Related Experiment Videos
New arylpiperazine derivatives with high affinity for alpha1A, D2 and 5-HT2A receptors
J C González-Gómez1, L Santana, E Uriarte
1Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago, Campus Sur s/n, E-15782 Santiago de Compostela, Spain. qolsant@usc.es
Abstract:
A series of novel long-chain arylpiperazines bearing a coumarin fragment was synthesized and the compounds were evaluated for their affinity at alpha(1), D(2 )and 5-HT(2A) receptors. Most of the new compounds showed high affinity for the three types of receptors alpha(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 (pK(i) values of 7.93 and 6.76 respectively). The higher alpha(1A) receptor affinity (pA(2)=9.07) of this compound could contribute to a more atypical antipsychotic profile than the haloperidol.