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 …
E Lacivita, D Patarnello, N Stroth, A Caroli…
文献索引：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 Journal of Medicinal Chemistry, 2012 , vol. 55, # 14 p. 6375 - 6380
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 ...
