title: Effectiveness of quenchers to reduce radiolysis of (111)In- or (177)Lu-labelled methionine-containing regulatory peptides. Maintaining radiochemical purity as measured by HPLC.
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.
authors: Department of Nucear Medicine, Rotterdam, The Netherlands.
authors: Erik
authors: E
authors: de Blois
authors: Ho Sze
authors: HS
authors: Chan
authors: Mark
authors: M
authors: Konijnenberg
authors: Rory
authors: R
authors: de Zanger
authors: Wouter A P
authors: WA
authors: Breeman
mesh_terms: D002614:Chelating Agents / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D005079:Excipients / Q000737:chemistry*; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry; D006801:Humans; D007205:Indium Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000592:standards*; D008187:Lutetium / Q000737:chemistry*; D008715:Methionine / Q000737:chemistry; D004369:Pentetic Acid / Q000737:chemistry; D010455:Peptides / Q000737:chemistry* / Q000302:isolation & purification; D055550:Protein Stability; D011851:Radioactivity; D011874:Radiometry; D019275:Radiopharmaceuticals / Q000737:chemistry*
chemical_list: D002614:Chelating Agents; D005079:Excipients; D006573:Heterocyclic Compounds, 1-Ring; D007205:Indium Radioisotopes; D010455:Peptides; D019275:Radiopharmaceuticals; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D008187:Lutetium; D004369:Pentetic Acid; D008715:Methionine