Abstract
An overview how to measure and to quantify radiolysis by the addition of quenchers and to maintain Radio- Chemical Purity (RCP) of vulnerable methionine-containing regulatory peptides is presented. High RCP was only achieved with a combination of quenchers. However, quantification of RCP is not standardized, and therefore comparison of radiolabelling and RCP of regulatory peptides between different HPLC-systems and between laboratories is cumbersome. Therefore we suggest a set of standardized requirements to quantify RCP by HPLC for radiolabelled DTPA- or DOTA-peptides. Moreover, a dosimetry model was developed to calculate the doses in the reaction vials during radiolabelling and storage of the radiopeptides, and to predict RCP in the presence and absence of quenchers. RCP was measured by HPLC, and a relation between radiation dose and radiolysis of RCP was established. The here described quenchers are tested individually as ƒ(concentration) to investigate efficacy to reduce radiolysis of radiolabelled methionine-containing regulatory peptides.
Keywords: gastrin releasing peptide, HPLC, minigastrin, quenchers, radiochemical purity, radiolysis, methionine, regulatory peptides
Current Topics in Medicinal Chemistry
Title:Effectiveness of Quenchers to Reduce Radiolysis of 111In- or 177Lu-Labelled Methionine-Containing Regulatory Peptides. Maintaining Radiochemical Purity as Measured by HPLC
Volume: 12 Issue: 23
Author(s): Erik de Blois, Ho Sze Chan, Mark Konijnenberg, Rory de Zanger and Wouter A.P. Breeman
Affiliation:
Keywords: gastrin releasing peptide, HPLC, minigastrin, quenchers, radiochemical purity, radiolysis, methionine, regulatory peptides
Abstract: An overview how to measure and to quantify radiolysis by the addition of quenchers and to maintain Radio- Chemical Purity (RCP) of vulnerable methionine-containing regulatory peptides is presented. High RCP was only achieved with a combination of quenchers. However, quantification of RCP is not standardized, and therefore comparison of radiolabelling and RCP of regulatory peptides between different HPLC-systems and between laboratories is cumbersome. Therefore we suggest a set of standardized requirements to quantify RCP by HPLC for radiolabelled DTPA- or DOTA-peptides. Moreover, a dosimetry model was developed to calculate the doses in the reaction vials during radiolabelling and storage of the radiopeptides, and to predict RCP in the presence and absence of quenchers. RCP was measured by HPLC, and a relation between radiation dose and radiolysis of RCP was established. The here described quenchers are tested individually as ƒ(concentration) to investigate efficacy to reduce radiolysis of radiolabelled methionine-containing regulatory peptides.
Export Options
About this article
Cite this article as:
de Blois Erik, Sze Chan Ho, Konijnenberg Mark, de Zanger Rory and A.P. Breeman Wouter, Effectiveness of Quenchers to Reduce Radiolysis of 111In- or 177Lu-Labelled Methionine-Containing Regulatory Peptides. Maintaining Radiochemical Purity as Measured by HPLC, Current Topics in Medicinal Chemistry 2012; 12 (23) . https://dx.doi.org/10.2174/1568026611212230005
DOI https://dx.doi.org/10.2174/1568026611212230005 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- 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
-
Third Generation Radiopharmaceuticals for Imaging and Targeted Therapy
Current Pharmaceutical Analysis miRNAs in Gastrointestinal and Liver Cancers: Their Perspectives and Clinical Applications
Current Pharmaceutical Design Soy Saponins and the Anticancer Effects of Soybeans and Soy-Based Foods
Current Medicinal Chemistry - Anti-Cancer Agents Analytical Methods for Metallothionein Detection
Current Analytical Chemistry 2-(ω-Carboxyethyl)pyrrole Antibody as a New Inhibitor of Tumor Angiogenesis and Growth
Anti-Cancer Agents in Medicinal Chemistry Frequency of Pathological Types of Hyperthyroidism in Thyroid Scan Patients
Current Medical Imaging The Endocannabinoid System in Ageing: A New Target for Drug Development
Current Drug Targets Synthesis and Evaluation of Antioxidant and Cytotoxicity of the N-Mannich Base of Berberine Bearing Benzothiazole Moieties
Anti-Cancer Agents in Medicinal Chemistry Chronic Inflammation and Cancer: The Role of Endothelial Dysfunction and Vascular Inflammation
Current Pharmaceutical Design Role of Nuclear Steroid Receptors in Apoptosis
Current Medicinal Chemistry TNF-α and Ghrelin: Opposite Effects on Immune System, Metabolism and Mental Health
Protein & Peptide Letters Pharmacological and Biological Therapies for Metabolic Bone Disease in Critical Illness: An Integrative Physiology Approach
Current Drug Therapy Liposomal Targeting of Angiogenic Vasculature
Current Drug Delivery Biomarkers in Molecularly Targeted Therapy for Cancer
Recent Patents on Biomarkers Stilbenes and Xanthones from Medicinal Plants as Potential Antitumor Agents
Current Bioactive Compounds Organosulphur Compounds Induce Apoptosis and Cell Cycle Arrest in Cervical Cancer Cells via Downregulation of HPV E6 and E7 Oncogenes
Anti-Cancer Agents in Medicinal Chemistry Potassium Channels: Novel Emerging Biomarkers and Targets for Therapy in Cancer
Recent Patents on Anti-Cancer Drug Discovery The Caveolin-1 Connection to Cell Death and Survival
Current Molecular Medicine Challenging the Current Approaches to Multiple Myeloma-Related Bone Disease: From Bisphosphonates to Target Therapy
Current Cancer Drug Targets Immunomodulatory Roles of VIP and PACAP in Models of Multiple Sclerosis
Current Pharmaceutical Design