The latest discovered subtype of serotonin receptors - 5-HT₇ - emerged as a new valuable therapeutic target. Based on its distribution and pharmacological studies, the 5-HT₇ receptors has been implicated in many different functions in CNS (like circadian rhythm, learning and memory, mood, endocrine regulation) as well as in the periphery. It was found that many of the previously described serotonin ligands showed a high level of 5-HT₇ receptor activity. The latter was observed for 5-HT_1A agents, in particular in the group of long-chain arylpiperazine derivatives (LCAPs).

As part of our research program directed toward development of potent and selective 5-HT₇ receptor ligands, we synthesized a novel series of LCAPs analogues. The structural modifications included replacement of terminal amide fragment by aryl sulfonamide moiety and/or changes of aromatic substituent in arylpiperazine fragment.

All the new compounds were evaluated for affinity at 5-HT₇ and 5-HT_1A receptors and preliminary structure-affinity relationships are presented.

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2. Searching for lead molecules as potential new CNS agents in the serotonin 5-HT₆ screening assay
3. Searching for the 5-HT₇ receptor ligands in the series of new 1,2,3,4-tetrahydroisoquinolines with imide fragment
4. Synthesis and molecular modeling of 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides as potential 5-HT₇ receptor ligands
5. 2-(1-Arylsulfonylpiperidin-2-yl)ethyl derivatives as 5-HT₇ receptor ligands: synthesis and their affinity for 5-HT_1A/5-HT_2A/5-HT₇/D₂ receptors
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