ArticleBiochemical pharmacology2015
New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling.
Article in Biochemical pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
19 citing papers in PubMed, 37 citations in OpenAlex.
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- Dopamine antagonist effects of the D2/D3 receptor partial agonist aripiprazole on effort-based choice tasks in male and female rats.Cognitive, affective & behavioral neuroscience · 2026Article
- A neuroimmune pathway drives bacterial infection.Science advances · 2025Article
- TAAR1 dependent and independent actions of the potential antipsychotic and dual TAAR1/5-HTNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2022Article
- Investigating the ligand agonism and antagonism at the DScientific reports · 2022Article
- Biased Ligands at the Kappa Opioid Receptor: Fine-Tuning Receptor Pharmacology.Handbook of experimental pharmacology · 2022Review
- Synthesis and In Vitro Evaluation of Novel Dopamine Receptor DBiomolecules · 2021Article
- State-dependent effects of the DNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2019Article
- Efficacy of low-dose DNeuropsychiatric disease and treatment · 2019Article
- Study on risk factors of extrapyramidal symptoms induced by antipsychotics and its correlation with symptoms of schizophrenia.General psychiatry · 2019Article
- Multi-Target Approach for Drug Discovery against Schizophrenia.International journal of molecular sciences · 2018Review
- Current Concepts and Treatments of Schizophrenia.Molecules (Basel, Switzerland) · 2018Review
- Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity.Current neuropharmacology · 2017Article
- Animal models for bipolar disorder: from bedside to the cage.International journal of bipolar disorders · 2017Review
- Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties.Science signaling · 2017Article
- Antipsychotic Induced Dopamine Supersensitivity Psychosis: A Comprehensive Review.Current neuropharmacology · 2017Review
- Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.Science signaling · 2016Article
- Biased agonism: An emerging paradigm in GPCR drug discovery.Bioorganic & medicinal chemistry letters · 2016Review
- Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways.The Journal of pharmacology and experimental therapeutics · 2015Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The dopamine D2 receptor (DRD2) is a G protein-coupled receptor (GPCR) that is generally considered to be a primary target in the treatment of schizophrenia. First generation antipsychotic drugs (e.g. haloperidol) are antagonists of the DRD2, while second generation antipsychotic drugs (e.g. olanzapine) antagonize DRD2 and 5HT2A receptors. Notably, both these classes of drugs may cause side effects associated with D2 receptor antagonism (e.g. hyperprolactemia and extrapyramidal symptoms). The novel, "third generation" antipsychotic drug, aripiprazole is also used to treat schizophrenia, with the remarkable advantage that its tendency to cause extrapyramidal symptoms is minimal. Aripiprazole is considered a partial agonist of the DRD2, but it also has partial agonist/antagonist activity for other GPCRs. Further, aripiprazole has been reported to have a unique activity profile in functional assays with the DRD2. In the present study the molecular pharmacology of aripiprazole was further examined in HEK cell models stably expressing the DRD2 and specific isoforms of adenylyl cyclase to assess functional responses of Gα and Gβγ subunits. Additional studies examined the activity of aripiprazole in DRD2-mediated heterologous sensitization of adenylyl cyclase and cell-based dynamic mass redistribution (DMR). Aripiprazole displayed a unique functional profile for modulation of G proteins, being a partial agonist for Gαi/o and a robust antagonist for Gβγ signaling. Additionally, aripiprazole was a weak partial agonist for both heterologous sensitization and dynamic mass redistribution.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.