728919-24-2Relevant academic research and scientific papers
Investigations on the 1-(2-biphenyl)piperazine motif: Identification of new potent and selective ligands for the serotonin7 (5-HT7) receptor with agonist or antagonist action in vitro or ex vivo
Lacivita, Enza,Patarnello, Daniela,Stroth, Nikolas,Caroli, Antonia,Niso, Mauro,Contino, Marialessandra,De Giorgio, Paola,Di Pilato, Pantaleo,Colabufo, Nicola A.,Berardi, Francesco,Perrone, Roberto,Svenningsson, Per,Hedlund, Peter B.,Leopoldo, Marcello
supporting information; experimental part, p. 6375 - 6380 (2012/10/08)
Here we report the design, synthesis, and 5-HT7 receptor affinity of a set of 1-(3-biphenyl)- and 1-(2-biphenyl)piperazines. The effect on 5-HT7 affinity of various substituents on the second (distal) phenyl ring was analyzed. Several compounds showed 5-HT7 affinities in the nanomolar range and >100-fold selectivity over 5-HT1A and adrenergic α1 receptors. 1-[2-(4-Methoxyphenyl)phenyl] piperazine (9a) showed 5-HT7 agonist properties in a guinea pig ileum assay but blocked 5-HT-mediated cAMP accumulation in 5-HT7- expressing HeLa cells.
