Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors

Development of a High-Throughput Screening–Compatible Cell-Based Functional Assay to Identify Small Molecule Probes of the Galanin 3 Receptor (GalR3)

(2013) James Robinson et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

Functional Selectivity of 6′-Guanidinonaltrindole (6′-GNTI) at κ-Opioid Receptors in Striatal Neurons

(2013) Cullen L. Schmid et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

(2013) Terry Kenakin et al.   NATURE REVIEWS DRUG DISCOVERY

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy

(2012) Kevin J. Frankowski et al.   ACS Chemical Neuroscience

6′-Guanidinonaltrindole (6′-GNTI) Is a G Protein-biased κ-Opioid Receptor Agonist That Inhibits Arrestin Recruitment

(2012) Marie-Laure Rives et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

14-Alkoxy- and 14-Acyloxypyridomorphinans: μ Agonist/δ Antagonist Opioid Analgesics with Diminished Tolerance and Dependence Side Effects

(2012) Subramaniam Ananthan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure of the human κ-opioid receptor in complex with JDTic

(2012) Huixian Wu et al.   NATURE

A Simple Method for Quantifying Functional Selectivity and Agonist Bias

(2011) Terry Kenakin et al.   ACS Chemical Neuroscience

Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors

(2011) Eric Reiter et al.   Annual Review of Pharmacology and Toxicology

β-arrestin-mediated receptor trafficking and signal transduction

(2011) Sudha K. Shenoy et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Quantification of Functional Selectivity at the Human  1A-Adrenoceptor

(2010) B. A. Evans et al.   MOLECULAR PHARMACOLOGY

The Therapeutic Potential of κ-Opioids for Treatment of Pain and Addiction

(2010) Charles Chavkin   NEUROPSYCHOPHARMACOLOGY

Kinase cascades and ligand-directed signaling at the kappa opioid receptor

(2010) Michael R. Bruchas et al.   PSYCHOPHARMACOLOGY

N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: Selective and Nonbasic κ-Opioid Receptor Ligands

(2010) Kevin J. Frankowski et al.   ACS Medicinal Chemistry Letters

Dynorphin, stress, and depression

(2009) Allison T. Knoll et al.   BRAIN RESEARCH

Morphine-induced physiological and behavioral responses in mice lacking G protein-coupled receptor kinase 6

(2009) Kirsten M. Raehal et al.   DRUG AND ALCOHOL DEPENDENCE

Kappa opioids promote the proliferation of astrocytes via Gβγ and β-arrestin 2-dependent MAPK-mediated pathways

(2008) Gregory P. McLennan et al.   JOURNAL OF NEUROCHEMISTRY

The Dysphoric Component of Stress Is Encoded by Activation of the Dynorphin  -Opioid System

(2008) B. B. Land et al.   JOURNAL OF NEUROSCIENCE

Repeated swim stress induces kappa opioid-mediated activation of extracellular signal-regulated kinase 1/2

(2008) Michael R. Bruchas et al.   NEUROREPORT

Physiological and pharmacological implications of beta-arrestin regulation

(2008) Cullen L. Schmid et al.   PHARMACOLOGY & THERAPEUTICS