Relationship between In Vivo Receptor Occupancy and Efficacy of Metabotropic Glutamate Receptor Subtype 5 Allosteric Modulators with Different In Vitro Binding Profiles

Identification of Specific Ligand–Receptor Interactions That Govern Binding and Cooperativity of Diverse Modulators to a Common Metabotropic Glutamate Receptor 5 Allosteric Site

(2014) Karen J. Gregory et al.   ACS Chemical Neuroscience

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

(2014) Andrew S. Doré et al.   NATURE

Opportunities and challenges in the discovery of allosteric modulators of GPCRs for treating CNS disorders

(2014) P. Jeffrey Conn et al.   NATURE REVIEWS DRUG DISCOVERY

Structure of a Class C GPCR Metabotropic Glutamate Receptor 1 Bound to an Allosteric Modulator

(2014) H. Wu et al.   SCIENCE

Discovery of VU0409106: A negative allosteric modulator of mGlu5 with activity in a mouse model of anxiety

(2013) Andrew S. Felts et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

mGlu5negative allosteric modulators: a patent review (2010 – 2012)

(2013) Kyle A Emmitte   EXPERT OPINION ON THERAPEUTIC PATENTS

18F-FPEB, a PET Radiopharmaceutical for Quantifying Metabotropic Glutamate 5 Receptors: A First-in-Human Study of Radiochemical Safety, Biokinetics, and Radiation Dosimetry

(2013) D. F. Wong et al.   JOURNAL OF NUCLEAR MEDICINE

Palladium mediated 11C-cyanation and characterization in the non-human primate brain of the novel mGluR5 radioligand [11C]AZD9272

(2013) Jan D. Andersson et al.   NUCLEAR MEDICINE AND BIOLOGY

Unique Signaling Profiles of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Determine Differences in In Vivo Activity

(2012) Jerri M. Rook et al.   BIOLOGICAL PSYCHIATRY

Radioligands for the PET Imaging of Metabotropic Glutamate Receptor Subtype 5 (mGluR5)

(2012) Linjing Mu et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

PET and SPECT tracers for glutamate receptors

(2012) Vattoly J. Majo et al.   DRUG DISCOVERY TODAY

Synthesis and SAR of centrally active mGlu5 positive allosteric modulators based on an aryl acetylenic bicyclic lactam scaffold

(2011) Richard Williams et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

AFQ056 treatment of levodopa-induced dyskinesias: Results of 2 randomized controlled trials

(2011) Daniela Berg et al.   MOVEMENT DISORDERS

Epigenetic Modification of the FMR1 Gene in Fragile X Syndrome Is Associated with Differential Response to the mGluR5 Antagonist AFQ056

(2011) S. Jacquemont et al.   Science Translational Medicine

Discovery of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Reveals Chemical and Functional Diversity and In Vivo Activity in Rat Behavioral Models of Anxiolytic and Antipsychotic Activity

(2010) A. L. Rodriguez et al.   MOLECULAR PHARMACOLOGY

The State of Innovation in Drug Development

(2008) I Kola   CLINICAL PHARMACOLOGY & THERAPEUTICS

Radiodefluorination of 3-Fluoro-5-(2-(2-[18F](fluoromethyl)-thiazol-4-yl)ethynyl)benzonitrile ([18F]SP203), a Radioligand for Imaging Brain Metabotropic Glutamate Subtype-5 Receptors with Positron Emission Tomography, Occurs by Glutathionylation in Rat Brain

(2008) H. U. Shetty et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia

(2008) P. Jeffrey Conn et al.   TRENDS IN PHARMACOLOGICAL SCIENCES