Studies on drug metabolism by use of isotopes XXVI: Determination of urinary metabolites of rutin in humans

1981 ◽  
Vol 70 (7) ◽  
pp. 780-782 ◽  
Author(s):  
Takashi Furuta ◽  
Masanobu Horie ◽  
Shigeo Baba ◽  
Hisashi Nakagawa
Keyword(s):  
Drug Metabolism ◽  
Urinary Metabolites

A validated UPLC-MS/MS method for the determination of urinary metabolites of Uvinul® A plus

2019 ◽  
Vol 411 (30) ◽  
pp. 8143-8152 ◽  
Author(s):  
Markus Stoeckelhuber ◽  
Nikola Pluym ◽  
Franz Bracher ◽  
Edgar Leibold ◽  
Gerhard Scherer ◽  
...  
Keyword(s):  
Urinary Metabolites

scholarly journals Structure Elucidation of Urinary Metabolites of Fentanyl and Five Fentanyl Analogs using LC-QTOF-MS, Hepatocyte Incubations and Synthesized Reference Standards

2020 ◽  
Author(s):  
Jakob Wallgren ◽  
Svante Vikingsson ◽  
Tobias Rautio ◽  
Enas Nasr ◽  
Anna Åstrand ◽  
...  
Keyword(s):  
Urinary Metabolites ◽  
Reference Standards ◽  
Urine Samples ◽  
Data Sets ◽  
Hydroxylated Metabolites ◽  
Flight Mass Spectrometry ◽  
Starting Point ◽  
Fentanyl Analogs ◽  
Hydroxylated Metabolite

Abstract Fentanyl analogs constitute a particularly dangerous group of new psychoactive compounds responsible for many deaths around the world. Little is known about their metabolism, and studies utilizing liquid chromatography quadrupole time-of-flight mass spectrometry (LC-QTOF-MS) analysis of hepatocyte incubations and/or authentic urine samples do not allow for determination of the exact metabolite structures, especially when it comes to hydroxylated metabolites. In this study, seven motifs (2-, 3-, 4- and β-OH as well as 3,4-diOH, 4-OH-3-OMe and 3-OH-4-OMe) of fentanyl and five fentanyl analogs, acetylfentanyl, acrylfentanyl, cyclopropylfentanyl, isobutyrylfentanyl and 4F-isobutyrylfentanyl were synthesized. The reference standards were analyzed by LC-QTOF-MS, which enabled identification of the major metabolites formed in hepatocyte incubations of the studied fentanyls. By comparison with our previous data sets, major urinary metabolites could tentatively be identified. For all analogs, β-OH, 4-OH and 4-OH-3-OMe were identified after hepatocyte incubation. β-OH was the major hydroxylated metabolite for all studied fentanyls, except for acetylfentanyl where 4-OH was more abundant. However, the ratio 4-OH/β-OH was higher in urine samples than in hepatocyte incubations for all studied fentanyls. Also, 3-OH-4-OMe was not detected in any hepatocyte samples, indicating a clear preference for the 4-OH-3-OMe, which was also found to be more abundant in urine compared to hepatocytes. The patterns appear to be consistent across all studied fentanyls and could serve as a starting point in the development of methods and synthesis of reference standards of novel fentanyl analogs where nothing is known about the metabolism.

scholarly journals From Omics to Drug Metabolism and High Content Screen of Natural Product in Zebrafish: A New Model for Discovery of Neuroactive Compound

2012 ◽  
Vol 2012 ◽  
pp. 1-20 ◽  
Author(s):  
Ming Wai Hung ◽  
Zai Jun Zhang ◽  
Shang Li ◽  
Benson Lei ◽  
Shuai Yuan ◽  
...  
Keyword(s):  
Drug Metabolism ◽  
Drug Screening ◽  
Environmental Science ◽  
Pharmacological Action ◽  
Zebrafish Model ◽  
Lead Compounds ◽  
Efficacy Parameters

The zebrafish (Danio rerio) has recently become a common model in the fields of genetics, environmental science, toxicology, and especially drug screening. Zebrafish has emerged as a biomedically relevant model forin vivohigh content drug screening and the simultaneous determination of multiple efficacy parameters, including behaviour, selectivity, and toxicity in the content of the whole organism. A zebrafish behavioural assay has been demonstrated as a novel, rapid, and high-throughput approach to the discovery of neuroactive, psychoactive, and memory-modulating compounds. Recent studies found a functional similarity of drug metabolism systems in zebrafish and mammals, providing a clue with why some compounds are active in zebrafishin vivobut notin vitro, as well as providing grounds for the rationales supporting the use of a zebrafish screen to identify prodrugs. Here, we discuss the advantages of the zebrafish model for evaluating drug metabolism and the mode of pharmacological action with the emerging omics approaches. Why this model is suitable for identifying lead compounds from natural products for therapy of disorders with multifactorial etiopathogenesis and imbalance of angiogenesis, such as Parkinson's disease, epilepsy, cardiotoxicity, cerebral hemorrhage, dyslipidemia, and hyperlipidemia, is addressed.

scholarly journals Structural determination of dog and human urinary metabolites of nipradilol (K-351), a new antihypertensive agent.

1985 ◽  
Vol 33 (8) ◽  
pp. 3456-3468 ◽  
Author(s):  
MITSUO YOSHIMURA ◽  
JUNJI KOJIMA ◽  
TERUFUMI ITO ◽  
JUNNOSUKE SUZUKI
Keyword(s):  
Antihypertensive Agent ◽  
Urinary Metabolites ◽  
Structural Determination
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