501083-58-5Relevant academic research and scientific papers
Synthesis and structure-affinity relationships of 1-[ω-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT7 receptor ligands
Perrone, Roberto,Berardi, Francesco,Colabufo, Nicola A.,Lacivita, Enza,Leopoldo, Marcello,Tortorella, Vincenzo
, p. 646 - 649 (2003)
Structural requirements for 5-HT7 receptor affinity and selectivity over that for the 5-HT1A receptor were studied on a series of 1-[ω-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones. The presence of a hydroxy or methoxy substituent on aryl ketone moiety, alkyl chain length, and the nature of N-1-piperazine substituent were explored. 6-[4-(3-Benzisoxazolyl)-1-piperazinyl]-1-(2-hydroxyphenyl)-1-hexanone (40) and its methoxy analogue 43 exhibited high 5-HT7 receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT7 receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction.
