Universität zu Köln

Thomas, Andreas ORCID: 0000-0003-1199-0743, Knoop, Andre, Schaenzer, Wilhelm and Thevis, Mario (2017). Characterization of in vitro generated metabolites of selected peptides < 2 kDa prohibited in sports. Drug Test. Anal., 9 (11-12). S. 1799 - 1804. HOBOKEN: WILEY. ISSN 1942-7611

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Abstract

With an increasing number of prohibited substances in doping controls, knowledge about their metabolism is crucial for efficient analysis. While for lowmolecularmassmolecules, standard protocols for in vitrometabolismexperiments are well established, the situation with peptidic drugs has been shown to be substantially more heterogeneous and complex. Two principle strategies aiming at simulating the metabolism of lower molecular mass peptides in vitro are presented within this study. The prohibited peptides ARA-290, GHRP-3, and Peforelin, with a to-date unknown metabolism, were chosen as model compounds for these experiments and metabolism after incubation with different blood specimens (DTA-, heparin-, citrate-plasma, and serum) and exposure to recombinant amidase were investigated. The characterization of in vitro generated drug-derived peptidic analytes was accomplished by means of liquid chromatography coupled to high resolutionmass spectrometry. Identification of the generated metabolites was ensured by dedicated high resolution product ion experiments after liquid chromatographic separation. While extensive exopeptidase-driven metabolism was observed for ARA-290 (with one main metabolite PyrEQLERALN), GHRP-3 and Peforelin were found to exhibit a considerable metabolic stability with a low tendency for deamidation only. Copyright (c) 2017 John Wiley & Sons, Ltd.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Thomas, Andreas UNSPECIFIED orcid.org/0000-0003-1199-0743 UNSPECIFIED Knoop, Andre UNSPECIFIED UNSPECIFIED UNSPECIFIED Schaenzer, Wilhelm UNSPECIFIED UNSPECIFIED UNSPECIFIED Thevis, Mario UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-211839
DOI:	10.1002/dta.2306
Journal or Publication Title:	Drug Test. Anal.
Volume:	9
Number:	11-12
Page Range:	S. 1799 - 1804
Date:	2017
Publisher:	WILEY
Place of Publication:	HOBOKEN
ISSN:	1942-7611
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language LIQUID-CHROMATOGRAPHY; O-METHYLATION; HIGENAMINE; PLASMA; URINE Multiple languages Biochemical Research Methods; Chemistry, Analytical; Pharmacology & Pharmacy Multiple languages
Refereed:	Yes
URI:	http://kups.ub.uni-koeln.de/id/eprint/21183