Comparison of binding of (/sup 3/H)misonidazole and (/sup 14/C)misonidazole in multicell spheroids
Uptake of (2-ring-/sup 14/C)misonidazole and (/sup 3/H)misonidazole with tritium in the side chain has been compared in 1-mm EMT-6/UW spheroids using liquid scintillation counting and autoradiography. The uptake of both labeled sensitizers as a function of incubation time was virtually identical. Uptake by the spheroids exceeded levels in the medium by 1 1/2 to 2 hr and was well modeled as a first-order binding process. The similar uptake of the two versions of this sensitizer labeled in different positions suggests that the metabolic actions which allow the drug to bind in hypoxic cells do not principally involve metabolites which separate the number 2 carbon of the imidazole ring from the side chain. The pattern of silver grains in autoradiographs was similar for both labeled sensitizers, with most labeled drug bound in an intermediate zone of cells between the necrotic center and the actively proliferating rim of the spheroids. The superior resolution possible with the tritiated compound showed that both nucleus and cytoplasm in viable looking cells were labeled while pycnotic cells were not labeled.
- Research Organization:
- Univ. of Washington, Seattle
- OSTI ID:
- 5828447
- Journal Information:
- Radiat. Res.; (United States), Journal Name: Radiat. Res.; (United States) Vol. 101:3; ISSN RAREA
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
62 RADIOLOGY AND NUCLEAR MEDICINE
ANIMAL CELLS
ANOXIA
ANTINEOPLASTIC DRUGS
AUTORADIOGRAPHY
AZOLES
CARBON 14 COMPOUNDS
CONNECTIVE TISSUE CELLS
COUNTING TECHNIQUES
DRUGS
FIBROBLASTS
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
LABELLED COMPOUNDS
MISONIDAZOLE
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIATION DOSE DISTRIBUTIONS
RADIOSENSITIZERS
SCINTILLATION COUNTING
SOMATIC CELLS
SPATIAL DOSE DISTRIBUTIONS
SPHEROIDS
TRITIUM COMPOUNDS
UPTAKE