Abstract |
A paired-label biodistribution was performed in athymic mice bearing SK-N-SH human neuroblastoma xenografts to compare the tissue uptake of meta-[211At]astatobenzylguanidine ([ 211At]MABG) and [131I] MIBG. Significantly higher (p < 0.05) uptake of [ 211At]MABG was seen in tumor (3.8 +/- 0.8% ID/g vs. 3.1 +/- 0.7% ID/g at 8 h) compared to [131I] MIBG. Desipramine reduced tumor uptake of [ 211At] MABG by 43%, suggesting that its accumulation was related to the specific uptake-1 mechanism. Higher uptake of [ 211At]MABG was also seen in normal tissue targets such as heart (6.0 +/- 0.9% ID/g vs. 4.5 +/- 0.8% ID/g at 8 h; p < 0.05). Pretreatment of mice with unlabeled MIBG increased tumor uptake of [ 211At]MABG by 1.5-fold while reducing uptake in heart and several other normal tissues. The vesicular uptake inhibitor tetrabenazine reduced heart uptake by 30% without reducing the tumor uptake. These results suggest such strategies might be useful for improving [ 211At]MABG tumor-to-normal tissue ratios.
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Authors | G Vaidyanathan, H S Friedman, S T Keir, M R Zalutsky |
Journal | Nuclear medicine and biology
(Nucl Med Biol)
Vol. 23
Issue 6
Pg. 851-6
(Aug 1996)
ISSN: 0969-8051 [Print] United States |
PMID | 8940730
(Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, P.H.S.)
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Chemical References |
- Antineoplastic Agents
- Guanidines
- Iodine Radioisotopes
- Iodobenzenes
- 1-(3-astatobenzyl)guanidine
- 3-Iodobenzylguanidine
- Astatine
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Topics |
- 3-Iodobenzylguanidine
- Animals
- Antineoplastic Agents
(pharmacokinetics)
- Astatine
- Disease Models, Animal
- Female
- Guanidines
(pharmacokinetics)
- Humans
- Iodine Radioisotopes
- Iodobenzenes
(pharmacokinetics)
- Male
- Mice
- Mice, Inbred BALB C
- Mice, Nude
- Neoplasm Transplantation
- Neuroblastoma
(metabolism)
- Tissue Distribution
- Transplantation, Heterologous
- Tumor Cells, Cultured
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