ArticleNeuropharmacology2008
Recruitment of beta-arrestin2 to the dopamine D2 receptor: insights into anti-psychotic and anti-parkinsonian drug receptor signaling.
Article in Neuropharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 79 citations in OpenAlex.
- D3 dopamine receptors implicate a striatal neuronal subtype in the aversive effects of the antipsychotic drug quetiapine.bioRxiv : the preprint server for biology · 2026Article
- Apomorphine differentially engages the cAMP and β-arrestin signaling pathways relative to dopamine at human dopamine receptors.Journal of neural transmission (Vienna, Austria : 1996) · 2025Article
- Molecular mechanism of β-arrestin 2 interaction with phosphorylated intracellular loop 3 of dopamine receptor D2.Communications biology · 2025Article
- In-Cell Arrestin-Receptor Interaction Assays.Current protocols · 2023Article
- Nanoscopic dopamine transporter distribution and conformation are inversely regulated by excitatory drive and D2 autoreceptor activity.Cell reports · 2022Article
- Review
- Translation-Focused Approaches to GPCR Drug Discovery for Cognitive Impairments Associated with Schizophrenia.ACS pharmacology & translational science · 2020Review
- Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation.Molecular psychiatry · 2020Article
- A Split Luciferase Complementation Assay for the Quantification of β-Arrestin2 Recruitment to Dopamine DInternational journal of molecular sciences · 2020Article
- A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework.Scientific reports · 2020Article
- Optical approaches for single-cell and subcellular analysis of GPCR-G protein signaling.Analytical and bioanalytical chemistry · 2019Review
- Evaluation of Functional Selectivity of Haloperidol, Clozapine, and LASSBio-579, an Experimental Compound With Antipsychotic-Like Actions in Rodents, at G Protein and Arrestin Signaling Downstream of the Dopamine DFrontiers in pharmacology · 2019Article
- The Beta-Arrestin-Biased Dopamine D2 Receptor Ligand, UNC9994, Is a Partial Agonist at G-Protein-Mediated Potassium Channel Activation.The international journal of neuropsychopharmacology · 2018Article
- Selective blockade of spinal D2DR by levo-corydalmine attenuates morphine tolerance via suppressing PI3K/Akt-MAPK signaling in a MOR-dependent manner.Experimental & molecular medicine · 2018Article
- Multi-Target Approach for Drug Discovery against Schizophrenia.International journal of molecular sciences · 2018Review
- Antipsychotic-Like Efficacy of Dopamine DMolecular neurobiology · 2018Article
- The role of beta-arrestin2 in shaping fMRI BOLD responses to dopaminergic stimulation.Psychopharmacology · 2017Article
- Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.Journal of medicinal chemistry · 2016Article
- The Conserved Arginine Cluster in the Insert of the Third Cytoplasmic Loop of the Long Form of the D₂ Dopamine Receptor (D2L-R) Acts as an Intracellular Retention Signal.International journal of molecular sciences · 2016Article
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 2 countries.
Funding
Abstract
Drugs acting at dopamine D2-like receptors play a pivotal role in the treatment of both schizophrenia and Parkinson's disease. Recent studies have demonstrated a role for G-protein independent D2 receptor signaling pathways acting through beta-arrestin. In this study we describe the establishment of a Bioluminescence Resonance Energy Transfer (BRET) assay for measuring dopamine induced recruitment of human beta-arrestin2 to the human dopamine D2 receptor. Dopamine, as well as the dopamine receptor agonists pramipexole and quinpirole, acted as full agonists in the assay as reflected by their ability to elicit marked concentration dependent increases in the BRET signal signifying beta-arrestin2 recruitment to the D2 receptor. As expected from their effect on G-protein coupling and cAMP levels mediated through the D2 receptor RNPA, pergolide, apomorphine, ropinirole, bromocriptine, 3PPP, terguride, aripiprazole, SNPA all acted as partial agonists with decreasing efficacy in the BRET assay. In contrast, a wide selection of typical and atypical anti-psychotics was incapable of stimulating beta-arrestin2 recruitment to the D2 receptor. Moreover, we observed that haloperidol, sertindole, olanzapine, clozapine and ziprasidone all fully inhibited the dopamine induced beta-arrestin2 recruitment to D2 receptor (short variant) in a concentration dependent manner. We conclude that most anti-psychotics are incapable of stimulating beta-arrestin2 recruitment to the dopamine D2 receptor, in accordance with their antagonistic properties at the level of G-protein coupling.
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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.