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Titolo:
Liquid chromatography-tandem mass spectrometry identification of metabolites of two 5-HT1A antagonists, N-{2-[4-(2-methoxylphenyl)piperazino]ethyl}-N-(2-pyridyl) trans- and cis-4-fluorocyclohexanecarboxamide, produced by human and rat hepatocytes
Autore:
Ma, Y; Lang, LX; Kiesewetter, DO; Jagoda, E; Sassaman, MB; Der, M; Eckelman, WC;
Indirizzi:
NIH, PET Dept, Warren G Magnuson Clin Ctr, Bethesda, MD 20892 USA NIH Bethesda MD USA 20892 ren G Magnuson Clin Ctr, Bethesda, MD 20892 USA
Titolo Testata:
JOURNAL OF CHROMATOGRAPHY B
fascicolo: 1-2, volume: 755, anno: 2001,
pagine: 47 - 56
SICI:
1387-2273(20010505)755:1-2<47:LCMSIO>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
RADIOACTIVE METABOLITES; RECEPTOR RADIOLIGAND; HUMAN PLASMA; MONKEY; PET;
Keywords:
5-HT1A antagonists;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
10
Recensione:
Indirizzi per estratti:
Indirizzo: Ma, Y NIH, PET Dept, Warren G Magnuson Clin Ctr, 10 Ctr Dr MSC 1180, Bethesda, MD 20892 USA NIH 10 Ctr Dr MSC 1180 Bethesda MD USA 20892 Bethesda, MD 20892 USA
Citazione:
Y. Ma et al., "Liquid chromatography-tandem mass spectrometry identification of metabolites of two 5-HT1A antagonists, N-{2-[4-(2-methoxylphenyl)piperazino]ethyl}-N-(2-pyridyl) trans- and cis-4-fluorocyclohexanecarboxamide, produced by human and rat hepatocytes", J CHROMAT B, 755(1-2), 2001, pp. 47-56

Abstract

Two 5-HT1A antagonists, t-FCWAY and c-FCWAY, were developed as imaging agents for positron emission tomography (PET). In order to evaluate these compounds, hepatocytes from both human and rat were utilized to produce metabolites and LC-MS-MS was used to identify metabolites. These in vitro metabolism studies indicate that hydrolysis of the amide linkage is the major metabolism pathway for humans, whereas aromatic ring-oxidation is the major metabolism pathway for rat. The rat hepatocyte results correlate well with in vivo rat metabolism studies. Based on the structures of the metabolites, we have developed an extraction procedure to determine the concentration of the parent compound in plasma. Published by Elsevier Science B.V.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/20 alle ore 21:25:19