Abstract
Neuronal nicotinic receptors (nAChRs) are a heterogeneous family of ion channels differently expressed in the nervous system where, by responding to the endogenous neurotransmitter acetylcholine, they contribute to a wide range of brain activities and influence a number of physiological functions. Over recent years, the application of newly developed molecular and cellular biological techniques has made it possible to correlate the subunit composition of nAChRs with specific nicotine-elicited behaviours, and refine some of the in vivo physiological functions of nAChR subtypes. The major new findings are the widespread expression of nAChRs, outside the nervous system, their specific and complex organisation, and their relevance to normal brain function. Moreover, the combination of clinical and basic research has better defined the involvement of nAChRs in a growing number of nervous pathologies other than degenerative diseases. However, there are still only a limited number of nicotinic-specific drugs and, although some nicotinic agonists have an interesting pharmacology, their clinical use is limited by undesirable side effects. Some selective nicotinic ligands have recently been developed and used to explore the complexity of nAChR subtype structure and function in the expectation that they will become rational therapeutic alternatives in a number of neurodegenerative, neuropsychiatric and neurological disorders. In this review, we will discuss the molecular basis of brain nAChR structural and functional diversity mainly in pharmacological and biochemical terms, and summarise current knowledge concerning the newly discovered drugs used to classify the numerous receptor subtypes and treat the brain diseases in which nAChRs are involved.
Keywords: Neuronal nicotinic receptors, molecular structure, knock-out mice, knock-in mice, toxins, nicotinic drugs, upregulation, nAChRs in pathology
Current Pharmaceutical Design
Title: Brain Neuronal Nicotinic Receptors as New Targets for Drug Discovery
Volume: 12 Issue: 4
Author(s): C. Gotti, L. Riganti, S. Vailati and F. Clementi
Affiliation:
Keywords: Neuronal nicotinic receptors, molecular structure, knock-out mice, knock-in mice, toxins, nicotinic drugs, upregulation, nAChRs in pathology
Abstract: Neuronal nicotinic receptors (nAChRs) are a heterogeneous family of ion channels differently expressed in the nervous system where, by responding to the endogenous neurotransmitter acetylcholine, they contribute to a wide range of brain activities and influence a number of physiological functions. Over recent years, the application of newly developed molecular and cellular biological techniques has made it possible to correlate the subunit composition of nAChRs with specific nicotine-elicited behaviours, and refine some of the in vivo physiological functions of nAChR subtypes. The major new findings are the widespread expression of nAChRs, outside the nervous system, their specific and complex organisation, and their relevance to normal brain function. Moreover, the combination of clinical and basic research has better defined the involvement of nAChRs in a growing number of nervous pathologies other than degenerative diseases. However, there are still only a limited number of nicotinic-specific drugs and, although some nicotinic agonists have an interesting pharmacology, their clinical use is limited by undesirable side effects. Some selective nicotinic ligands have recently been developed and used to explore the complexity of nAChR subtype structure and function in the expectation that they will become rational therapeutic alternatives in a number of neurodegenerative, neuropsychiatric and neurological disorders. In this review, we will discuss the molecular basis of brain nAChR structural and functional diversity mainly in pharmacological and biochemical terms, and summarise current knowledge concerning the newly discovered drugs used to classify the numerous receptor subtypes and treat the brain diseases in which nAChRs are involved.
Export Options
About this article
Cite this article as:
Gotti C., Riganti L., Vailati S. and Clementi F., Brain Neuronal Nicotinic Receptors as New Targets for Drug Discovery, Current Pharmaceutical Design 2006; 12 (4) . https://dx.doi.org/10.2174/138161206775474486
DOI https://dx.doi.org/10.2174/138161206775474486 |
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
-
Biologic Therapy in Psoriasis: Safety Profile
Current Drug Safety Anti-Respiratory Syncytial Virus Mechanism of <i>Houttuynia cordata</i> Thunb Exploration based on Network Pharmacology
Combinatorial Chemistry & High Throughput Screening Antioxidants and its Properties as Affected by Extrusion Process: A Review
Recent Patents on Food, Nutrition & Agriculture Air Pollution, Platelet Activation and Atherosclerosis
Inflammation & Allergy - Drug Targets (Discontinued) Flt3 Receptor Tyrosine Kinase as a Drug Target in Leukemia
Current Pharmaceutical Design Inhibitors of Nitric Oxide Synthase: What's up and What's Next?
Current Enzyme Inhibition Good Practice in Umbilical Cord Blood Collection in Order to Identify Suitable Units Before Cryopreservation
Letters in Drug Design & Discovery Antigenic Peptide Vaccination: Provoking Immune Response and Clinical Benefit for Cancer
Current Immunology Reviews (Discontinued) Current Biological Therapies for Inflammatory Bowel Disease
Current Pharmaceutical Design Targeting Ion Channels in Leukemias: A New Challenge for Treatment
Current Medicinal Chemistry p38 MAP Kinase Inhibitors as Potential Therapeutic Drugs for Neural Diseases
Central Nervous System Agents in Medicinal Chemistry Pathophysiogenesis of Mesial Temporal Lobe Epilepsy: Is Prevention of Damage Antiepileptogenic?
Current Medicinal Chemistry Aqueous Extract of <i>Cola nitida</i> and <i>Garcinia kola</i> Synergistically Enhances Hippocampal-hypothalamic Glutamate and Na+ /K+ -ATPase Activity in Male Wistar Rats
Current Drug Discovery Technologies Pregnancy, Programming and Preeclampsia: Gap Junctions at the Nexus of Pregnancy-induced Adaptation of Endothelial Function and Endothelial Adaptive Failure in PE
Current Vascular Pharmacology Melatonin Leads to Axonal Regeneration, Reduction in Oxidative Stress, and Improved Functional Recovery Following Sciatic Nerve Injury
Current Neurovascular Research Teenage-Pregnancies - A Biomedical and a Sociocultural Approach to a Current Problem
Current Women`s Health Reviews Melatonin and Aromatase in Breast Cancer
Clinical Cancer Drugs Technological Prospecting: Mapping Patents on L-asparaginases from Extremophilic Microorganisms
Recent Patents on Biotechnology Effects of Verbascoside Administration on the Blood Parameters and Oxidative Status in Jennies and Their Suckling Foals: Potential Improvement of Milk for Human Use
Endocrine, Metabolic & Immune Disorders - Drug Targets The Role of Proteomics in Osteoarthritis Pathogenesis Research
Current Drug Targets