Aripiprazole: what is the role of dopamine D(2) receptor partial agonism?

  title={Aripiprazole: what is the role of dopamine D(2) receptor partial agonism?},
  author={Robert M. Kessler},
  journal={The American journal of psychiatry},
  volume={164 9},
  • R. Kessler
  • Published 1 September 2007
  • Psychology
  • The American journal of psychiatry

Aripiprazole combination for reversal of paliperidone-induced increase in prolactin level

It is found that the prolactin level was decreased after the administration of a combination with a low-dose aripiprazole, a common side effect of antipsychotic drugs.

Aripiprazole reversed gastroparesis in a child with 1q21.1–q21.2 microdeletion

An 11-year-old Caucasian boy, with a microdeletion in the 1q 21.1–q21.2 region, had multiple medical conditions including gastroparesis documented initially at the age of 5, and was started on metoclopramide with an increase in his appetite, oral intake and weight gain.

Spontaneous Ejaculations Associated with Aripiprazole.

The partial agonistic effect of aripiprazole on D2 receptors may have augmented the mesolimbic dopaminergic pathway, which was suppressed by risperidone, causing spontaneous ejaculations in this patient.

Aripiprazole an atypical antipsychotic protects against ethanol induced gastric ulcers in rats.

ARI showed significant antiulcer and gastroprotective activity against ethanol induced gastric ulcers in rats and may be due to its anti-secretory, antioxidant and anti-inflammatory action and also due to the restoration of the depleted gastric serotonin levels.

Hyperprolactinemia with Aripiprazole: a Case Report and Review of the Literature

Hyperprolactinemia is an important but often a neglected side effect of antipsychotic treatment. Aripiprazole is one of the new atypical antipsychotics that has partial agonist effects on dopamine ...

Key functional circuitry altered in schizophrenia involves parietal regions associated with sense of self

The findings identify the key functional circuitry altered in schizophrenia involving the default network midline cortical system and the cortical mirror neuron system, both playing important roles in sensory and cognitive processing and particularly self‐processing, all of which are affected in this disorder.

Two Cases of Hypersexuality Probably Associated with Aripiprazole

It is argued that aripiprazole's unique pharmacological profile, partial agonism with high affinity at dopamine D2-receptor, may have contributed to the development of hypersexuality symptoms in two female patients with schizophrenia who were receiving treatment with aripIPrazole.

History of Antipsychotic Drug Development

The history of antipsychotic drugs starting with the birth of typical antipsychotics developed over a half century ago, the current newer safer atypical agents for treatment of schizophrenia, and novel emerging therapies being developed in the new millennium are reviewed.

Système sérotoninergique 5-HT1A et schizophrénie : étude par tomographie par émission de positons au p-[18F]MPPF chez des patients schizophrènes traités par antipsychotiques

La comparaison des images TEP obtenues chez les patients selon que le traitement antipsychotique recu a une action agoniste 5-HT1A (aripiprazole) ou en soit depourvu (olanzapine, risperidone) a montre une diminution plus importante du [18F]MPPF BPND.



Aripiprazole: a novel atypical antipsychotic drug with a uniquely robust pharmacology.

Clinical trials indicate that aripiprazole is effective in treating the positive and negative symptoms of schizophrenia, and pilot data suggest that a revised dosing strategy, based on weight, is indicated in this population of patients.

Evaluation of EMD 128 130 occupancy of the 5-HT1A and the D2 receptor: a human PET study with [11]WAY-100635 and [11C]raclopride

Investigation of the occupancy of EMD 128 130 in vivo at the human D2 and 5-HT1A receptors with positron emission tomography using the radiotracers [ 11C]raclopride and [11C]WAY-100635 found a significant occupancy was demonstrated at thehuman D2 receptor while there was no consistent effect observed at the 5- HT1A receptor.

Serotonin receptors : their key role in drugs to treat schizophrenia

Antipsychotic-Like vs Cataleptogenic Actions in Mice of Novel Antipsychotics Having D2 Antagonist and 5-HT1A Agonist Properties

It is confirmed that 5-HT1A receptor activation reduces or even completely prevents the cataleptogenic potential of novel antipsychotic agents and indicates that the balance of affinity and/or efficacy between D2 and 5- HT1A receptors profoundly influences their pharmacological activities, and will likely impact their therapeutic profiles.

Dissociation between In Vivo Occupancy and Functional Antagonism of Dopamine D2 Receptors: Comparing Aripiprazole to Other Antipsychotics in Animal Models

Investigating the discrepancy between D2RO, 5HT2 receptor occupancy (5-HT2RO) and in vivo functional activity of aripiprazole in comparison to haloperidol and risperidone in animal models provides a framework for understanding occupancy-functional relationships of partial D2 agonist antipsychotics.

Occupancy of Agonist Drugs at the 5-HT1A Receptor

It is concluded that 5-HT1A receptor agonists produce detectable occupancy only at higher doses that would produce unacceptable levels of side effects in man, although lower doses are sufficient to produce pharmacological effects.

Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology

The results support the hypothesis that the unique actions of aripiprazole in humans are likely a combination of ‘functionally selective’ activation of D2 (and possibly D3)-dopamine receptors, coupled with important interactions with selected other biogenic amine receptors—particularly 5-HT receptor subtypes (5-HT1A, 5- HT2A).

Effectiveness of long-term aripiprazole therapy in patients with acutely relapsing or chronic, stable schizophrenia: a 52-week, open-label comparison with olanzapine

Aripiprazole showed similar efficacy to olanzapine for long-term treatment of acutely psychotic and chronic, stable schizophrenia patients, with a lower liability for weight gain or increased lipid levels.

The neurocognitive effects of aripiprazole: an open-label comparison with olanzapine

The findings from this open-label study suggest that the neurocognitive effects of aripiprazole are at least as good as those of olanzapine.