In vitro metabolism of misonidazole.

Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using...

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Detalles Bibliográficos
Autores principales: Josephy, P. D., Palcic, B., Skarsgard, L. D.
Formato: Texto
Lenguaje:English
Publicado: Nature Publishing Group 1981
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2010618/
https://www.ncbi.nlm.nih.gov/pubmed/7236487
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author Josephy, P. D.
Palcic, B.
Skarsgard, L. D.
author_facet Josephy, P. D.
Palcic, B.
Skarsgard, L. D.
author_sort Josephy, P. D.
collection PubMed
description Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using hypoxic mammalian (CHO) cells in vitro. Organic-soluble and acid-soluble metabolites are formed, and radioactivity is bound to macromolecules. The organic-soluble products are separated by TLC and HPLC. Evidence is presented to show that one of the metabolites is hydroxylamino-misonidazole. The significance of metabolic nitroreduction is discussed. IMAGES:
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spelling pubmed-20106182009-09-10 In vitro metabolism of misonidazole. Josephy, P. D. Palcic, B. Skarsgard, L. D. Br J Cancer Research Article Misonidazole (MISO) is a nitroimidazole drug currently undergoing clinical trials as a radiosensitizer of hypoxic tumour cells. The drug is also toxic to such cells, probably because of metabolic activation of the nitro group under hypoxia. The metabolic fate of 14C-labelled MISO is examined, using hypoxic mammalian (CHO) cells in vitro. Organic-soluble and acid-soluble metabolites are formed, and radioactivity is bound to macromolecules. The organic-soluble products are separated by TLC and HPLC. Evidence is presented to show that one of the metabolites is hydroxylamino-misonidazole. The significance of metabolic nitroreduction is discussed. IMAGES: Nature Publishing Group 1981-04 /pmc/articles/PMC2010618/ /pubmed/7236487 Text en https://creativecommons.org/licenses/by/4.0/This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit https://creativecommons.org/licenses/by/4.0/.
spellingShingle Research Article
Josephy, P. D.
Palcic, B.
Skarsgard, L. D.
In vitro metabolism of misonidazole.
title In vitro metabolism of misonidazole.
title_full In vitro metabolism of misonidazole.
title_fullStr In vitro metabolism of misonidazole.
title_full_unstemmed In vitro metabolism of misonidazole.
title_short In vitro metabolism of misonidazole.
title_sort in vitro metabolism of misonidazole.
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2010618/
https://www.ncbi.nlm.nih.gov/pubmed/7236487
work_keys_str_mv AT josephypd invitrometabolismofmisonidazole
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