{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Ostrowska K"],"funding":["Medical University of Warsaw, Faculty of Pharmacy"],"pagination":["2779"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC9917830"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["24(3)"],"pubmed_abstract":["A series of 15 new derivatives of 6-acetyl-7-hydroxy-4-methylcoumarin containing a piperazine group were designed with the help of computational methods and were synthesized to study their affinity for the serotonin 5-HT<sub>1A</sub> and 5-HT<sub>2A</sub> receptors. Among them, 6-acetyl-7-{4-[4-(3-bromophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (<b>4</b>) and 6-acetyl-7-{4-[4-(2-chlorophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (<b>7</b>) exhibited excellent activity for 5-HT<sub>1A</sub> receptors with Ki values 0.78 (0.4-1.4) nM and 0.57 (0.2-1.3) nM, respectively, comparable to the Ki values of 8-OH-DPAT (0.25 (0.097-0.66) nM). The equilibrium dissociation constant values of the tested compounds showed differential intrinsic activities of the agonist and antagonist modes."],"journal":["International journal of molecular sciences"],"pubmed_title":["New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT<sub>1A</sub> Receptor Agents."],"pmcid":["PMC9917830"],"funding_grant_id":["FW24/2/F/GW/N/20","FW24/F/PW2/N/20"],"pubmed_authors":["Bujalska-Zadrozny M","Dobrzycki L","Gryczka W","Ostrowska K","Lesniak A","Trzaskowski B"],"additional_accession":[]},"is_claimable":false,"name":"New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT<sub>1A</sub> Receptor Agents.","description":"A series of 15 new derivatives of 6-acetyl-7-hydroxy-4-methylcoumarin containing a piperazine group were designed with the help of computational methods and were synthesized to study their affinity for the serotonin 5-HT<sub>1A</sub> and 5-HT<sub>2A</sub> receptors. Among them, 6-acetyl-7-{4-[4-(3-bromophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (<b>4</b>) and 6-acetyl-7-{4-[4-(2-chlorophenyl)piperazin-1-yl]butoxy}-4-methylchromen-2-one (<b>7</b>) exhibited excellent activity for 5-HT<sub>1A</sub> receptors with Ki values 0.78 (0.4-1.4) nM and 0.57 (0.2-1.3) nM, respectively, comparable to the Ki values of 8-OH-DPAT (0.25 (0.097-0.66) nM). The equilibrium dissociation constant values of the tested compounds showed differential intrinsic activities of the agonist and antagonist modes.","dates":{"release":"2023-01-01T00:00:00Z","publication":"2023 Feb","modification":"2026-04-08T14:15:01.195Z","creation":"2025-02-19T02:23:59.774Z"},"accession":"S-EPMC9917830","cross_references":{"pubmed":["36769117"],"doi":["10.3390/ijms24032779"]}}