NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID

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NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID. / Tjornelund, J.; Hansen, S. H.; Cornett, Claus.

In: Xenobiotica, Vol. 21, No. 5, 1991, p. 605-612.

Research output: Contribution to journalJournal articleResearchpeer-review

Harvard

Tjornelund, J, Hansen, SH & Cornett, C 1991, 'NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID', Xenobiotica, vol. 21, no. 5, pp. 605-612.

APA

Tjornelund, J., Hansen, S. H., & Cornett, C. (1991). NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID. Xenobiotica, 21(5), 605-612.

Vancouver

Tjornelund J, Hansen SH, Cornett C. NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID. Xenobiotica. 1991;21(5):605-612.

Author

Tjornelund, J. ; Hansen, S. H. ; Cornett, Claus. / NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID. In: Xenobiotica. 1991 ; Vol. 21, No. 5. pp. 605-612.

Bibtex

@article{afa60896ed704295b78f393fb2c2455b,
title = "NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID",
abstract = "1. A new metabolite of the drug 5-aminosalicylic acid (5-ASA) has been found in urine from pigs and in plasma of humans. The metabolite has been isolated from pig urine using an XAD-2 column and purified using preparative h.p.l.c. 2. The metabolite has been identified as N-formyl-5-ASA (5-formamidosalicylic acid) using H-1- and C-13-n.m.r. spectrometry and mass spectroscopy and the structure was confirmed by chemical synthesis. 3. N-Formyl-5-ASA is stable in human plasma and in potassium phosphate buffers between pH 3.0 and 9.0. It is hydrolysed below pH 3.0. 4. N-Formyl-5-ASA was readily formed in rat liver homogenate when 5-ASA and N-formyl-L-kynurenine were added. Thus N-formyl-5-ASA might be formed by the actions of formamidase in vivo. 5. N-Formyl-5-ASA has been found in human plasma from healthy volunteers dosed i.v. with 5-ASA (250 mg). N-beta-D-glucopyranosyl-5-ASA, N-acetyl-5-ASA and N-formyl-5-ASA were quantified in human plasma using a h.p.l.c. assay.",
keywords = "4-formylaminoantipyrine biotransformation 1-nitropyrene aminopyrine invivo rat",
author = "J. Tjornelund and Hansen, {S. H.} and Claus Cornett",
year = "1991",
language = "Udefineret/Ukendt",
volume = "21",
pages = "605--612",
journal = "Xenobiotica",
issn = "0049-8254",
publisher = "Taylor & Francis",
number = "5",

}

RIS

TY - JOUR

T1 - NEW METABOLITES OF THE DRUG 5-AMINOSALICYLIC ACID .2. N-FORMYL-5-AMINOSALICYLIC ACID

AU - Tjornelund, J.

AU - Hansen, S. H.

AU - Cornett, Claus

PY - 1991

Y1 - 1991

N2 - 1. A new metabolite of the drug 5-aminosalicylic acid (5-ASA) has been found in urine from pigs and in plasma of humans. The metabolite has been isolated from pig urine using an XAD-2 column and purified using preparative h.p.l.c. 2. The metabolite has been identified as N-formyl-5-ASA (5-formamidosalicylic acid) using H-1- and C-13-n.m.r. spectrometry and mass spectroscopy and the structure was confirmed by chemical synthesis. 3. N-Formyl-5-ASA is stable in human plasma and in potassium phosphate buffers between pH 3.0 and 9.0. It is hydrolysed below pH 3.0. 4. N-Formyl-5-ASA was readily formed in rat liver homogenate when 5-ASA and N-formyl-L-kynurenine were added. Thus N-formyl-5-ASA might be formed by the actions of formamidase in vivo. 5. N-Formyl-5-ASA has been found in human plasma from healthy volunteers dosed i.v. with 5-ASA (250 mg). N-beta-D-glucopyranosyl-5-ASA, N-acetyl-5-ASA and N-formyl-5-ASA were quantified in human plasma using a h.p.l.c. assay.

AB - 1. A new metabolite of the drug 5-aminosalicylic acid (5-ASA) has been found in urine from pigs and in plasma of humans. The metabolite has been isolated from pig urine using an XAD-2 column and purified using preparative h.p.l.c. 2. The metabolite has been identified as N-formyl-5-ASA (5-formamidosalicylic acid) using H-1- and C-13-n.m.r. spectrometry and mass spectroscopy and the structure was confirmed by chemical synthesis. 3. N-Formyl-5-ASA is stable in human plasma and in potassium phosphate buffers between pH 3.0 and 9.0. It is hydrolysed below pH 3.0. 4. N-Formyl-5-ASA was readily formed in rat liver homogenate when 5-ASA and N-formyl-L-kynurenine were added. Thus N-formyl-5-ASA might be formed by the actions of formamidase in vivo. 5. N-Formyl-5-ASA has been found in human plasma from healthy volunteers dosed i.v. with 5-ASA (250 mg). N-beta-D-glucopyranosyl-5-ASA, N-acetyl-5-ASA and N-formyl-5-ASA were quantified in human plasma using a h.p.l.c. assay.

KW - 4-formylaminoantipyrine biotransformation 1-nitropyrene aminopyrine invivo rat

M3 - Tidsskriftartikel

VL - 21

SP - 605

EP - 612

JO - Xenobiotica

JF - Xenobiotica

SN - 0049-8254

IS - 5

ER -

ID: 38062419