Synthesis of [U-14C]Arg labelled decapeptide cetrorelix, a novel lutenizing hormone — releasing hormone antagonist

✍ Scribed by Mathias Locher; James Johnston; Thomas Müller; Harald O. Borbe; Bernhard Kutscher; Jürgen Engel

• Publisher: John Wiley and Sons
• Year: 1994
• Tongue: French
• Weight: 319 KB
• Volume: 34
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.2580341113

✦ Synopsis

Abstract

The decapeptide cetrorelix is a novel luteinizing hormone — releasing hormone (LH‐RH) antagonist. For nonclinical studies concerning absorption, distribution, metabolism and excretion (ADME) in animals the [^14^C]‐lebelled compound is essential. Therefore, [U‐^14^C]Arg cetrorelix acetate salt was synthesized by Amersham International, Buckinghamshire (England) from precursor peptides provided by Degussa AG, Hanau‐Wolfgang (Germany). [U‐^14^C]Arg labelled cetrorelix peptide base has a specific activity of 8.13 MBq/mg (220 μCi/mg) and a molecular weight of 1442.6 g/mol at this specific activity. The chemical and radiochemical purity (92.2 % decapeptide content and 97.6%, respectively) determined by HPLC is suitable for nonclinical investigations.