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Aripiprazole as dopamine partial agonist model: Basic concepts and clinical impact

Abstract : Aripiprazole may be viewed as the prototype of third-generation antipsychotics. This concept is based on the notion of D2 partial agonism, whereas all molecules of first-and second generation were D2 antagonists. After reviewing the basic pharmacological notions linked to such concepts, the mechanisms of action of these molecules are addressed, with a particular focus on functional selectivity and biased ligand. One of the essential pharmacological properties of D2 agonists, and particularity aripiprazole, is their ability to not induce D2 supersensitivity as well as to reverse this supersensitivity when it has been induced by D2 antagonists. In clinical practice, this impacts the choice of treatment in first episode psychosis as well as in refractory schizophrenia. Animal research shows that D2 supersensitivity could contribute to worsen addictive trends. The pharmacokinetic incidence of D2 supersensitivity tends to favour the long-acting forms of partial agonists. The notion of partial agonism could finally lead to design fourth-generation antipsychotics, on the basis on research focusing on functional selectivity. (C) 2018
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https://hal-amu.archives-ouvertes.fr/hal-02146872
Contributor : Jean-Charles Dufour <>
Submitted on : Tuesday, June 4, 2019 - 11:49:19 AM
Last modification on : Wednesday, March 25, 2020 - 2:35:53 PM

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N. Simon, J. -M. Azorin. Aripiprazole as dopamine partial agonist model: Basic concepts and clinical impact. L'Encéphale, Elsevier Masson, 2018, 44 (6), pp.558-564. ⟨10.1016/j.encep.2018.10.003⟩. ⟨hal-02146872⟩

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