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

Autor: James Johnston, Jürgen Engel, Harald Borbe, Mathias Locher, Bernhard Kutscher, Thomas Müller
Rok vydání: 1994
Předmět:
Zdroj: Journal of Labelled Compounds and Radiopharmaceuticals. 34:1091-1098
ISSN: 0362-4803
DOI: 10.1002/jlcr.2580341113
Popis: 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 [14C]-lebelled compound is essential. Therefore, [U-14C]Arg cetrorelix acetate salt was synthesized by Amersham International, Buckinghamshire (England) from precursor peptides provided by Degussa AG, Hanau-Wolfgang (Germany). [U-14C]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.
Databáze: OpenAIRE