Metabotropic glutamate receptors as therapeutic targets for schizophrenia
PN Vinson, PJ Conn - Neuropharmacology, 2012 - Elsevier
Treatment options for schizophrenia that address all symptom categories (positive, negative,
and cognitive) are lacking in current therapies for this disorder. Compounds targeting the …
and cognitive) are lacking in current therapies for this disorder. Compounds targeting the …
Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral …
…, TN Blatt, S Jadhav, UN Menon, PN Vinson… - Molecular …, 2010 - ASPET
Modulators of metabotropic glutamate receptor subtype 5 (mGluR5) may provide novel
treatments for multiple central nervous system (CNS) disorders, including anxiety and …
treatments for multiple central nervous system (CNS) disorders, including anxiety and …
[PDF][PDF] Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents
Schizophrenia is associated with disruptions in N-methyl-D-aspartate glutamate receptor
subtype (NMDAR)-mediated excitatory synaptic signaling. The metabotropic glutamate …
subtype (NMDAR)-mediated excitatory synaptic signaling. The metabotropic glutamate …
Functional impact of allosteric agonist activity of selective positive allosteric modulators of metabotropic glutamate receptor subtype 5 in regulating central nervous …
MJ Noetzel, JM Rook, PN Vinson, HP Cho, E Days… - Molecular …, 2012 - ASPET
Positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGlu 5
) have emerged as an exciting new approach for the treatment of schizophrenia and other …
) have emerged as an exciting new approach for the treatment of schizophrenia and other …
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity
…, MJ Noetzel, WA Pouliot, TM Bridges, PN Vinson… - Biological …, 2013 - Elsevier
BACKGROUND: Metabotropic glutamate receptor subtype 5 (mGlu 5 ) activators have
emerged as a novel approach to the treatment of schizophrenia. Positive allosteric modulators (…
emerged as a novel approach to the treatment of schizophrenia. Positive allosteric modulators (…
Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity …
KJ Gregory, MJ Noetzel, JM Rook, PN Vinson… - Molecular …, 2012 - ASPET
Drug discovery programs increasingly are focusing on allosteric modulators as a means to
modify the activity of G protein-coupled receptor (GPCR) targets. Allosteric binding sites are …
modify the activity of G protein-coupled receptor (GPCR) targets. Allosteric binding sites are …
A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling
MJ Noetzel, KJ Gregory, PN Vinson, JT Manka… - Molecular …, 2013 - ASPET
Metabotropic glutamate receptor 5 (mGlu 5 ) is a target for the treatment of central nervous
system (CNS) disorders, such as schizophrenia and Alzheimer’s disease. Furthermore, mGlu …
system (CNS) disorders, such as schizophrenia and Alzheimer’s disease. Furthermore, mGlu …
Approaches for probing allosteric interactions at 7 transmembrane spanning receptors
MT Klein, PN Vinson, CM Niswender - Progress in molecular biology and …, 2013 - Elsevier
… Shown are data collected during a thallium flux assay in hM 4 muscarinic receptor/GIRK-HEK
cell line (PN Vinson, previously unpublished data). The M 4 PAM, VU0152100, was added …
cell line (PN Vinson, previously unpublished data). The M 4 PAM, VU0152100, was added …
Discovery of N-(4-methoxy-7-methylbenzo [d] thiazol-2-yl) isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the …
JM Salovich, PN Vinson, DJ Sheffler, A Lamsal… - Bioorganic & medicinal …, 2012 - Elsevier
Herein we describe the discovery and development of a novel class of M 4 positive allosteric
modulators, culminating in the discovery of ML293. ML293 exhibited modest potency at the …
modulators, culminating in the discovery of ML293. ML293 exhibited modest potency at the …
[HTML][HTML] Screening for AMPA receptor auxiliary subunit specific modulators
CM Azumaya, EL Days, PN Vinson, S Stauffer… - PLoS …, 2017 - journals.plos.org
AMPA receptors (AMPAR) are ligand gated ion channels critical for synaptic transmission
and plasticity. Their dysfunction is implicated in a variety of psychiatric and neurological …
and plasticity. Their dysfunction is implicated in a variety of psychiatric and neurological …