Neurobiological bases and clinical aspects of the use of aripiprazole in treatment-resistant major depressive disorder

Arylpiperazinylalkyl derivatives of 8-amino-1,3-dimethylpurine-2,6-dione as novel multitarget 5-HT/D receptor agents with potential antipsychotic activity

“…Among the evaluated compounds, weak 5-HT 7 R antagonistic properties were observed in the case of 34 (Table 5). Taking into account the functional profile, the evaluated compounds corresponded to aripiprazole which exerts not only partial dopaminergic activity but also a 5-HT 1A and 5-HT 2C receptor partial agonist and 5-HT 2A and 5-HT 7 antagonist and this mechanism of action may contribute to its broad efficacyantipsychotic, antidepressant, and anxiolytic [53][54][55] . Moreover, among the evaluated compounds, 43 and 46 showed 5-HT 6 antagonistic properties (IC 50 values ¼ 676 and 847 nM, respectively) ( Table 5).…”

Differential and Converging Molecular Mechanisms of Antidepressants’ Action in the Hippocampal Dentate Gyrus

“…Strikingly, a high percentage of patients treated with the currently available therapies do not show full remission (Lang and Borgwardt, 2013) and present treatment resistance (Blier and Blondeau, 2011). Although the pathophysiology of depression is still incompletely understood, dysregulation of monoaminergic systems, neuroplasticity, and immunological responses (Villanueva, 2013;Willner et al, 2013) are considered to contribute to the disease.…”

Evaluating The Antidepressant Efficacy of Aripiprazole Using a Chronic Mild Stress Model: An Experimental Study

“…It is also known that dopamine activity in the frontal cortical area is impaired in depression 8 . Preclinic data supports that aripiprazole may be effective in depression treatment through partial dopamine agonism and 5-HT antagonism [40][41][42][43] . In studies with animal depression models, depression was shown to be related to dopaminergic deficiency and this condition may be reversed by dopamine agonists 8 .…”