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Sökning: id:"swepub:oai:DiVA.org:uu-344303" > Equine in vivo-deri...

LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00004003naa a2200445 4500
001oai:DiVA.org:uu-344303
003SwePub
008180306s2018 | |||||||||||000 ||eng|
024a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-3443032 URI
024a https://doi.org/10.1016/j.jchromb.2017.12.0102 DOI
040 a (SwePub)uu
041 a engb eng
042 9 SwePub
072 7a ref2 swepub-contenttype
072 7a art2 swepub-publicationtype
100a Hansson, Annelieu Uppsala universitet,Analytisk vetenskap4 aut0 (Swepub:uu)annha905
2451 0a Equine in vivo-derived metabolites of the SARM LGD-4033 and comparison with human and fungal metabolites.
264 1b Elsevier BV,c 2018
338 a print2 rdacarrier
520 a LGD-4033 has been found in human doping control samples and has the potential for illicit use in racehorses as well. It belongs to the pharmacological class of selective androgen receptor modulators (SARMs) and can stimulate muscle growth, much like anabolic steroids. However, SARMs have shown superior side effect profiles compared to anabolic steroids, which arguably makes them attractive for use by individuals seeking an unfair advantage over their competitors. The purpose of this study was to investigate the metabolites formed from LGD-4033 in the horse in order to find suitable analytical targets for doping controls. LGD-4033 was administered to three horses after which plasma and urine samples were collected and analyzed for metabolites using ultra high performance liquid chromatography coupled to a high resolution mass spectrometer. In horse urine, eight metabolites, both phase I and phase II, were observed most of which had not been described in other metabolic systems. Six of these were also detected in plasma. The parent compound was detected in plasma, but not in non-hydrolyzed urine. The longest detection times were observed for unchanged LGD-4033 in plasma and in urine hydrolyzed with β-glucuronidase and is thus suggested as the analytical target for doping control in the horse. The metabolite profile determined in the horse samples was also compared to those of human urine and fungal incubate from Cunninghamella elegans. The main human metabolite, dihydroxylated LGD-4033, was detected in the horse samples and was also produced by the fungus. However, it was a not a major metabolite for horse and fungus, which highlights the importance of performing metabolism studies in the species of interest.
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Läkemedelskemi0 (SwePub)301032 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Medicinal Chemistry0 (SwePub)301032 hsv//eng
653 a Doping
653 a LGD-4033
653 a Horse
653 a Mass Spectrometry
653 a Metabolite
653 a SARM
653 a Selective Androgen Receptor Modulator
700a Knych, Heather4 aut
700a Stanley, Scott4 aut
700a Berndtson, Emmau Uppsala universitet,Analytisk vetenskap,Natl Vet Inst SVA, Dept Chem Environm & Feed Hyg, SE-75651 Uppsala, Sweden4 aut
700a Jackson, Liorau Uppsala universitet,Analytisk vetenskap,Natl Vet Inst SVA, Dept Chem Environm & Feed Hyg, SE-75651 Uppsala, Sweden4 aut
700a Bondesson, Ulfu Uppsala universitet,Analytisk vetenskap,Natl Vet Inst SVA, Dept Chem Environm & Feed Hyg, SE-75651 Uppsala, Sweden4 aut0 (Swepub:uu)ulfbonde
700a Thevis, Mario4 aut
700a Hedeland, Mikaelu Uppsala universitet,Analytisk vetenskap,Natl Vet Inst SVA, Dept Chem Environm & Feed Hyg, SE-75651 Uppsala, Sweden4 aut0 (Swepub:uu)mikahede
710a Uppsala universitetb Analytisk vetenskap4 org
773t Journal of chromatography. Bd : Elsevier BVg 1074-1075, s. 91-98q 1074-1075<91-98x 1570-0232x 1873-376X
8564 8u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-344303
8564 8u https://doi.org/10.1016/j.jchromb.2017.12.010

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