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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Effectiveness of Quenchers to Reduce Radiolysis of 111In- or 177Lu-Labelled Methionine-Containing Regulatory Peptides. Maintaining Radiochemical Purity as Measured by HPLC

Author(s): Erik de Blois, Ho Sze Chan, Mark Konijnenberg, Rory de Zanger and Wouter A.P. Breeman

Volume 12 , Issue 23 , 2012

Page: [2677 - 2685] Pages: 9

DOI: 10.2174/1568026611212230005

Price: $65


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

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