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The Dopamine D2 Receptor Partial Agonist Antipsychotics, Aripiprazole, and Brexpiprazole

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NeuroPsychopharmacotherapy

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Abstract

Aripiprazole (Abilify®), a carbostyril derivative, is an antipsychotic with a new mechanism of action that differs from those of existing dopamine D2 receptor antagonist antipsychotics; that is, dopamine D2 receptor partial agonist activity and was discovered by Otsuka Pharmaceutical Co., Ltd. and was developed in collaboration with Bristol-Myers Squibb. With its dopamine D2 receptor partial agonist activity, aripiprazole does not cause excessive blockade of the dopamine D2 receptor-mediated signaling. Therefore, the risk of causing D2 receptor antagonism-related side effects is very low, unlike existing dopamine D2 receptor antagonist antipsychotics. Because of these properties, aripiprazole contributes to the enhancement of treatment compliance and consequently to the prevention of disease recurrence, attesting to its long-term effectiveness. More than a decade after Otsuka’s discovery of aripiprazole, Otsuka also discovered the dopamine D2 receptor partial agonist antipsychotic, brexpiprazole (Rexulti®). As part of its mechanism of action, brexpiprazole has dopamine D2 receptor partial agonist activity as well as potent serotonergic activities that aripiprazole does not have. Brexpiprazole was developed in collaboration with Lundbeck. In this review, we describe pharmacological properties and clinical use of aripiprazole and brexpiprazole.

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Authors and Affiliations

  1. New Drug Research Division, Pharmaceutical Business Division, Otsuka Pharmaceutical Co. Ltd., Tokushima, Japan

    Tetsuro Kikuchi & Tsuyoshi Hirose

  2. Department of Lead Discovery Research, New Drug Research Division, Pharmaceutical Business Division, Otsuka Pharmaceutical Co., Ltd., Tokushima, Japan

    Kenji Maeda

  3. Medical Affairs, Otsuka Pharmaceutical Co., Ltd., Tokyo, Japan

    Sakiko Yamada

  4. Department of CNS Research, New Drug Research Division, Pharmaceutical Business Division, Otsuka Pharmaceutical Co., Ltd., Tokushima, Japan

    Mikio Suzuki & Takashi Futamura

  5. Otsuka Pharmaceutical Development & Commercialization, Inc., Princeton, NJ, USA

    Robert D. McQuade

Authors
  1. Tetsuro Kikuchi
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  2. Kenji Maeda
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  3. Sakiko Yamada
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  4. Mikio Suzuki
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  5. Tsuyoshi Hirose
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  6. Takashi Futamura
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  7. Robert D. McQuade
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Correspondence to Tetsuro Kikuchi .

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Editors and Affiliations

  1. Clinic and Policlinic for Psychiatry, Psychosomatics and Psychotherapy, University Hospital Wuerzburg, Wuerzburg, Germany

    Peter Riederer

  2. Institute of Psychological Medicine (IPM), Soyen, Germany

    Gerd Laux

  3. Centre for Research Promotion and Support, Fujita Health University, Toyoake, Aichi, Japan

    Toshiharu Nagatsu

  4. Center Translational Res Neurol Diseases, Dalian Med Uni Shanghai Inst Health Sc Center Translational Res Neurol Diseases, Dalian, China

    Weidong Le

  5. Würzburg, Germany

    Christian Riederer

Section Editor information

  1. Department of Psychiatry, University Hospital Leipzig, Leipzig, Germany

    Frank Schmidt

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Kikuchi, T. et al. (2022). The Dopamine D2 Receptor Partial Agonist Antipsychotics, Aripiprazole, and Brexpiprazole. In: Riederer, P., Laux, G., Nagatsu, T., Le, W., Riederer, C. (eds) NeuroPsychopharmacotherapy. Springer, Cham. https://doi.org/10.1007/978-3-030-62059-2_424

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  • DOI: https://doi.org/10.1007/978-3-030-62059-2_424

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-030-62058-5

  • Online ISBN: 978-3-030-62059-2

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