Abstract
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.
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