| 17517509 |
Leopoldo M, Lacivita E, Colabufo NA, Niso M, Berardi F, Perrone R: Bivalent ligand approach on 4-[2-(3-methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine: synthesis and binding affinities for 5-HT (7) and 5-HT (1A) receptors. Bioorg Med Chem. 2007 Aug 1;15(15):5316-21. Epub 2007 May 6.
We here report on the synthesis and binding properties at 5-HT (7) and 5-HT (1A) receptors of ligands 3-12, that were designed according to the 'bivalent ligand' approach. Two moieties of the 5-HT (7)/5-HT (1A) ligand 4-[2-(3-methoxyphenyl) ethyl]-1-(2-methoxyphenyl) piperazine (1) were linked through their 3-methoxy substituent by polymethylene chains of variable length, with the aim to increase the affinity for 5-HT (7) receptor and the selectivity over 5-HT (1A) receptors. In the best cases, the dimers showed affinities for 5-HT (7) receptors as high as the monomer with no improvement in selectivity. Some dimers displayed 5-HT (1A) receptor affinities slightly higher than monomer 1. |
113(1,2,2,3) |