Abstract
The only bromine and iodine radioisotopes worth using in PET or SPECT in vivo investigations during the development of a new drug are 76Br and 123I. It is most of the time impossible to isotopically label a drug with 76Br or 123I since the occurrence of drugs having a bromine or an iodine atom within their chemical structure is quite limited. However, by using specific radiobrominated or radioiodinated probes, it is possible to study in vivo the potential interaction of a drug with biochemical processess such as blood flow, glucose consumption, protein synthesis or cell proliferation and neurotransmission. Radiobrominated and radioiodinated probes have been described mainly for assessing cell proliferation. For imaging various classes of specific binding sites involved in neuronal or hormonal transmission, a great number of radiohalogenated ligands have been proposed and validated. The two-steps strategy consists of performing an “in vivo assay” by using first of all, one of these specific radio-brominated / -iodinated ligands (or probes) for targeting specific binding sites (receptor, transporter, enzymes) and in a second step by assessing the interaction of the cold drug on the binding of these probes. This indirect observation of drug-receptor (transporter, enzyme) occupancy allows predicting response, optimum dose and optimum scheduling. The most important radiobrominated and radioiodinated ligands specific for dopaminergic, serotoninergic, cholinergic and gabaergic binding sites and their application in drug development processes are reviewed.
Keywords: Bromine, Iodine Radiohalogenated Tracers, muscarinic receptors, nicotinic receptors, gabaergic specific binding site
Current Pharmaceutical Design
Title: Use of Bromine-76 and Iodine-123 Radiohalogenated Tracers in the Drug Development Process
Volume: 7 Issue: 18
Author(s): Bernard Maziere and Christian Loc'h
Affiliation:
Keywords: Bromine, Iodine Radiohalogenated Tracers, muscarinic receptors, nicotinic receptors, gabaergic specific binding site
Abstract: The only bromine and iodine radioisotopes worth using in PET or SPECT in vivo investigations during the development of a new drug are 76Br and 123I. It is most of the time impossible to isotopically label a drug with 76Br or 123I since the occurrence of drugs having a bromine or an iodine atom within their chemical structure is quite limited. However, by using specific radiobrominated or radioiodinated probes, it is possible to study in vivo the potential interaction of a drug with biochemical processess such as blood flow, glucose consumption, protein synthesis or cell proliferation and neurotransmission. Radiobrominated and radioiodinated probes have been described mainly for assessing cell proliferation. For imaging various classes of specific binding sites involved in neuronal or hormonal transmission, a great number of radiohalogenated ligands have been proposed and validated. The two-steps strategy consists of performing an “in vivo assay” by using first of all, one of these specific radio-brominated / -iodinated ligands (or probes) for targeting specific binding sites (receptor, transporter, enzymes) and in a second step by assessing the interaction of the cold drug on the binding of these probes. This indirect observation of drug-receptor (transporter, enzyme) occupancy allows predicting response, optimum dose and optimum scheduling. The most important radiobrominated and radioiodinated ligands specific for dopaminergic, serotoninergic, cholinergic and gabaergic binding sites and their application in drug development processes are reviewed.
Export Options
About this article
Cite this article as:
Maziere Bernard and Loc'h Christian, Use of Bromine-76 and Iodine-123 Radiohalogenated Tracers in the Drug Development Process, Current Pharmaceutical Design 2001; 7 (18) . https://dx.doi.org/10.2174/1381612013396844
DOI https://dx.doi.org/10.2174/1381612013396844 |
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
Blood-based biomarkers in large-scale screening for neurodegenerative diseases
Disease biomarkers are necessary tools that can be employ in several clinical context of use (COU), ranging from the (early) diagnosis, prognosis, prediction, to monitor of disease state and/or drug efficacy. Regarding neurodegenerative diseases, in particular Alzheimer’s disease (AD), a battery of well-validated biomarkers are available, such as cerebrospinal fluid ...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
Diabetes mellitus: advances in diagnosis and treatment driving by precision medicine
Diabetes mellitus (DM) is a chronic degenerative metabolic disease with ever increasing prevalence worldwide which is now an epidemic disease affecting 500 million people worldwide. Insufficient insulin secretion from pancreatic β cells unable to maintain blood glucose homeostasis is the main feature of this disease. Multifactorial and complex nature of ...read more
![](/images/wayfinder.jpg)
- 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
-
Metabolic Therapy of Heart Failure
Current Pharmaceutical Design Molecular Aspects of Modulation of L-type Calcium Channels by Protein Kinase C
Current Molecular Pharmacology Expression of microRNAs (133b and 138) and Correlation with Echocardiographic Parameters in Patients with Alcoholic Cardiomyopathy
MicroRNA Perioperative Considerations in Diabetic Patients
Current Diabetes Reviews Micro-RNA in Disease and Gene Therapy
Current Drug Discovery Technologies Anti-T. cruzi Agents: Our Experience in the Evaluation of More than Five Hundred Compounds
Mini-Reviews in Medicinal Chemistry Green Tea Catechins and Cardiovascular Health: An Update
Current Medicinal Chemistry Surgical Ventricular Restoration to Reverse Left Ventricular Remodeling
Current Cardiology Reviews Evolving Concepts Concerning Cardiac β-Adrenoceptor Function in Heart Failure
Current Pharmaceutical Design Phosphoinositide-3 Kinase Signaling in Cardiac Hypertrophy and Heart Failure
Current Pharmaceutical Design Lifestyle Changes and Surgical Treatment for Hypertension in the Elderly
Cardiovascular & Hematological Agents in Medicinal Chemistry Melatonin Alleviates Pyroptosis of Retinal Neurons Following Acute Intraocular Hypertension
CNS & Neurological Disorders - Drug Targets Pitavastatin and 4-Hydroxy-3-Methoxyacetophenone (HMAP) Reduce Cognitive Dysfunction in Vascular Dementia During Experimental Diabetes
Current Neurovascular Research Acetylome Regulation by Sirtuins in the Brain: From Normal Physiology to Aging and Pathology
Current Pharmaceutical Design Clinical Application of Ghrelin
Current Pharmaceutical Design Anti-inflammatory Treatment of Acute Coronary Syndromes
Current Pharmaceutical Design Targeting Cyclooxygenase and Nitric Oxide Pathway Cross-Talk: A New Signal Transduction Pathway for Developing More Effective Anti- Inflammatory Drugs
Current Signal Transduction Therapy A Critical and Comprehensive Insight on Heme Oxygenase and Related Products Including Carbon Monoxide, Bilirubin, Biliverdin and Ferritin in Type-1 and Type-2 Diabetes
Current Pharmaceutical Design High-Density Lipoprotein-Raising Strategies: Update 2010
Current Pharmaceutical Design Atrial Fibrillation in Heart Failure: An Innocent Bystander?
Current Cardiology Reviews