[HTML][HTML] Allosteric modulation of GPCRs: new insights and potential utility for treatment of schizophrenia and other CNS disorders

DJ Foster, PJ Conn - Neuron, 2017 - cell.com
G-protein-coupled receptors (GPCRs) play critical roles in regulating brain function. Recent
advances have greatly expanded our understanding of these receptors as complex …

Large-scale functional connectivity networks in the rodent brain

A Gozzi, AJ Schwarz - Neuroimage, 2016 - Elsevier
Abstract Resting-state functional Magnetic Resonance Imaging (rsfMRI) of the human brain
has revealed multiple large-scale neural networks within a hierarchical and complex …

Emraclidine, a novel positive allosteric modulator of cholinergic M4 receptors, for the treatment of schizophrenia: a two-part, randomised, double-blind, placebo …

JH Krystal, JM Kane, CU Correll, DP Walling, M Leoni… - The Lancet, 2022 - thelancet.com
Background Emraclidine is a novel, brain-penetrant, highly selective M4 receptor positive
allosteric modulator in development for the treatment of schizophrenia. We aimed to …

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

PJ Conn, CW Lindsley, J Meiler… - Nature reviews Drug …, 2014 - nature.com
Novel allosteric modulators of G protein-coupled receptors (GPCRs) are providing
fundamental advances in the development of GPCR ligands with high subtype selectivity …

Targeting muscarinic acetylcholine receptors for the treatment of psychiatric and neurological disorders

SP Moran, J Maksymetz, PJ Conn - Trends in pharmacological sciences, 2019 - cell.com
Muscarinic acetylcholine receptors (mAChR) play important roles in regulating complex
behaviors such as cognition, movement, and reward, making them ideally situated as …

Targeting muscarinic receptors to treat schizophrenia

DJ Foster, ZK Bryant, PJ Conn - Behavioural brain research, 2021 - Elsevier
Schizophrenia is a severe neuropsychiatric disorder characterized by a diverse range of
symptoms that can have profound impacts on the lives of patients. Currently available …

Antipsychotic-like effects of M4 positive allosteric modulators are mediated by CB2 receptor-dependent inhibition of dopamine release

DJ Foster, JM Wilson, DH Remke, MS Mahmood… - 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 …

Selective Activation of M4 Muscarinic Acetylcholine Receptors Reverses MK-801-Induced Behavioral Impairments and Enhances Associative Learning in Rodents

M Bubser, TM Bridges, D Dencker… - ACS chemical …, 2014 - ACS Publications
Positive allosteric modulators (PAMs) of the M4 muscarinic acetylcholine receptor (mAChR)
represent a novel approach for the treatment of psychotic symptoms associated with …

Fine tuning muscarinic acetylcholine receptor signaling through allostery and bias

ET Van der Westhuizen, KHC Choy, C Valant… - Frontiers in …, 2021 - frontiersin.org
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug
targets for neurological diseases, in particular for Alzheimer's disease and schizophrenia …

Cell-type-specific translation profiling reveals a novel strategy for treating fragile X syndrome

SR Thomson, SS Seo, SA Barnes, SR Louros… - Neuron, 2017 - cell.com
Excessive mRNA translation downstream of group I metabotropic glutamate receptors (mGlu
1/5) is a core pathophysiology of fragile X syndrome (FX); however, the differentially …