• Title/Summary/Keyword: lactamization

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Analysis of Amineptine and its Metabolites in Human Urine by Gas Chromatography/Mass Spectrometry (Gas Chromatography/Mass Spectrometry를 이용한 뇨중 Amineptine과 그 대사체 분석방법에 관한 연구)

  • Lee, Jeong Ae;Kim, Younglim;Lho, Dong-Seok
    • Analytical Science and Technology
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    • v.13 no.3
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    • pp.385-393
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    • 2000
  • A gas chromatography-mass spectrometric (GC/MS) procedure for the determination of amineptine (dihydro-10, 11-dibenzo[a, d] cycloheptenyl-5-amino-7-heptanoic acid) and its main metabolites in human urine was described. Amineptine has been known to be extensively metabolized by the ${\beta}$-oxidation of the heptanoic side chain with formation of pentanoic side chain metabolite ($C_5$-metabolite), and lactamizarion by internal dehydration of (${\beta}$-oxidized metabolite (${\delta}$-lactam). The detection of these compounds was based on acid hydrolysis, liquid-liquid extraction and trimethylsilylated derivatization of the carboxylic acid group. For the determination of amineptine and its metabolites in biological fluids, selected ions at the m/ 192, molecular ion and one of the characteristic ions were monitored by GC/MS. On the excretion study of amineptine in human urine, 70-90% of amineptine, ${\delta}$-lactam, and $C_5$-metabolite were found to be excreted within 4 hours and their excretion completed within 20 hours.

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