Further characterization of 4-bromomisonidazole as a potential detector of hypoxic cells

Journal Article · Mon Apr 01 04:00:00 EST 1985 · Radiat. Res.; (United States)

DOI:https://doi.org/10.2307/3576431· OSTI ID:5653371

Rasey, J S; Krohn, K A; Grunbaum, Z; Conroy, P J; Bauer, K; Sutherland, R M

(/sup 14/C)Bromomisonidazole was prepared by direct bromination of (ring-2) (/sup 14/C)misonidazole in dioxane. The uptake and binding of the two labeled sensitizers were compared in vitro in 1-mm EMT-6 spheroids which contain a necrotic core. Using liquid scintillation counting it was shown that spheroids incubated with 50 ..mu..M (/sup 14/C)bromomisonidazole concentrated drug above levels in the medium by 1 1/2 hr and achieved maximum concentration by 10 hr with no further increase at 23 hr. Spheroids incubated with 50 ..mu..M(/sup 14/C)misonidazole may concentrate the sensitizer more slowly but ultimately reached the same fivefold increase over levels in the medium by 23 hr as was observed for bromomisonidazole. Autoradiographs prepared from spheroids after incubation with (/sup 14/C)misonidazole or (/sup 14/C)bromomisonidazole showed silver grains preferentially located over viable hypoxic cells in the inner half of the spheroid rim adjacent to the necrotic center, with lower grain density over nonviable necrotic areas and many fewer grains over oxic cells at the periphery of the spheroid. The data support the potential of radiolabled bromomisonidazole for in vivo imaging pending additional studies of the metabolism of this agent.

• Research Organization: Univ. of Washington, Seattle
• OSTI ID: 5653371
• Journal Information: Radiat. Res.; (United States), Journal Name: Radiat. Res.; (United States) Vol. 102:1; ISSN RAREA
• Country of Publication: United States
• Language: English

Related Subjects

560121* -- Radiation Effects on Cells-- External Source-- (-1987)
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ALKALI METAL ISOTOPES
ANIMAL CELLS
ANOXIA
ANTINEOPLASTIC DRUGS
AUTORADIOGRAPHY
AZOLES
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
CARBON 14 COMPOUNDS
CESIUM 137
CESIUM ISOTOPES
DETECTION
DRUGS
ELECTROMAGNETIC RADIATION
GAMMA RADIATION
HETEROCYCLIC COMPOUNDS
IMIDAZOLES
IN VITRO
IONIZING RADIATIONS
ISOTOPES
LABELLED COMPOUNDS
MISONIDAZOLE
NUCLEI
ODD-EVEN NUCLEI
ORGANIC BROMINE COMPOUNDS
ORGANIC COMPOUNDS
ORGANIC HALOGEN COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
RADIATIONS
RADIOISOTOPES
RADIOSENSITIVITY EFFECTS
RADIOSENSITIZERS
SPHEROIDS
TUMOR CELLS
UPTAKE
YEARS LIVING RADIOISOTOPES