Discovery of bishomo(hetero)arylpiperazines as novel multifunctional ligands targeting dopamine D(3) and serotonin 5-HT(1A) and 5-HT(2A) receptors.
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.
Butini
Stefania
S
European Research Centre for Drug Discovery and Development, Universita di Siena, 53100 Siena, Italy.
Campiani
Giuseppe
G
Franceschini
Silvia
S
Trotta
Francesco
F
Kumar
Vinod
V
Guarino
Egeria
E
Borrelli
Giuseppe
G
Fiorini
Isabella
I
Novellino
Ettore
E
Fattorusso
Caterina
C
Persico
Marco
M
Orteca
Nausicaa
N
Sandager-Nielsen
Karin
K
Jacobsen
Thomas Amos
TA
Madsen
Kim
K
Scheel-Kruger
Jorgen
J
Gemma
Sandra
S
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
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