Abstract
Many physiological and biochemical measurements can be performed noninvasively in humans with modern imaging techniques like magnetic resonance imaging (MRI), positron emission tomography (PET) or single-photon emission computed tomography (SPECT). This review focuses on the monitoring of drugreceptor interactions in patients and healthy volunteers with PET. Such studies depend on the availability of a suitable radioligand; they are already possible for classical and atypical neuroleptics, anxiolytics, antidepressants, anticholinergics, antihistamines, antiepileptics, beta-blockers and hypnotic drugs. In Phase I-II human studies, measurements of plasma pharmacokinetics can be combined with images of receptor occupancy and be quantitatively related to pharmacologic effects which are induced in the same subjects. Optimal dosing schedules can be defined and valuable information for the design of Phase III studies can be acquired. Moreover, the effect of interventions (e.g. change of dose, additional medication) can be predicted. Medical imaging techniques will play an increasing role in clinical pharmacology and allow well-informed go/no-go decisions in future drug development
Current Pharmaceutical Design
Title: Measuring Receptor Occupancy with PET
Volume: 6 Issue: 16
Author(s): Aren van Waarde
Affiliation:
Abstract: Many physiological and biochemical measurements can be performed noninvasively in humans with modern imaging techniques like magnetic resonance imaging (MRI), positron emission tomography (PET) or single-photon emission computed tomography (SPECT). This review focuses on the monitoring of drugreceptor interactions in patients and healthy volunteers with PET. Such studies depend on the availability of a suitable radioligand; they are already possible for classical and atypical neuroleptics, anxiolytics, antidepressants, anticholinergics, antihistamines, antiepileptics, beta-blockers and hypnotic drugs. In Phase I-II human studies, measurements of plasma pharmacokinetics can be combined with images of receptor occupancy and be quantitatively related to pharmacologic effects which are induced in the same subjects. Optimal dosing schedules can be defined and valuable information for the design of Phase III studies can be acquired. Moreover, the effect of interventions (e.g. change of dose, additional medication) can be predicted. Medical imaging techniques will play an increasing role in clinical pharmacology and allow well-informed go/no-go decisions in future drug development
Export Options
About this article
Cite this article as:
van Waarde Aren, Measuring Receptor Occupancy with PET, Current Pharmaceutical Design 2000; 6 (16) . https://dx.doi.org/10.2174/1381612003398951
DOI https://dx.doi.org/10.2174/1381612003398951 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
- 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
-
Xenobiotic Acyl Glucuronides and Acyl CoA Thioesters as Protein- Reactive Metabolites With the Potential to Cause Idiosyncratic Drug Reactions
Current Drug Metabolism AMPA Receptor Antagonists: Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Proteins Structures in Leishmania Amastigotes for Clinical Remission of Psoriasis
Current Proteomics AMPA Receptors in the Therapeutic Management of Depression
CNS & Neurological Disorders - Drug Targets Conventional (Continuous) EEG Monitoring in the NICU
Current Pediatric Reviews The Emerging Role of Metabotropic Glutamate Receptors in the Pathophysiology of Chronic Stress-Related Disorders
Current Neuropharmacology Benzimidazole Derivatives as Centerally Acting Agents
Current Drug Therapy Inherited Copper Transport Disorders: Biochemical Mechanisms, Diagnosis, and Treatment
Current Drug Metabolism Recent Developments in Group I Metabotropic Glutamate Receptor Allosteric Modulators for the Treatment of Psychiatric and Neurological Disorders (2014-May 2015)
Current Topics in Medicinal Chemistry Taurine Analogues; A New Class of Therapeutics: Retrospect and Prospects
Current Medicinal Chemistry The Safety, Tolerability, Pharmacokinetics and Cognitive Effects of GSK239512, a Selective Histamine H<sub>3</sub> Receptor Antagonist in Patients with Mild to Moderate Alzheimer’s Disease: A Preliminary Investigation
Current Alzheimer Research Synthesis, Anticonvulsant Evaluation of 2,3,4,5-Tetrahydro-7-alkoxy-1H-2-benzazepin-1-ones
Letters in Drug Design & Discovery Gene Therapy for Angelman Syndrome: Contemporary Approaches and Future Endeavors
Current Gene Therapy Monitoring Antiepileptic Drugs: A Level-Headed Approach
Current Neuropharmacology Integration of <sup>18</sup>FDG-PET Metabolic and Functional Connectomes in the Early Diagnosis and Prognosis of the Alzheimer's Disease
Current Alzheimer Research A Comprehensive Investigation of Molecular Signatures and Pathways Linking Alzheimer’s Disease and Epilepsy <i>via</i> Bioinformatic Approaches
Current Alzheimer Research Therapeutic Hypothermia as a Neuroprotective Strategy in Neonatal Hypoxic-Ischemic Brain Injury and Traumatic Brain Injury
Current Molecular Medicine Nano-medicine Improving the Bioavailability of Small Molecules for the Prevention of Neurodegenerative Diseases
Current Pharmaceutical Design The Role of Spiritual Health Experience with Intensity and Duration of Labor Pain While Childbearing and Postpartum
Current Women`s Health Reviews HtrA Serine Proteases as Potential Therapeutic Targets in Cancer
Current Cancer Drug Targets