Structure–Functional Selectivity Relationship Studies of β-Arrestin-Biased Dopamine D 2 Receptor Agonists (original) (raw)
Discovery of β-Arrestin–Biased Dopamine D 2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy
William Wetsel
Proceedings of the National Academy of Sciences, 2011
View PDFchevron_right
D2 Dopamine Receptor G Protein-Biased Partial Agonists Based on Cariprazine
William Wetsel
Journal of Medicinal Chemistry, 2019
View PDFchevron_right
Synthesis and characterization of selective dopamine D2 receptor ligands using aripiprazole as the lead compound
Robert Mach
Bioorganic Medicinal Chemistry, 2011
View PDFchevron_right
Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties
William Wetsel
Proceedings of the National Academy of Sciences of the United States of America, 2016
View PDFchevron_right
A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor
Anh Thơ Nguyen
Journal of Medicinal Chemistry, 2013
View PDFchevron_right
Discovery and Characterization of a G Protein-biased Agonist that Inhibits -arrestin Recruitment to the D2 Dopamine Receptor
Adrian Padron
Molecular Pharmacology, 2014
View PDFchevron_right
Dopamine D4 Receptor-Selective Compounds Reveal Structure–Activity Relationships that Engender Agonist Efficacy
Russell Burkhardt
Journal of Medicinal Chemistry, 2019
View PDFchevron_right
Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors
Perry Molinoff
Journal of Pharmacology and Experimental Therapeutics, 2002
View PDFchevron_right
Antagonism of dopamine D2 receptor/ -arrestin 2 interaction is a common property of clinically effective antipsychotics
Michael Didriksen
Proceedings of the National Academy of Sciences, 2008
View PDFchevron_right
Bias analyses of preclinical and clinical d2 dopamine ligands: studies with immediate and complex signaling pathways
Val Watts
The Journal of pharmacology and experimental therapeutics, 2015
View PDFchevron_right
Antipsychotic-Like Efficacy of Dopamine D2 Receptor-Biased Ligands is Dependent on Adenosine A2A Receptor Expression
Maricel Gómez-soler
Molecular Neurobiology, 2017
View PDFchevron_right
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 D2 Receptor
François Noël
Frontiers in Pharmacology, 2019
View PDFchevron_right
Dopamine D 2 receptor partial agonists display differential or contrasting characteristics in membrane and cell-based assays of dopamine D 2 receptor signaling
Shaun Jordan
Progress in Neuro-psychopharmacology & Biological Psychiatry, 2007
View PDFchevron_right
Functionally biased D2R antagonists: Targeting the β-arrestin pathway to improve antipsychotic treatment
Michelle Palmer
ACS chemical biology, 2018
View PDFchevron_right
Dopamine Receptor Ligand Selectivity—An In Silico/In Vitro Insight
Daniela Schuster
Biomedicines
View PDFchevron_right
Receptor reserve-dependent properties of antipsychotics at human dopamine D2 receptors
Robert McQuade
European Journal of Pharmacology, 2009
View PDFchevron_right
Discovery, Optimization, and Characterization of Novel D2 Dopamine Receptor Selective Antagonists
Joseph Steiner
Journal of Medicinal Chemistry, 2014
View PDFchevron_right
Beyond small-molecule sar: Using the dopamine d3 receptor crystal structure to guide drug design
Thomas M. Keck
2014
View PDFchevron_right
Characterization of aripiprazole partial agonist activity at human dopamine D3 receptors
Robert McQuade
European Journal of Pharmacology, 2008
View PDFchevron_right
Active-State Model of a Dopamine D2 Receptor - Gαi Complex Stabilized by Aripiprazole-Type Partial Agonists
Nuska Tschammer
PLoS ONE, 2014
View PDFchevron_right
Aripiprazole has Functionally Selective Actions at Dopamine D2 Receptor-Mediated Signaling Pathways
Richard Mailman
Neuropsychopharmacology, 2007
View PDFchevron_right
Identification of a Tool Compound to Study the Mechanisms of Functional Selectivity between D2 and D3 Dopamine Receptors
Abdelouahid Samadi
ACS Omega
View PDFchevron_right
New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling
Val Watts
Biochemical Pharmacology, 2015
View PDFchevron_right
Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands
Ferran Sanz
Bioorganic & Medicinal Chemistry Letters, 2009
View PDFchevron_right
Structure−Activity Relationships for a Novel Series of Dopamine D2-like Receptor Ligands Based on N-Substituted 3-Aryl-8-azabicyclo[3.2.1]octan-3-ol
Jonathan Katz
Journal of Medicinal Chemistry, 2008
View PDFchevron_right
Synthesis, Molecular Properties Estimations, and Dual Dopamine D2 and D3 Receptor Activities of Benzothiazole-Based Ligands
Bassem S H A B A N Sadek
Frontiers in Chemistry
View PDFchevron_right
Ligand with Two Modes of Interaction with the Dopamine D2 Receptor–An Induced-Fit Mechanism of Insurmountable Antagonism
Kristoffer Sahlholm
ACS Chemical Neuroscience
View PDFchevron_right
Interactions of the Novel Antipsychotic Aripiprazole (OPC14597) with Dopamine and Serotonin Receptor Subtypes
John Schetz, Richard Mailman
Neuropsychopharmacology, 1999
View PDFchevron_right
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure
steve watson
Bioorganic & Medicinal Chemistry Letters, 2010
View PDFchevron_right
Role of the extracellular amino terminus and first membrane-spanning helix of dopamine D1 and D5 receptors in shaping ligand selectivity and efficacy
Mario Tiberi
Cellular Signalling, 2010
View PDFchevron_right