Structure-functional selectivity relationship studies of β-arrestin-biased dopamine D₂ receptor agonists.

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2012-08-23

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/jm300603yPMID 22845053PMCID PMC3443605
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Discovery of PF-00217830: aryl piperazine napthyridinones as D2 partial agonists for schizophrenia and bipolar disorder.

  2011cited by this paper
• Discovery of β-Arrestin–Biased Dopamine D2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy

  2011cited by this paper
• Synthesis and characterization of selective dopamine D₂ receptor ligands using aripiprazole as the lead compound.

  2011cited by this paper
• Third generation antipsychotic drugs: partial agonism or receptor functional selectivity?

  2010cited by this paper
• Cariprazine (RGH-188), a Dopamine D3 Receptor-Preferring, D3/D2 Dopamine Receptor Antagonist–Partial Agonist Antipsychotic Candidate: In Vitro and Neurochemical Profile

  2010cited by this paper
• A β-Arrestin–Biased Agonist of the Parathyroid Hormone Receptor (PTH1R) Promotes Bone Formation Independent of G Protein Activation

  2009cited by this paper
• Discovery of a new class of potential multifunctional atypical antipsychotic agents targeting dopamine D3 and serotonin 5-HT1A and 5-HT2A receptors: design, synthesis, and effects on behavior.

  2009cited by this paper
• The genetic design of signaling cascades to record receptor activation

  2008cited by this paper
• Arresting serotonin

  2008cited by this paper
• Effects of aripiprazole/OPC-14597 on motor activity, pharmacological models of psychosis, and brain activity in rats.

  2008influential reference
• [Design, synthesis and vasorelaxant activity of R, S-1-(substituted phenyl)-4-[3-(naphtha-1-yl-oxy)-2-hydroxypropyl]-piperazine derivatives].

  2007cited by this paper
• Regulation of Akt Signaling by D2 and D3 Dopamine Receptors In Vivo

  2007cited by this paper
• GPCR functional selectivity has therapeutic impact.

  2007cited by this paper
• Aripiprazole has Functionally Selective Actions at Dopamine D2 Receptor-Mediated Signaling Pathways

  2007cited by this paper
• Functional Selectivity and Classical Concepts of Quantitative Pharmacology

  2007cited by this paper
• Beta-arrestin-biased ligands at seven-transmembrane receptors.

  2007cited by this paper
• β-Arrestin-biased ligands at seven-transmembrane receptors

  2007cited by this paper
• Intrinsic Efficacy of Antipsychotics at Human D2, D3, and D4 Dopamine Receptors: Identification of the Clozapine Metabolite N-Desmethylclozapine as a D2/D3 Partial Agonist

  2005cited by this paper
• An Akt /-Arrestin 2 / PP 2 A Signaling Complex Mediates Dopaminergic Neurotransmission and Behavior

  2005cited by this paper
• Transduction of Receptor Signals by ß-Arrestins

  2005cited by this paper
• Differential phospholipase C activation by phenylalkylamine serotonin 5‐HT2A receptor agonists

  2005cited by this paper
• Pharmacokinetics, Tolerability, and Safety of Aripiprazole following Multiple Oral Dosing in Normal Healthy Volunteers

  2004cited by this paper
• Functional selectivity of dopamine receptor agonists. I. Selective activation of postsynaptic dopamine D2 receptors linked to adenylate cyclase.

  2002cited by this paper
• Functional selectivity of dopamine receptor agonists. II. Actions of dihydrexidine in D2L receptor-transfected MN9D cells and pituitary lactotrophs.

  2002cited by this paper
• Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.

  2001cited by this paper
• Characterization of dopaminergic compounds at hD2short, hD4.2 and hD4.7 receptors in agonist-stimulated [35S]GTPγS binding assays

  2000cited by this paper
• Enhanced morphine analgesia in mice lacking beta-arrestin 2.

  1999cited by this paper
• Clozapine and other 5-hydroxytryptamine-2A receptor antagonists alter the subcellular distribution of 5-hydroxytryptamine-2A receptors in vitro and in vivo.

  1999cited by this paper
• Interactions of the Novel Antipsychotic Aripiprazole (OPC-14597) with Dopamine and Serotonin Receptor Subtypes

  1999cited by this paper
• Beta-arrestin-dependent formation of beta2 adrenergic receptor-Src protein kinase complexes.

  1999cited by this paper
• Novel antipsychotic agents with dopamine autoreceptor agonist properties: synthesis and pharmacology of 7-[4-(4-phenyl-1-piperazinyl)butoxy]-3,4-dihydro-2(1H)-quinolinone derivatives.

  1998cited by this paper
• Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: evidence for agonist-directed trafficking of receptor stimulus.

  1998influential reference
• Serotonergic Antagonist Effects on Trafficking of Serotonin 5‐HT2A Receptors in Vitro and in Vivo a

  1998cited by this paper
• NMR Chemical Shifts of Common Laboratory Solvents as Trace Impurities.

  1997cited by this paper
• N-arylpiperazinyl-N'-propylamino derivatives of heteroaryl amides as functional uroselective alpha 1-adrenoceptor antagonists.

  1997cited by this paper
• 8,9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: A Potent Full Dopamine D1 Agonist Containing a Rigid β-Phenyldopamine Pharmacophore

  1996cited by this paper
• Rapid agonist-induced internalization of the 5-hydroxytryptamine2A receptor occurs via the endosome pathway in vitro.

  1996cited by this paper
• 9-Dihydroxy-2,3,7,11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: a potent full dopamine D1 agonist containing a rigid-beta-phenyldopamine pharmacophore.

