Abstract
Positron emission tomography (PET) is a useful technique to quantify various target molecules in vivo such as neuroreceptors, transporters and amyloid plaques using various successful radioligands. The technique has been widely used for the drug development in recent years. There are several approaches such as microdosing, measurement of in vivo receptor occupancy, and biomarkers. As for microdosing, the biodistrubution of the drugs in the human body could be evaluated in the very early phase of the drug development. The measurement of receptor occupancy in vivo could help to determine the optimal doses clinically before the largescale clinical trials are perfomred. As biomarkers, radioligands could detect the pathological changes such as the accumulation of betaamyloid and microglia. Especially the measurement of dopamine D2 receptor occupancy has been useful in the evaluation of antipsychotics. Based on it, the optimal clinical doses were evaluated and determined for the patients with schizophrenia. Although currently available antipsychotics have efficacy to the positive symptoms such as hallucination and delusion, they, regardless of the generations of antipsychotics, have only limited efficacy to the cognitive dysfunction and the negative symptoms such as apathy and social withdrawal. To aim to treat the cognitive dysfunction and negative symptoms, various targets such as glutamate receptors, tachykinin receptors, cannabinoid receptors, and nicotinic acetylcholine receptors, have been investigated recently. PET technique with the radioligands developed for these targets has potentials to rationalize and speed up the process of the drug development for the treatment of schizophrenia.
Keywords: PET Technique, Novel Antipsychotics, neuroreceptors, amyloid plaques, dopamine D2 receptor
Current Pharmaceutical Design
Title: The Application of PET Technique for the Development and Evaluation of Novel Antipsychotics
Volume: 16 Issue: 3
Author(s): Akihiro Takano
Affiliation:
Keywords: PET Technique, Novel Antipsychotics, neuroreceptors, amyloid plaques, dopamine D2 receptor
Abstract: Positron emission tomography (PET) is a useful technique to quantify various target molecules in vivo such as neuroreceptors, transporters and amyloid plaques using various successful radioligands. The technique has been widely used for the drug development in recent years. There are several approaches such as microdosing, measurement of in vivo receptor occupancy, and biomarkers. As for microdosing, the biodistrubution of the drugs in the human body could be evaluated in the very early phase of the drug development. The measurement of receptor occupancy in vivo could help to determine the optimal doses clinically before the largescale clinical trials are perfomred. As biomarkers, radioligands could detect the pathological changes such as the accumulation of betaamyloid and microglia. Especially the measurement of dopamine D2 receptor occupancy has been useful in the evaluation of antipsychotics. Based on it, the optimal clinical doses were evaluated and determined for the patients with schizophrenia. Although currently available antipsychotics have efficacy to the positive symptoms such as hallucination and delusion, they, regardless of the generations of antipsychotics, have only limited efficacy to the cognitive dysfunction and the negative symptoms such as apathy and social withdrawal. To aim to treat the cognitive dysfunction and negative symptoms, various targets such as glutamate receptors, tachykinin receptors, cannabinoid receptors, and nicotinic acetylcholine receptors, have been investigated recently. PET technique with the radioligands developed for these targets has potentials to rationalize and speed up the process of the drug development for the treatment of schizophrenia.
Export Options
About this article
Cite this article as:
Takano Akihiro, The Application of PET Technique for the Development and Evaluation of Novel Antipsychotics, Current Pharmaceutical Design 2010; 16 (3) . https://dx.doi.org/10.2174/138161210790170102
DOI https://dx.doi.org/10.2174/138161210790170102 |
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
-
Recent Progress in Dendrimer-based Gene Delivery Systems
Current Organic Chemistry Systemic Redox Biomarkers in Neurodegenerative Diseases
Current Drug Metabolism From Preclinical to Clinical Trials: An Update on Potential Therapies for Huntington’s Disease
Current Psychopharmacology Lithium and its Neuroprotective and Neurotrophic Effects: Potential Treatment for Post-Ischemic Stroke Sequelae
Current Drug Targets Disease-Specific iPS Cell Models in Neuroscience
Current Molecular Medicine Biological Function and Medicinal Research Significance of G-Quadruplex Interactive Proteins
Current Topics in Medicinal Chemistry The Molecular Pathology of Huntingtons Disease (HD)
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents An Overview of Published Papers and Important Developments in the Past Three Years
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Editorial [Hot topic: Role of Inflammation in Neurological and Psychiatric Disorders (Guest Editor: Mohtashem Samsam)]
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Receptor for AGEs (RAGE) as Mediator of NF-kB Pathway Activation in Neuroinflammation and Oxidative Stress
CNS & Neurological Disorders - Drug Targets The Role of Mitochondria in Cancer Induction, Progression and Changes in Metabolism
Mini-Reviews in Medicinal Chemistry An Overview of Drug Screening Using Primary and Embryonic Stem Cells
Combinatorial Chemistry & High Throughput Screening Curcumin as an Anti-Cancer Agent: Review of the Gap Between Basic and Clinical Applications
Current Medicinal Chemistry Recents Patents for Isolating, Delivering and Tracking Adult Stem Cells in Regenerative Medicine
Recent Patents on Drug Delivery & Formulation Hyperhomocysteinemia, Pteridines and Oxidative Stress
Current Drug Metabolism In silico Modeling Studies of 5-HT2B Antagonistic Activity of 2-(2- phenylethyl)chromone Derivatives from Cucumis melo Seeds
Letters in Drug Design & Discovery Histone Deacetylase Inhibitors: Therapeutic Agents and Research Tools for Deciphering Motor Neuron Diseases
Current Medicinal Chemistry Oxidative Stress and Antioxidant Potential of One Hundred Medicinal Plants
Current Topics in Medicinal Chemistry A MicroRNA-BDNF Negative Feedback Signaling Loop in Brain: Implications for Alzheimer’s Disease
MicroRNA Population Studies of Association Between Lithium and Risk of Neurodegenerative Disorders
Current Alzheimer Research