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Descoberta de novos protótipos N-fenilpiperazínicos heteroarilazólicos candidatos a fármacos antipsicóticos atípicos
(2010) Fraga, Carlos Alberto Manssour; Menegatti, Ricardo; Barreiro, Eliezer Jesus de Lacerda; Neves, G.; Betti, Andresa Heemann; Kliemann, Mariéle; Rates, Stela M. K.; Tasso, L.; Conrado, D. J.; Costa, T. D.; Oliveira, V. de; Noël, F.
This 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.