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  • Title: Design and synthesis of new homo and hetero bis-piperazinyl-1-propanone derivatives as 5-HT7R selective ligands over 5-HT1AR.
    Author: Intagliata S, Modica MN, Pittalà V, Salerno L, Siracusa MA, Cagnotto A, Salmona M, Romeo G.
    Journal: Bioorg Med Chem Lett; 2016 Aug 15; 26(16):4052-6. PubMed ID: 27396505.
    Abstract:
    In this work we report the discovery of new homo and hetero bis-piperazinyl-1-propanone derivatives as selective ligands for 5-HT7 over 5-HT1A receptor. These newly synthesized compounds possess a 4-arylpiperazine linked through an acyl spacer to another substituted piperazine system and were tested for their binding properties on human cloned 5-HT1A and 5-HT7 serotonin receptors. Among these, phenyl, 4- and 2-chlorophenyl, 2-methoxyphenyl, 2-pyridyl, and 2-pyrimidyl derivatives 15, 24, 25, and 27-29 displayed nanomolar affinity values for the 5-HT7 receptor (Ki 23.5-52.0nM) and no affinity for the 5-HT1A receptor.
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