The 5-HT₇ receptor is the latest identified serotonin (5-hydroxytryptamine, 5-HT) receptor subtype. The brain distribution of 5-HT₇ receptors suggests their significant role in many mental diseases [1]. Thus, the novel and selective 5-HT₇ receptor ligands which may have potential therapeutic implications are a putative targets for novel drug discovery [2[.

Here we report the synthesis of a series of 1,2,3,4-tetrahydroisoquinolines with mono- or disubstituted arylsulfonamide moiety. The structure of new compounds was confirmed by ¹H NMR spectra as well as by C, H, N analysis. For all compounds the 5-HT₇ receptor affinity was determined and some structure-affinity relationships are discussed.

Molecular modeling techniques were used to rationalize the structure-activity relationships. The studied compounds were docked to the homology model of 5-HT₇ receptor and the binding modes were described.

[1] Thomas, D.R.; Hagan, J.J. Curr. Drug Targets – CNS & Neurological Disorders 2004, 3, 81-90.
[2] Leopoldo M. Curr. Med. Chem. 2004, 11, 629-661.

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1. Searching for the 5-HT₇ receptor ligands in the series of new 1,2,3,4-tetrahydroisoquinolines with imide fragment
2. 4,6-DISUBSTITUTED 2-(4-METHYL-1-PIPERA- ZINYL)PYRIDINES: SYNTHESIS AND THEIR BINDING TO SEROTONIN 5-HT_1A, 5-HT_2A, AND 5-HT₇ RECEPTORS
3. STRUCTURAL MODIFICATIONS OF SOME ARYLPIPERAZINE LIGANDS TOWARDS IMPROVED SELECTIVITY FOR 5-HT₇ RECEPTORS
4. THE BIOLOGICAL TARGET DERIVED PHARMACOPHORIC MODEL FOR 5-HT₇ SEROTONIN RECEPTOR ANTAGONISM