2018-10-192018-10-192010Fraga, C. A. M. et al. Descoberta de novos protótipos N-fenilpiperazínicos heteroarilazólicos candidatos a fármacos antipsicóticos atípicos. Revista Virtual de Química, Niterói, v. 2, n. 1, p. 28-37, 2010.e- 1984-6835http://repositorio.bc.ufg.br/handle/ri/16215This work describes the discovery of new N-phenylpiperazine prototypes belonging to pyrazole series, i.e. LASSBio-579 (10a), or to 1,2,3-triazole series, represented by LASSBio-581 (10c), which were designed from the structural simplification of the atypical antipsychotic drug clozapine (8). The evaluation of the affinity and intrinsic activity profiles of LASSBio-579 and LASSBio-581 indicate its ability to bind dopamine receptors from D 2 -like family, acting as pre-synaptic agonists. Additionally, the investigation of the antipsychotic properties of these two prototypes in behavioral models has confirmed its effectiveness, which is also dependent on the modulation of serotoninergic receptors 5-HT 2A and 5-HT 1A . The pronounced antipsychotic effect evidenced for these N-phenylpiperazine derivatives through in vivo pharmacological assays confirmed their importance as new neuroactive drug-candidate prototypes for the treatment of schizophrenia.porAcesso AbertoN-phenylpiperazineDrug designPyrazoleMultitarget drugs1,2,3-triazoleAntipsychotic drugsN-fenilpiperazina;Planejamento de fármacosPirazolaFármacos multirreceptores1,2,3-triazolFármacos antipsicóticosArtigo10.5935/1984-6835.20100004