Abstract
One of the consistent findings in the brains of Alzheimers Disease (AD) patients is loss of cholinergic function. The cholinergic approach to treatment of AD involves counteracting this loss in cholinergic activity by pharmacological intervention to increase cholinergic transmission. The cognitive effects of acetylcholine are mediated via the muscarinic M1 receptor. Direct stimulation of this receptor using muscarinic M1 agonists improves cognition in animal models and improves performance in cognitive tests in Alzheimers patients. Alternatively, antagonists of central presynaptic M2 receptors improves cognition by increasing the central release of acetylcholine. Both approaches require high selectivity for one muscarinic receptor sub-type both for efficacy and to avoid cholinergic side effects. In this review summarizes recent progress in the identification and characterization of selective muscarinic receptor ligands for the treatment of Alzheimers disease.
Keywords: alzheimers disease, cognition, muscarinic receptor
Current Pharmaceutical Design
Title: Muscarinic Receptor Agonists and Antagonists in the Treatment of Alzheimers Disease
Volume: 11 Issue: 26
Author(s): J. W. Clader and Y. Wang
Affiliation:
Keywords: alzheimers disease, cognition, muscarinic receptor
Abstract: One of the consistent findings in the brains of Alzheimers Disease (AD) patients is loss of cholinergic function. The cholinergic approach to treatment of AD involves counteracting this loss in cholinergic activity by pharmacological intervention to increase cholinergic transmission. The cognitive effects of acetylcholine are mediated via the muscarinic M1 receptor. Direct stimulation of this receptor using muscarinic M1 agonists improves cognition in animal models and improves performance in cognitive tests in Alzheimers patients. Alternatively, antagonists of central presynaptic M2 receptors improves cognition by increasing the central release of acetylcholine. Both approaches require high selectivity for one muscarinic receptor sub-type both for efficacy and to avoid cholinergic side effects. In this review summarizes recent progress in the identification and characterization of selective muscarinic receptor ligands for the treatment of Alzheimers disease.
Export Options
About this article
Cite this article as:
Clader W. J. and Wang Y., Muscarinic Receptor Agonists and Antagonists in the Treatment of Alzheimers Disease, Current Pharmaceutical Design 2005; 11 (26) . https://dx.doi.org/10.2174/138161205774370762
DOI https://dx.doi.org/10.2174/138161205774370762 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
From Treatment Adherence to Advanced Shared Decision Making: New Professional Strategies and Attitudes in Mental Health Care
Current Clinical Pharmacology Emerging Treatment Strategies and Potential Therapeutic Targets in Primary Sjogrens Syndrome
Inflammation & Allergy - Drug Targets (Discontinued) A Therapeutic Paradigm to Appraise the Competence of Chitosan Oligosaccharide Lactate Targeting Monoamine Oxidase-A and PGlycoprotein to Contest Depression by Channeling the Blood Brain Barrier
Current Bioinformatics Conotoxins: Structure, Therapeutic Potential and Pharmacological Applications
Current Pharmaceutical Design Adherence to Anti-Retroviral Therapy in North Central Nigeria
Current HIV Research Chemical Components of Citrus Essential Oils from Brazil
The Natural Products Journal Genetic Interactions Effects of Cardiovascular Disorder Using Computational Models: A Review
Current Biotechnology TRYCAT Pathways Link Peripheral Inflammation, Nicotine, Somatization and Depression in the Etiology and Course of Parkinson’s Disease
CNS & Neurological Disorders - Drug Targets New Psychoactive Substances: A Matter of Time
Current Neuropharmacology Morin Inhibits Ovarian Cancer Growth through the Inhibition of NF-κB Signaling Pathway
Anti-Cancer Agents in Medicinal Chemistry Predictive Molecular Markers of Response to Epidermal Growth Factor Receptor(EGFR) Family-Targeted Therapies
Current Cancer Drug Targets Amyloid β-Peptide: The Inside Story
Current Alzheimer Research Technology-Dependent Children: The Chronically Ventilated Child
Current Pediatric Reviews Neurotrophic Effects of the Peptide NAP: A Novel Neuroprotective Drug Candidate
Current Alzheimer Research How to Manage the Infectious Risk under Anti-TNF in Inflammatory Bowel Disease
Current Drug Targets MMP-2 Selectivity in Hydroxamate-Type Inhibitors
Current Medicinal Chemistry B-Mode Ultrasound Study of Carotid Plaques in HIV-Positive Patients to Detect the Presence of Inflammatory Endothelial Lesions
Current HIV Research A Systematic Review of Drugs in Late-Stage Development for the Treatment of Multiple Sclerosis: A Focus on Oral Synthetic Drugs
Inflammation & Allergy - Drug Targets (Discontinued) The Sirtuin Inhibitor Nicotinamide Enhances Neuronal Cell Survival During Acute Anoxic Injury Through AKT, BAD, PARP, and Mitochondrial Associated "Anti-Apoptotic" Pathways
Current Neurovascular Research Monoclonal Antibodies in the Treatment of Neuroimmunological Diseases
Current Pharmaceutical Design