| 12570387 |
Perrone R, Berardi F, Colabufo NA, Lacivita E, Leopoldo M, Tortorella V: Synthesis and structure-affinity relationships of 1-[omega-(4-aryl-1-piperazinyl) alkyl]-1-aryl ketones as 5-HT (7) receptor ligands. J Med Chem. 2003 Feb 13;46(4):646-9.
Structural requirements for 5-HT (7) receptor affinity and selectivity over that for the 5-HT (1A) receptor were studied on a series of 1-[omega-(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-HT (7) receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT (7) receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction. |
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