Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral …
…, S Jadhav, UN Menon, PN Vinson, JM Rook… - 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 …
[PDF][PDF] Antipsychotic-like effects of M4 positive allosteric modulators are mediated by CB2 receptor-dependent inhibition of dopamine release
…, CK Jones, Z Xiang, CW Lindsley, JM Rook… - Neuron, 2016 - cell.com
Muscarinic receptors represent a promising therapeutic target for schizophrenia, but the
mechanisms underlying the antipsychotic efficacy of muscarinic modulators are not well …
mechanisms underlying the antipsychotic efficacy of muscarinic modulators are not well …
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 …
Activation of M1 and M4 muscarinic receptors as potential treatments for Alzheimer's disease and schizophrenia
…, DL Choi, PJ Conn, JM Rook - … disease and treatment, 2014 - Taylor & Francis
Alzheimer’s disease (AD) and schizophrenia (SZ) are neurological disorders with overlapping
symptomatology, including both cognitive deficits and behavioral disturbances. Current …
symptomatology, including both cognitive deficits and behavioral disturbances. Current …
Metabotropic glutamate receptor 3 activation is required for long-term depression in medial prefrontal cortex and fear extinction
…, CJ Wenthur, Z Xiang, JM Rook… - Proceedings of the …, 2015 - National Acad Sciences
Clinical studies have revealed that genetic variations in metabotropic glutamate receptor 3 (mGlu
3 ) affect performance on cognitive tasks dependent upon the prefrontal cortex (PFC) …
3 ) affect performance on cognitive tasks dependent upon the prefrontal cortex (PFC) …
Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity
JM Rook, MJ Noetzel, WA Pouliot, TM Bridges… - 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 (…
M1-positive allosteric modulators lacking agonist activity provide the optimal profile for enhancing cognition
…, DW Engers, CW Lindsley, JM Rook… - …, 2018 - nature.com
Highly selective positive allosteric modulators (PAMs) of the M 1 subtype of muscarinic
acetylcholine receptor have emerged as an exciting new approach for improving cognitive …
acetylcholine receptor have emerged as an exciting new approach for improving cognitive …
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 M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity
JM Rook, JL Bertron, HP Cho… - ACS chemical …, 2018 - ACS Publications
Selective activation of the M 1 subtype of muscarinic acetylcholine receptor, via positive
allosteric modulation (PAM), is an exciting strategy to improve cognition in schizophrenia and …
allosteric modulation (PAM), is an exciting strategy to improve cognition in schizophrenia and …