title: Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
abstract: As a continuation of our efforts to develop innovative ligands for D(3), 5-HT(1A), and 5-HT(2A) receptors with low propensity to block hERG channels, we propose a series bishetero(homo)arylpiperazines 5a-m as novel and potent multifunctional ligands characterized by low occupancy at D(2) and 5-HT(2C) receptors.
authors.affiliation: European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy.
authors.forename: Stefania
authors.initials: S
authors.lastname: Butini
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Campiani
authors.forename: Silvia
authors.initials: S
authors.lastname: Franceschini
authors.forename: Francesco
authors.initials: F
authors.lastname: Trotta
authors.forename: Vinod
authors.initials: V
authors.lastname: Kumar
authors.forename: Egeria
authors.initials: E
authors.lastname: Guarino
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Borrelli
authors.forename: Isabella
authors.initials: I
authors.lastname: Fiorini
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Caterina
authors.initials: C
authors.lastname: Fattorusso
authors.forename: Marco
authors.initials: M
authors.lastname: Persico
authors.forename: Nausicaa
authors.initials: N
authors.lastname: Orteca
authors.forename: Karin
authors.initials: K
authors.lastname: Sandager-Nielsen
authors.forename: Thomas Amos
authors.initials: TA
authors.lastname: Jacobsen
authors.forename: Kim
authors.initials: K
authors.lastname: Madsen
authors.forename: Jorgen
authors.initials: J
authors.lastname: Scheel-Kruger
authors.forename: Sandra
authors.initials: S
authors.lastname: Gemma
mesh_terms: D000818:Animals; D014150:Antipsychotic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors / Q000378:metabolism; D006801:Humans; D008024:Ligands; D051379:Mice; D008958:Models, Molecular; D010879:Piperazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*; D050637:Receptors, Dopamine D3 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D014150:Antipsychotic Agents; D000072237:ERG1 Potassium Channel; D051638:Ether-A-Go-Go Potassium Channels; C000606913:KCNH2 protein, human; D008024:Ligands; D010879:Piperazines; D044402:Receptor, Serotonin, 5-HT2A; D050637:Receptors, Dopamine D3; D044282:Receptor, Serotonin, 5-HT1A