Universität zu Köln

Lange, Tobias, Thomas, Andreas, Goergens, Christian, Bidlingmaier, Martin, Schilbach, Katharina, Fichant, Eric, Delahaut, Philippe ORCID: 0000-0003-2328-3042 and Thevis, Mario (2021). Comprehensive insights into the formation of metabolites of the ghrelin mimetics capromorelin, macimorelin and tabimorelin as potential markers for doping control purposes. Biomed. Chromatogr., 35 (6). HOBOKEN: WILEY. ISSN 1099-0801

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Abstract

Analytical methods to determine the potential misuse of the ghrelin mimetics capromorelin (CP-424,391), macimorelin (macrilen, EP-01572) and tabimorelin (NN703) in sports were developed. Therefore, different extraction strategies, i.e. solid-phase extraction, protein precipitation, as well as a dilute-and-inject approach, from urine and EDTA-plasma were assessed and comprehensive in vitro/in vivo experiments were conducted, enabling the identification of reliable target analytes by means of high resolution mass spectrometry. The drugs' biotransformation led to the preliminary identification of 51 metabolites of capromorelin, 12 metabolites of macimorelin and 13 metabolites of tabimorelin. Seven major metabolites detected in rat urine samples collected post-administration of 0.5-1.0 mg of a single oral dose underwent in-depth characterization, facilitating their implementation into future confirmatory test methods. In particular, two macimorelin metabolites exhibiting considerable abundances in post-administration rat urine samples were detected, which might contribute to an improved sensitivity, specificity, and detection window in case of human sports drug testing programs. Further, the intact drugs were implemented into World Anti-Doping Agency-compliant initial testing (limits of detection 0.02-0.60 ng/ml) and confirmation procedures (limits of identification 0.18-0.89 ng/ml) for human urine and blood matrices. The obtained results allow extension of the test spectrum of doping agents in multitarget screening assays for growth hormone-releasing factors from human urine.

Item Type:	Journal Article
Creators:	Creators Email ORCID ORCID Put Code Lange, Tobias UNSPECIFIED UNSPECIFIED UNSPECIFIED Thomas, Andreas UNSPECIFIED UNSPECIFIED UNSPECIFIED Goergens, Christian UNSPECIFIED UNSPECIFIED UNSPECIFIED Bidlingmaier, Martin UNSPECIFIED UNSPECIFIED UNSPECIFIED Schilbach, Katharina UNSPECIFIED UNSPECIFIED UNSPECIFIED Fichant, Eric UNSPECIFIED UNSPECIFIED UNSPECIFIED Delahaut, Philippe UNSPECIFIED orcid.org/0000-0003-2328-3042 UNSPECIFIED Thevis, Mario UNSPECIFIED UNSPECIFIED UNSPECIFIED
URN:	urn:nbn:de:hbz:38-582687
DOI:	10.1002/bmc.5075
Journal or Publication Title:	Biomed. Chromatogr.
Volume:	35
Number:	6
Date:	2021
Publisher:	WILEY
Place of Publication:	HOBOKEN
ISSN:	1099-0801
Language:	English
Faculty:	Unspecified
Divisions:	Unspecified
Subjects:	no entry
Uncontrolled Keywords:	Keywords Language Biochemical Research Methods; Biochemistry & Molecular Biology; Chemistry, Analytical; Pharmacology & Pharmacy Multiple languages
URI:	http://kups.ub.uni-koeln.de/id/eprint/58268