ReviewDrug discovery today2013
Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.
Review in Drug discovery today, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 67 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
67 citing papers in PubMed, 121 citations in OpenAlex.
- Safety, tolerability, pharmacokinetic and pharmacodynamic effects of the muscarinic MAlzheimer's research & therapy · 2025Trial
- Safety, pharmacokinetics and pharmacodynamics of HTL0009936, a selective muscarinic MBritish journal of clinical pharmacology · 2021Trial
- Article
- Discovery of VU6052254: A Novel, Potent MACS chemical neuroscience · 2025Article
- Exploring GPR120/FFAR4 pharmacology: Unveiling novel therapeutic avenues through molecular signaling pathways for Alzheimer's disease intervention.Brain, behavior, & immunity - health · 2025Review
- Alzheimer's Disease Etiology Hypotheses and Therapeutic Strategies: A Perspective.International journal of molecular sciences · 2025Review
- Application of Deuterium in an MACS chemical neuroscience · 2025Article
- Control of cortical slow oscillations and epileptiform discharges with photoswitchable type 1 muscarinic ligands.PNAS nexus · 2025Article
- Discovery of VU0467319: an MACS chemical neuroscience · 2025Article
- The novel orthosteric agonist M1 muscarinic acetylcholine receptor reveals anti-Alzheimer's disease activity.Scientific reports · 2024Article
- Discovery of VU6007496: Challenges in the Development of an MACS chemical neuroscience · 2024Article
- What Remains to Be Discovered in Schizophrenia Therapeutics: Contributions by Advancing the Molecular Mechanisms of Drugs for Psychosis and Schizophrenia.Biomolecules · 2024Review
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- The effects of clinical and pharmacological factors on the ratio of clozapine to norclozapine in psychiatric patients.Frontiers in pharmacology · 2024Article
- Cross-diagnostic determinants of cognitive functioning: the muscarinic cholinergic receptor as a model system.Translational psychiatry · 2023Review
- Current Status of Oligonucleotide-Based Protein Degraders.Pharmaceutics · 2023Review
- Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders.Biomedicines · 2022Review
- A computational lens on menopause-associated psychosis.Frontiers in psychiatry · 2022Article
- Biased M1 muscarinic receptor mutant mice show accelerated progression of prion neurodegenerative disease.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor MBioorganic & medicinal chemistry letters · 2021Article
7 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Allosteric modulation of AMPA, NR2B, mGlu2, mGlu5 and M1, targeting glutamatergic dysfunction, represents a significant area of research for the treatment of schizophrenia. Of these targets, clinical promise has been demonstrated using muscarinic activators for the treatment of Alzheimer's disease (AD) and schizophrenia. These diseases have inspired researchers to determine the effects of modulating cholinergic transmission in the forebrain, which is primarily regulated by one of five subtypes of muscarinic acetylcholine receptor (mAChR), a subfamily of G-protein-coupled receptors (GPCRs). Of these five subtypes, M1 is highly expressed in brain regions responsible for learning, cognition and memory. Xanomeline, an orthosteric muscarinic agonist with modest selectivity, was one of the first compounds that displayed improvements in behavioral disturbances in AD patients and efficacy in schizophrenics. Since these initial clinical results, many scientists, including those in our laboratories, have strived to elucidate the role of M1 with compounds that display improved selectivity for this receptor by targeting allosteric modes of receptor activation. A survey of selected compounds in this area will be presented.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.