title: Synthesis of benzopyrano[3,4-c]pyridin-5-ones as dopamine D4 receptor ligands.
abstract: The dopamine D4 receptor is highly expressed in prefrontal cortex, hippocampus, amygdala, hypothalamus and is hypothesized to relate with the pathophysiology and pharmacotherapy of schizophrenia while its level in brain regions is much lower. To date, no specific ligand is available for the study of D4 receptor in vivo. In this study, we report the synthesis and in vitro receptor binding assay of three benzopyrano[3,4-c]pyridin-5-ones as potential dopamine D4 receptor ligands. These new compounds have higher affinity and selectivity toward dopamine D4 receptor and their K(i) values for D4 receptor are in the nanomolar (nM) range.
authors.affiliation: College of Chemistry and Chemical Engineering, Hunan Institute of Engineering, China. ligucai@163.com
authors.forename: Li
authors.initials: L
authors.lastname: Gu-Cai
authors.forename: Wei
authors.initials: W
authors.lastname: Wen-Ting
authors.forename: Yuan
authors.initials: Y
authors.lastname: Li-Hua
authors.forename: Gao
authors.initials: G
authors.lastname: Tang-Jie
mesh_terms: D001578:Benzopyrans / Q000138:chemical synthesis* / Q000494:pharmacology*; D015259:Dopamine Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes / Q000737:chemistry; D007553:Isotope Labeling; D008024:Ligands; D011485:Protein Binding; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology*; D050638:Receptors, Dopamine D4 / Q000187:drug effects*
chemical_list: D001578:Benzopyrans; D015259:Dopamine Agents; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D008024:Ligands; D011728:Pyridones; D050638:Receptors, Dopamine D4