Author/Authors :
J. C. Gonz?lez-G?mez، نويسنده , , L. Santana، نويسنده , , E. Uriarte، نويسنده , , J. Brea، نويسنده , , M. Villaz?n، نويسنده , , M. I. Loza، نويسنده , , M. De Luca، نويسنده , , M. E. Rivas، نويسنده , , G. Y. Montenegro، نويسنده , , J. A. Fontenla، نويسنده ,
Abstract :
A series of novel long-chain arylpiperazines bearing a coumarin fragment was synthesized and the compounds were evaluated for their affinity at α1, D2 and 5-HT2A receptors. Most of the new compounds showed high affinity for the three types of receptors α1A, D2 and 5-HT2A which depends, fundamentally, on the substitution of the N4 of the piperazine ring. From the series emerged compound 6, which had an haloperidol-like profile at D2 and 5HT2A receptors (pKi values of 7.93 and 6.76 respectively). The higher α1A receptor affinity (pA2=9.07) of this compound could contribute to a more atypical antipsychotic profile than the haloperidol.
