Creativity in the Development of the Drug, Aripiprazle: A novel partial dopamine D2 receptors agonist for the treatment of schizophrenia Michio TORU 1,2 2Mental Clinic Ogikubo Keyword: Aripiprazole , Schizophrenia , Dopamine D2 partial agonist , 5-HT1A and 5-HT2A , Safety and tolerability pp.855-864
Published Date 2004/8/15
DOI https://doi.org/10.11477/mf.1405100536
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 Herein is presented a review of the history of the development of aripiprazole, a drug primarily for the treatment of schizophrenia. Aripiprazole is the name given to OPC-14597, a quinolinone derivative that was synthesized in 1987 by Y. Oshiro, a chemist. T. Kikuchi, a behavioral pharmacologist, conducted repeated experiments with hundreds of quinolinone derivatives, and finally concluded that aripiprazole was a dopamine autoreceptor agonist possessing a potent antagonistic action at dopamine D2 receptors. Aripiprazole is also a potent partial agonist at serotonin 5-HT1A receptors and an antagonist at 5-HT2A receptors. Thus, aripiprazole is not merely a dopaminergic stabilizer, but rather a dopamine-serotonin system stabilizer that has a favorable safety profile. In clinical studies, aripiprazole has been demonstrated to be effective against both the positive and negative symptoms of schizophrenia, to be associated with low incidences of extrapyramidal symptoms, tardive dyskinesia, weight gain, sedation, hyperprolactinemia, and QTc prolongation, and to have no adverse effects on glucose and lipid levels. Aripiprazole has the potential to be one of the best agents for the treatment of schizophrenia.

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