscript>, and H<subscript>1</subscript> receptors, indicating a low liability to induce side effects such as weight gain, orthostatic hypotension and QT prolongation. In vivo behavioral studies suggested that 6j has favorable effects in alleviating the schizophrenia-like symptoms without causing catalepsy. Taken together, compound 6j has the potential to be further developed as a novel atypical antipsychotic. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 14203049
- Volume :
- 25
- Issue :
- 18
- Database :
- Complementary Index
- Journal :
- Molecules
- Publication Type :
- Academic Journal
- Accession number :
- 146144189
- Full Text :
- https://doi.org/10.3390/molecules25184107