Document Detail

Misonidazole retention by normal tissues: a distinction between label on the ring and side chain.
MedLine Citation:
PMID:  3744949     Owner:  NLM     Status:  MEDLINE    
The retention of misonidazole by mouse normal tissues and EMT6/Ed tumors was studied 24 hr after injection of ring labelled (2-14C) and side chain-labelled (3H) drug. Slightly more 3H than 14C was retained by tumors, but this was considered to be within experimental error of no difference. The ring label (14C) activity retained by tumors was 5-12 times greater than that retained by heart, kidney, brain, muscle and spleen. However, in the same animals, the side chain label (3H) was retained to an appreciably greater extent by the normal tissues, so that the ratio of activities retained in tumors and normal tissues was 3 to 4. This difference in discrimination between tumors and normal tissues implies that gamma-emitting or NMR-active analogues of misonidazole will detect hypoxia in tumors in situ more efficiently, if the active isotope is situated on the ring. The data also indicate that fragmentation products of the metabolism of misonidazole, which contain the side chain and exclude the 2-carbon, are responsible for 50-70% of the misonidazole retained by normal tissues when a side chain-label is used.
A J Franko; B M Garrecht
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  International journal of radiation oncology, biology, physics     Volume:  12     ISSN:  0360-3016     ISO Abbreviation:  Int. J. Radiat. Oncol. Biol. Phys.     Publication Date:  1986 Jul 
Date Detail:
Created Date:  1986-10-08     Completed Date:  1986-10-08     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7603616     Medline TA:  Int J Radiat Oncol Biol Phys     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1259-62     Citation Subset:  IM    
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MeSH Terms
Carbon Radioisotopes
Mice, Inbred BALB C
Misonidazole / metabolism*
Neoplasm Transplantation
Neoplasms, Experimental / metabolism*
Tissue Distribution
Reg. No./Substance:
0/Carbon Radioisotopes; 10028-17-8/Tritium; 13551-87-6/Misonidazole

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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