| Metabolism of the new ribonucleotide reductase inhibitor amidox in the isolated perfused rat liver. | |
| | |
MedLine Citation:
|
PMID: 11131656 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
BACKGROUND: Amidox (AX) is a novel anticancer drug currently undergoing pre-clinical studies. Though AX shows activity against various tumor cells, its biotransformation is still unknown. MATERIAL AND METHODS: Livers of male Wistar and mutant TR- rats were perfused with AX in a single pass system and bile and effluent perfusate analyzed by HPLC for AX and its metabolites. RESULTS: In bile, seven biotransformation products but not AX could be quantified though their total excretion into bile was low. However, the cumulative efflux of AX metabolites into the effluent perfusate was high with about 55% of AX applied to the liver during perfusion. Biliary excretion of AX metabolites in TR- rats was substantially reduced compared to Wistar rats, indicating that metabolites are substrates of the canalicular multispecific organic anion transporter cmoat. CONCLUSION: Metabolism of AX in rat liver is high and has to be considered during cancer therapy of patients. |
| | |
Authors:
|
A Salamon; E Vielnascher; B Hagenauer; T Szekeres; M Szekeres-Fritzer; T Thalhammer; W Jäger |
Related Documents
:
|
2088746 - The effect of mono(2-ethylhexyl)phthalate on an isolated perfused rat heart-lung prepar... 2012206 - Aldosterone metabolism in combined isolated perfused rat liver and kidney. 11979566 - Proton magnetization transfer effect in rat liver lactate. 1201006 - Effect of 3-mercaptopicolinic acid on gluconeogenesis and gluconeogenic metabolite conc... 935186 - Lipophilic and respiratory properties of nadh and succinate dehydrogenase sites in mito... 15098936 - Striatal damage and oxidative stress induced by the mitochondrial toxin malonate are re... |
Publication Detail:
|
Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
|
Title: Anticancer research Volume: 20 ISSN: 0250-7005 ISO Abbreviation: Anticancer Res. Publication Date: 2000 Sep- Oct |
Date Detail:
|
Created Date: 2000-12-21 Completed Date: 2001-01-04 Revised Date: 2006-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 8102988 Medline TA: Anticancer Res Country: Greece |
Other Details:
|
Languages: eng Pagination: 3521-6 Citation Subset: IM |
Affiliation:
|
Institute of Pharmaceutical Chemistry, University of Vienna, Althanstrasse 14, A-1090 Vienna, Austria. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Animals Anion Transport Proteins Antineoplastic Agents / metabolism, pharmacokinetics* Bile / metabolism Biotransformation Carrier Proteins / genetics, metabolism Chromatography, High Pressure Liquid Drug Resistance, Neoplasm Enzyme Inhibitors / metabolism, pharmacokinetics Liver / metabolism* Male Oximes / metabolism, pharmacokinetics* Perfusion Rats Rats, Mutant Strains Rats, Wistar Ribonucleotide Reductases / antagonists & inhibitors |
| Chemical | |
Reg. No./Substance:
|
0/Anion Transport Proteins; 0/Antineoplastic Agents; 0/Carrier Proteins; 0/Enzyme Inhibitors; 0/Oximes; 95933-72-5/Amidox; EC 1.17.4.-/Ribonucleotide Reductases |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Hyaluronidase-induced periodic modulation of the interstitial fluid pressure increases selective ant...
Next Document: Dual effects of four members of the fibroblast growth factor member family on multiplication and mot...