  1996cited by this paper
• Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands.

  1994cited by this paper
• Inverse agonist activity of beta-adrenergic antagonists.

  1994cited by this paper
• Activity of aromatic substituted phenylpiperazines lacking affinity for dopamine binding sites in a preclinical test of antipsychotic efficacy.

  1989cited by this paper
• 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.

  1988cited by this paper
• Studies on 2(1H)-quinolinone derivatives as neuroleptic agents I. Synthesis and biological activities of (4-phenyl-1-piperazinyl)-propoxy-2(1H)-quinolinone derivatives.

  1988cited by this paper
• Multiple mechanisms of serotonergic signal transduction.

  1987cited by this paper
• 2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 1.

  1987cited by this paper
• Evidence that LY-141865 specifically stimulates the D-2 dopamine receptor

  1981cited by this paper
• Long-term antidepressant treatment decreases spiroperidol-labeled serotonin receptor binding.

  1980cited by this paper

• Receptor dimers and biased ligands: Novel strategies for targeting G protein-coupled receptors.

  2025cites this paper
• A hydrogenative oxidation strategy for the single-step synthesis of lactams from N-heteroarenes using water

  2025cites this paper
• Biased Allosteric Modulation in GPCR Drug Discovery.

  2025cites this paper
• Molecular Glues: A New Approach to Modulating GPCR Signaling Bias

  2025cites this paper
• Therapeutic exploration of biased ligands at class A G protein-coupled receptors over the past 20 years.

  2025cites this paper
• Exploring Bias in GPCR Signaling and its Implication in Drug Development: A One-Sided Affair.

  2024cites this paper
• The multifaceted functions of β-arrestins and their therapeutic potential in neurodegenerative diseases

  2024cites this paper
• Molecular glues as potential GPCR therapeutics.

  2024cites this paper
• Open Bite Malocclusion Following Aripiprazole Treatment in Children and Adolescents.

  2023cites this paper
• Optical Control of Dopamine D2-like Receptors with Cell-Specific Fast-Relaxing Photoswitches

  2023cites this paper
• The histamine H3 receptor modulates dopamine D2 receptor–dependent signaling pathways and mouse behaviors

  2023cites this paper
• Transformation of a Dopamine D2 Receptor Agonist to Partial Agonists as Novel Antipsychotic Agents.

  2023cites this paper
• Recent Studies on Serotonin 5-HT2A Receptor Antagonists in Medicinal Chemistry: A Last Decades Survey.

  2023cites this paper
• Selective Signal Capture from Multidimensional GPCR Outputs with Biased Agonists: Progress Towards Novel Drug Development

  2022cites this paper
• Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists

  2022cites this paper
• Identification of Novel Dopamine D2 Receptor Ligands—A Combined In Silico/In Vitro Approach

  2022cites this paper
• Recent advances in dopamine D2 receptor ligands in the treatment of neuropsychiatric disorders

  2022cites this paper
• Synthesis, biological evaluation, and molecular docking of novel hydroxyzine derivatives as potential AR antagonists

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  2021cites this paper
• Functionally selective activation of the dopamine receptor D2 is mirrored by the protein expression profiles

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  2021cites this paper
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  2020cites this paper
• Controlling receptor function from the extracellular vestibule of G-protein coupled receptors.

  2020cites this paper
• A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework

  2020cites this paper
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  2019cites this paper
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• The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists.

  2019cites this paper
• Evaluation of SYA16263 as a new potential antipsychotic agent without catalepsy

  2019cites this paper
• Synthesis and biological evaluation of arylpiperazine derivatives as potential anti-prostate cancer agents.

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• Novel and Potent Dopamine D2 Receptor Go-Protein Biased Agonists

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• Misfolding of vasopressin receptors: biased agonist pharmacochaperones as potential therapeutics.

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  2019cites this paper
• Synthesis, biological evaluation and molecular docking of 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs containing the piperazine moiety.

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• A new kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework

  2019cites this paper
• Dopamine D 2 Partial Agonists – Discovery, Evolution, and Therapeutic Potential

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• D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine.

  2019cites this paper
• Biased signaling of G protein coupled receptors (GPCRs): Molecular determinants of GPCR/transducer selectivity and therapeutic potential.

  2019cites this paper
• Biased signalling: from simple switches to allosteric microprocessors

  2018cites this paper
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  2018cites this paper
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  2017cites this paper
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• Biased Agonist Pharmacochaperones: Small Molecules in the Toolbox for Selectively Modulating GPCR Activity

  2017cites this paper
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  2017cites this paper
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• The Treatment of Adult Bipolar Disorder with Aripiprazole: A Systematic Review

  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
• Structural optimization and structure-functional selectivity relationship studies of G protein-biased EP2 receptor agonists.

  2016cites this paper
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  2016cites this paper
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  2016cites this paper
• Biased agonism: An emerging paradigm in GPCR drug discovery.

  2016cites this paper
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  2016cites this paper
• Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.

  2016cites this paper
• Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology.

  2016cites this paper
• β-Arrestin-Dependent Dopaminergic Regulation of Calcium Channel Activity in the Axon Initial Segment.

  2016cites this paper
• NC-IUPHAR REVIEW Dopamine receptors - IUPHAR Review 13

  2015cites this paper
• Selectivity of pharmacological tools: implications for use in cell physiology. A review in the theme: Cell signaling: proteins, pathways and mechanisms.

  2015cites this paper
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  2015cites this paper
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  2015cites this paper
• Molecular determinants of biased agonism at the dopamine D₂ receptor.

  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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