New arylpiperazine derivatives with high affinity for α 1A, D 2 and 5-HT 2A receptors

Abstract

A series of novel long-chain arylpiperazines bearing a coumarin fragment was synthesized and the compounds were evaluated for their affinity at α 1, D 2 and 5-HT 2A receptors. Most of the new compounds showed high affinity for the three types of receptors α 1A, D 2 and 5-HT 2A which depends, fundamentally, on the substitution of the N 4 of the piperazine ring. From the series emerged compound 6, which had an haloperidol-like profile at D 2 and 5HT 2A receptors (p K i values of 7.93 and 6.76 respectively). The higher α 1A receptor affinity (p A 2=9.07) of this compound could contribute to a more atypical antipsychotic profile than the haloperidol.