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

  title={Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology},
  author={David A. Shapiro and Sean M Renock and Elaine G Arrington and Louis A. Chiodo and Li-xin Liu and David R. Sibley and Bryan L. Roth and Richard B. Mailman},
Atypical antipsychotic drugs have revolutionized the treatment of schizophrenia and related disorders. The current clinically approved atypical antipsychotic drugs are characterized by having relatively low affinities for D2-dopamine receptors and relatively high affinities for 5-HT2A serotonin receptors (5-HT, 5-hydroxytryptamine (serotonin)). Aripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity D2-dopamine receptor partial agonist. We now… 

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.

Aripiprazole acts as a selective dopamine D2 receptor partial agonist

Data is reviewed that suggest that aripiprazole acts as a selective partial agonist at the dopamine D2 receptor and does not affect 5-HT receptors at therapeutic doses.

Current Limitations and Candidate Potential of 5-HT7 Receptor Antagonism in Psychiatric Pharmacotherapy

To explore candidate novel applications for the treatment of several neuropsychiatric disorders, including mood disorders, schizophrenia, and other cognitive disturbance disorders, the effects of 5-HT7R antagonism on transmission and intracellular signaling systems are discussed.

Psychopharmacology of atypical antipsychotic drugs: From the receptor binding profile to neuroprotection and neurogenesis

A critical review of the pharmacology of atypical APD is provided, especially from the viewpoint of receptor binding profiles and neurotransmitter regulations as well as neuroprotection and neurogenesis, to suggest that GSK‐3β might play a role in the action mechanisms of atymic APD, in both the 5‐HT‐dependent and BDNF‐dependent mechanisms.

Aripiprazole, A Drug that Displays Partial Agonism and Functional 

A combination of factors such as dopamine system stabilization via partial agonism, functional selectivity at D2 receptors, and serotonin-dopamine system interaction may contribute to the ability of aripiprazole to successfully manage schizophrenia symptoms.

The psychopharmacology of ziprasidone: receptor-binding properties and real-world psychiatric practice.

Ziprasidone targets the key hypothetical neurochemical disturbance in psychosis-excessive dopamine neurotransmission at dopamine D2 receptors in the mesolimbic pathway of the brain-presumably responsible for the positive symptoms of schizophrenia.



Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.

It is demonstrated that both typical and atypical antipsychotic drugs may exhibit inverse agonist effects at the 5- HT2C-INI isoform of the human 5-HT2C receptor and that no relationship exists between inverse agonists actions and attypicality.

Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors

These results, together with previous studies demonstrating partial agonist activity at serotonin 5-hydroxytryptamine (5-HT)1A receptors and antagonist activity at 5-HT2A receptors, support the identification of aripiprazole as a dopamine-serotonin system stabilizer.

H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

It is recommended that the next generation of atypical antipsychotic drugs be screened to avoid H1-histamine receptors, which are known to induce weight gain with chronic use.

Aripiprazole: profile on efficacy and safety

Early data suggest that aripiprazole may induce reductions in plasma prolactin, as well as in plasma glucose and lipid profiles, and results also support the proposition that it may lead to reductions in corrected QT interval and have minimal drug interactions.

Interactions of the Novel Antipsychotic Aripiprazole (OPC-14597) with Dopamine and Serotonin Receptor Subtypes

Activation is Hallucinogenic and Antagonism is Therapeutic: Role of 5-HT2A Receptors in Atypical Antipsychotic Drug Actions

Evidence is presented demonstrating that atypical antipsychotic drugs, as a group, have a preferentially high affinity for 5-HT2A receptors, compared with their affinities for other neurotransmitter receptors.

Binding of typical and atypical antipsychotic drugs to multiple neurotransmitter receptors.

Serotonin receptors : their key role in drugs to treat schizophrenia