Abstract
Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-D-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.
Keywords: Positron Emission Tomography, Ion Channel, γ-Aminobutyric Acid-Benzodiazapine Receptor, Nicotinic Acetylcholine Receptor, N-Methyl-D-Aspartate Receptor.
Current Topics in Medicinal Chemistry
Title:Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors
Volume: 16 Issue: 16
Author(s): Alina Kassenbrock, Neil Vasdev and Steven H. Liang
Affiliation:
Keywords: Positron Emission Tomography, Ion Channel, γ-Aminobutyric Acid-Benzodiazapine Receptor, Nicotinic Acetylcholine Receptor, N-Methyl-D-Aspartate Receptor.
Abstract: Positron emission tomography (PET) neuroimaging of ion channel linked receptors is a developing area of preclinical and clinical research. The present review focuses on recent advances with radiochemistry, preclinical and clinical PET imaging studies of three receptors that are actively pursued in neuropsychiatric drug discovery: namely the γ-aminobutyric acid-benzodiazapine (GABA) receptor, nicotinic acetylcholine receptor (nAChR), and N-methyl-D-aspartate (NMDA) receptor. Recent efforts to develop new PET radioligands for these targets with improved brain uptake, selectivity, stability and pharmacokinetics are highlighted.
Export Options
About this article
Cite this article as:
Kassenbrock Alina, Vasdev Neil and H. Liang Steven, Selected PET Radioligands for Ion Channel Linked Neuroreceptor Imaging: Focus on GABA, NMDA and nACh Receptors, Current Topics in Medicinal Chemistry 2016; 16 (16) . https://dx.doi.org/10.2174/1568026616666160315142457
DOI https://dx.doi.org/10.2174/1568026616666160315142457 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...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
-
The Antiepileptic Potential of Nucleosides
Current Medicinal Chemistry Dysiherbaine: A New Generation of Excitatory Amino Acids of Marine Origin
Central Nervous System Agents in Medicinal Chemistry Caffeine as a Lead Compound for the Design of Therapeutic Agents for the Treatment of Parkinson’s Disease
Current Medicinal Chemistry Ester Prodrugs of Ketoprofen: Synthesis, In Vitro Stability, In Vivo Biological Evaluation and In Silico Comparative Docking Studies Against COX-1 and COX-2
Current Drug Discovery Technologies Targeting S100B Protein as a Surrogate Biomarker and its Role in Various Neurological Disorders
Current Neuropharmacology Commentary [Research Highlights (Making Sense Out of Antisense in Huntington’s Disease)]
CNS & Neurological Disorders - Drug Targets Targeting Mitochondrial Oxidative Stress Through Lipoic Acid Synthase: A Novel Strategy to Manage Diabetic Cardiovascular Disease
Cardiovascular & Hematological Agents in Medicinal Chemistry <i>Nigella sativa</i> – A Functional Spice From A Pharaoh’s Tomb to Modern Healthcare
The Natural Products Journal Commentary: Gut Microbiota and Brain Function: A New Target for Brain Diseases?
CNS & Neurological Disorders - Drug Targets Anti-Carcinogenic Effects of Carnosol-An Updated Review
Current Drug Discovery Technologies Physiopathological Roles of P2X Receptors in the Central Nervous System
Current Medicinal Chemistry p38 MAP Kinase Inhibitors as Potential Therapeutic Drugs for Neural Diseases
Central Nervous System Agents in Medicinal Chemistry Recent Developments on KCNQ Potassium Channel Openers
Current Medicinal Chemistry Therapeutic Potential of Natural Products from Terrestrial Plants as TNF-α Antagonist
Current Topics in Medicinal Chemistry Clinical Trials of Cancer Therapies Targeting Prostate-Specific Membrane Antigen
Reviews on Recent Clinical Trials Pathophysiological Role of Mitochondrial Potassium Channels and their Modulation by Drugs
Current Medicinal Chemistry Patent Selections:
Recent Patents on Anti-Cancer Drug Discovery Third and Fourth Generation Fluoroquinolone Antibacterials: A Systematic Review of Safety and Toxicity Profiles
Current Drug Safety Inhibition of Human Serine Racemase, an Emerging Target for Medicinal Chemistry
Current Drug Targets Susceptibility Genes for the Side Effect of Antipsychotics on Body Weight and Obesity
Current Drug Targets