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
-
Patented Small Molecules Used for Reprogramming
Recent Patents on Regenerative Medicine 3D-QSAR and Docking Simulation Studies of Some Benzopyrone Derivatives as Inhibitors for Breast Cancer Stem Cell Growth via PGlycoprotein Mediated Efflux
Current Bioinformatics Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs
Current Drug Metabolism Relationship Between Susceptibility to DMCM-Induced Generalized Motor Convulsions and Low-Affinity [3H]-Ouabain Binding in Membranes in Rat Brain
Current Molecular Pharmacology Patent Annotations
Recent Patents on Anti-Cancer Drug Discovery The Effects of Locus Coeruleus and Norepinephrine in Methamphetamine Toxicity
Current Neuropharmacology Phenotypic Screening Strategies for Neurodegenerative Diseases: A Pathway to Discover Novel Drug Candidates and Potential Disease Targets or Mechanisms
CNS & Neurological Disorders - Drug Targets Brain Serotonin, Psychoactive Drugs, and Effects on Reproduction
Central Nervous System Agents in Medicinal Chemistry Pharmacological Regulators of Intracellular Calcium Release Channels
Current Pharmaceutical Design Global Expression Studies of Schizophrenic Brain: A Meta-Analysis Study Linking Neurological Immune System with Psychological Disorders
CNS & Neurological Disorders - Drug Targets Tactile Angle Discrimination Decreases due to Subjective Cognitive Decline in Alzheimer’s Disease
Current Alzheimer Research Environment, Physical Activity, and Neurogenesis: Implications for Prevention and Treatment of Alzhemiers Disease
Current Alzheimer Research Synthesis and Analysis of Anticonvulsant Activities of New 4-[2-(4- alkoxybenzylamino)ethyl]-2H-1,2,4-triazol-3(4H)-one Derivatives
Letters in Drug Design & Discovery Finding the Smoking Gun: Protein Tyrosine Phosphatases as Tools and Targets of Unicellular Microorganisms and Viruses
Current Medicinal Chemistry Macrophage Derived Cystatin B/Cathepsin B in HIV Replication and Neuropathogenesis
Current HIV Research Interactions of β - and Hydroxypropyl-β-Cyclodextrin with Some Purine Alkaloids:Thermodynamic Study
Current Drug Discovery Technologies Antipsychotic and Antiepileptic Drugs in Bipolar Disorder: The Importance of Therapeutic Drug Monitoring
Current Medicinal Chemistry The Role of Sodium Channels in the Mechanism of Action of Antidepressants and Mood Stabilizers
Current Drug Targets Recent Patents on Epilepsy Genetics
Recent Patents on DNA & Gene Sequences Recent Patents and Discovery of Anti-inflammatory Agents from Marine Source
Recent Patents on Inflammation & Allergy Drug Discovery