Effectiveness of quenchers to reduce radiolysis of 111- or 177-labelled methionine-containing regulatory peptides. maintaining radiochemical purity as measured by HPLC
Current Topics in Medicinal Chemistry , Volume 12 - Issue 23 p. 2677- 2685
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 radiola-belling 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 f(concentration) to investigate efficacy to reduce radiolysis of radiolabelled methionine-containing regulatory peptides. © 2012 Bentham Science Publishers.