Abstract
Homomeric α7 nicotinic acetylcholine receptors (nAChRs) are implicated in the regulation of cognitive processes such as memory and attention and have potential as therapeutic targets for the treatment of the cognitive deficits associated with schizophrenia. Though numerous α7 nAChR agonists have been developed, and several have progressed to clinical trials, these are derived from few common chemotypes. Consequently, many of these α7 nAChR clinical candidates share unfavorable side-effect profile. SEN12333 represents a novel chemotype for the development of α7 nAChR agonists, and exploration of this scaffold has produced structurally diverse ligands with promising pharmacological properties. This review will summarize structure-affinity and -activity relationships surrounding analogs of SEN12333.
Keywords: Nicotinic receptors, schizophrenia, Alzheimer’s disease, SEN12333.
Current Pharmaceutical Design
Title:The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases
Volume: 22 Issue: 14
Author(s): Corinne Beinat, Samuel D. Banister, Marco Herrera and Michael Kassiou
Affiliation:
Keywords: Nicotinic receptors, schizophrenia, Alzheimer’s disease, SEN12333.
Abstract: Homomeric α7 nicotinic acetylcholine receptors (nAChRs) are implicated in the regulation of cognitive processes such as memory and attention and have potential as therapeutic targets for the treatment of the cognitive deficits associated with schizophrenia. Though numerous α7 nAChR agonists have been developed, and several have progressed to clinical trials, these are derived from few common chemotypes. Consequently, many of these α7 nAChR clinical candidates share unfavorable side-effect profile. SEN12333 represents a novel chemotype for the development of α7 nAChR agonists, and exploration of this scaffold has produced structurally diverse ligands with promising pharmacological properties. This review will summarize structure-affinity and -activity relationships surrounding analogs of SEN12333.
Export Options
About this article
Cite this article as:
Beinat Corinne, Banister D. Samuel, Herrera Marco and Kassiou Michael, The Recent Development of α7 Nicotinic Acetylcholine Receptor (nAChR) Ligands as Therapeutic Candidates for the Treatment of Central Nervous System (CNS) Diseases, Current Pharmaceutical Design 2016; 22 (14) . https://dx.doi.org/10.2174/1381612822666160127114125
DOI https://dx.doi.org/10.2174/1381612822666160127114125 |
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
-
Heteromerization of G Protein-Coupled Receptors: Relevance to Neurological Disorders and Neurotherapeutics
CNS & Neurological Disorders - Drug Targets Shutting Down the Furnace: Preferential Killing of Cancer Cells with Mitochondrial-Targeting Molecules
Current Medicinal Chemistry B7-H3 Immune Checkpoint Protein in Human Cancer
Current Medicinal Chemistry Hsp20 Protects Neuroblastoma Cells from Ischemia/Reperfusion Injury by Inhibition of Apoptosis via a Mechanism that Involves the Mitochondrial Pathways
Current Neurovascular Research The Role for Oxidative Stress in Aberrant DNA Methylation in Alzheimer’s Disease
Current Alzheimer Research Molecular and Cellular Mechanisms for Alzheimers Disease:Understanding APP Metabolism
Current Molecular Medicine Neuroinflammation: A Therapeutic Target of Cotinine for the Treatment of Psychiatric Disorders?
Current Pharmaceutical Design Trichostatin A - like Hydroxamate Histone Deacetylase Inhibitors as Therapeutic Agents: Toxicological Point of View
Current Medicinal Chemistry Conformational Changes of Prion Protein and Nucleic Acid Arising from their Interaction and Relation of the Altered Structures in Causing Prion Disease
Mini-Reviews in Medicinal Chemistry Interaction Between Estrogen Receptor Alpha and Insulin/IGF Signaling in Breast Cancer
Current Cancer Drug Targets Therapeutic Potential of Ferulic Acid in Alzheimer's Disease
Current Drug Delivery Trends in Mitochondrial Therapeutics for Neurological Disease
Current Medicinal Chemistry Multiple Protective Functions of Sigma1 Receptor
Current Protein & Peptide Science Immune System Modulation by Thyroid Axis Includes Direct Genomic and Nongenomic Actions of Thyroid Hormones on Immune Cells
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Diversity and Variability of the Effects of Nicotine on Different Cortical Regions of the Brain. Therapeutic and Toxicological Implications
Central Nervous System Agents in Medicinal Chemistry Advancing Drug Therapy for Brain Tumours: A Current Review of the Pro-inflammatory Peptide Substance P and its Antagonists as Anti-cancer Agents
Recent Patents on CNS Drug Discovery (Discontinued) ras Genes and Human Cancer: Different Implications and Different Roles
Current Genomics Neuroprotective Effects of Citrus Fruit-Derived Flavonoids, Nobiletin and Tangeretin in Alzheimer's and Parkinson's Disease
CNS & Neurological Disorders - Drug Targets Evolving Therapeutic Targets in Ischemic Stroke: A Concise Review
Current Drug Targets L-carnitine: Searching for New Therapeutic Strategy for Sepsis Management
Current Medicinal Chemistry