New arylpiperazine derivatives with high affinity for alpha1A,D2 and 5-HT2A receptors |
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Authors: | González-Gómez J C Santana L Uriarte E Brea J Villazón M Loza M I De Luca M Rivas M E Montenegro G Y Fontenla J A |
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Affiliation: | Department of Organic Chemistry, Faculty of Pharmacy, University of Santiago, Campus Sur s/n, E-15782 Santiago de Compostela, Spain. qolsant@usc.es |
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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. |
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