Abstract
The cholinergic activity in the brain is fundamental for cognitive functions. The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Accumulating evidence indicates that both nAChR and mAChRs can modulate the release of several other neurotransmitters, modify the threshold of long-term plasticity, finally improving learning and memory processes. Importantly, the expression, distribution, and/or function of these systems are altered in several neurological diseases. The aim of this review is to discuss our current knowledge on cholinergic receptors and their regulating synaptic functions and neuronal network activities as well as their use as targets for the development of new and clinically useful cholinergic ligands. These new therapies involve the development of novel and more selective cholinergic agonists and allosteric modulators as well as selective cholinesterase inhibitors, which may improve cognitive and behavioral symptoms, and also provide neuroprotection in several brain diseases. The review will focus on two nAChR receptor subtypes found in the mammalian brain and the most commonly targeted in drug discovery programs for neuropsychiatric disorder, the ligands of α4β2 nAChR and α7 nAChRs.
Keywords: Acetylcholine, nicotinic receptors, muscarinic receptors, synaptic plasticity, neurological disease.
Current Pharmaceutical Design
Title:Role of Nicotinic and Muscarinic Receptors on Synaptic Plasticity and Neurological Diseases
Volume: 22 Issue: 14
Author(s): Marco Fuenzalida, Miguel Ángel Pérez and Hugo R. Arias
Affiliation:
Keywords: Acetylcholine, nicotinic receptors, muscarinic receptors, synaptic plasticity, neurological disease.
Abstract: The cholinergic activity in the brain is fundamental for cognitive functions. The modulatory activity of the neurotransmitter acetylcholine (ACh) is mediated by activating a variety of nicotinic acetylcholine receptors (nAChR) and muscarinic acetylcholine receptors (mAChR). Accumulating evidence indicates that both nAChR and mAChRs can modulate the release of several other neurotransmitters, modify the threshold of long-term plasticity, finally improving learning and memory processes. Importantly, the expression, distribution, and/or function of these systems are altered in several neurological diseases. The aim of this review is to discuss our current knowledge on cholinergic receptors and their regulating synaptic functions and neuronal network activities as well as their use as targets for the development of new and clinically useful cholinergic ligands. These new therapies involve the development of novel and more selective cholinergic agonists and allosteric modulators as well as selective cholinesterase inhibitors, which may improve cognitive and behavioral symptoms, and also provide neuroprotection in several brain diseases. The review will focus on two nAChR receptor subtypes found in the mammalian brain and the most commonly targeted in drug discovery programs for neuropsychiatric disorder, the ligands of α4β2 nAChR and α7 nAChRs.
Export Options
About this article
Cite this article as:
Fuenzalida Marco, Pérez Ángel Miguel and Arias R. Hugo, Role of Nicotinic and Muscarinic Receptors on Synaptic Plasticity and Neurological Diseases, Current Pharmaceutical Design 2016; 22 (14) . https://dx.doi.org/10.2174/1381612822666160127112021
DOI https://dx.doi.org/10.2174/1381612822666160127112021 |
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
-
Editorial [Hot topic: Central and Peripheral Metabolic Changes in Neurodegenerative Diseases (Guest Editor: Ana Cristina Rego)]
Current Drug Targets Bridge Between Neuroimmunity and Traumatic Brain Injury
Current Pharmaceutical Design Angiogenic and Vascular Modulation by Extracellular Matrix Cleavage Products
Current Pharmaceutical Design Neurodevelopmental Delay and Intellectual Disability in Pediatric Heart Transplant
Current Psychiatry Reviews The Potential of Secondary Metabolites from Plants as Drugs or Leads Against Protozoan Neglected Diseases – Part I
Current Medicinal Chemistry Nitric Oxide Synthases and Their Natural Inhibitors
Current Enzyme Inhibition Pictorial US, CT and MRI Findings of Common Hepatic Tumours
Current Medical Imaging Antitumor Properties of Natural Compounds and Related Molecules
Recent Patents on Anti-Cancer Drug Discovery Transforming Growth Factor-Beta and the Kidney: What We Know and What We Can Do?
Current Enzyme Inhibition Cytochromes P450 in Brain: Function and Significance
Current Drug Metabolism Oxidative and Nitrosative Stress and Immune-inflammatory Pathways in Patients with Myalgic Encephalomyelitis (ME)/Chronic Fatigue Syndrome (CFS)
Current Neuropharmacology Histopathology, Immunohistochemistry and Molecular Biology of Follicular Epithelium-Derived Pediatric Thyroid Carcinomas
Current Pediatric Reviews Genetics of Chronic Obstructive Pulmonary Disease
Current Respiratory Medicine Reviews Mitochondrial Uncoupler Proteins
Current Enzyme Inhibition Advanced Methods for the Analysis of Testosterone
Current Medicinal Chemistry Importance of Environmental Factors on Production of Computationally- Defined Natural Molecules against COVID-19 Pandemic
Current Topics in Medicinal Chemistry Histone Deacetylase Inhibitors in Cancer Therapy: New Compounds and Clinical Update of Benzamide-Type Agents
Current Topics in Medicinal Chemistry News in the Indications of Direct Oral Anticoagulants According to the American College of Chest Physicians 2016 Guidelines
Current Drug Metabolism Critical Roles of EGFR Family Members in Breast Cancer and Breast Cancer Stem Cells: Targets for Therapy
Current Pharmaceutical Design Inhibition of Cdc42-Interacting Protein 4 (CIP4) Impairs Osteosarcoma Tumor Progression
Current Cancer Drug Targets