2-{4-[ω-[4-(2-methoxyphenyl)-1-piperazinyl] alkoxy] phenyl}phthalimides as ligands for some 5-HT, dopamine and adrenergic receptor subtypes

We have prepared and studied some new 2-methoxyphenylpiperazine derivatives as combined ligands for 5-HT1A and D3 receptor subtypes. The introduction of a phenyloxy moiety between the phthalimido group and the polymethylene chain of nanserone does not impair the typical high affinity for 5-HT1A receptors, but reduces in different measures the affinity for 5-HT2, D2 and α1-receptors. Good affinity for the D3-receptor subtype has also been observed. The polymethylene chain length remains a critical factor in determining optimal affinity and selectivity.