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New metabolites of hongdenafil, homosildenafil and hydroxyhomosildenafil
  • Yeo, Miseon ;
  • Park, Yujin ;
  • Lee, Heesang ;
  • Choe, Sanggil ;
  • Baek, Seung Hoon ;
  • Kim, Hye Kyung ;
  • Pyo, Jae Sung
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Publication Year
2018-02-05
Journal
Journal of Pharmaceutical and Biomedical Analysis
Publisher
Elsevier B.V.
Citation
Journal of Pharmaceutical and Biomedical Analysis, Vol.149, pp.586-590
Keyword
HomosildenafilHongdenafilHydroxyhomosildenafilLiquid chromatography quadrupole-time of flight mass spectrometrySildenafil analogues metabolites
Mesh Keyword
AnimalsChemistry, PharmaceuticalChromatography, High Pressure LiquidCounterfeit DrugsForensic ToxicologyHumansMaleMicrosomes, LiverPhosphodiesterase 5 InhibitorsRatsRats, Sprague-DawleyReference StandardsSildenafil CitrateTandem Mass SpectrometryUrological Agents
All Science Classification Codes (ASJC)
Analytical ChemistryPharmaceutical ScienceDrug DiscoverySpectroscopyClinical Biochemistry
Abstract
Recently, illegal sildenafil analogues have emerged, causing serious social issues. In spite of the importance of sildenafil analogues, their metabolic profiles or clinical effects have not been reported yet. In this study, new metabolites of illegal sildenafil analogues such as hongdenafil, homosildenafil, and hydroxyhomosildenafil were determined using liquid chromatography quadrupole-time of flight mass spectrometry (LC-Q-TOF-MS) and tandem mass spectrometry (LC-Q-TOF-MS/MS). To prepare metabolic samples, in vitro and in vivo studies were performed. For in vivo metabolites analysis, urine and feces samples of rats treated with sildenafil analogues were analyzed. For in vitro metabolites analysis, human liver microsomes incubated with sildenafil analogues were extracted and analyzed. All metabolites were characterized by LC-Q-TOF-MS and LC-Q-TOF-MS/MS. As a result, five, six, and seven metabolites were determined in hongdenafil, homosildenafil, and hydroxyhomosildenafil treated samples, respectively. These results could be applied to forensic science and other analytical fields. Moreover, these newly identified metabolites could be used as fundamental data to determine the side effect and toxicity of illegal sildenafil analogues.
ISSN
1873-264X
Language
eng
URI
https://aurora.ajou.ac.kr/handle/2018.oak/30035
https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85036532864&origin=inward
DOI
https://doi.org/10.1016/j.jpba.2017.11.057
Journal URL
www.elsevier.com/locate/jpba
Type
Article
Funding
This research was supported by Kyungsung University Research Grants in 2017 .
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