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Evaluation of meta-[211At]astatobenzylguanidine in an athymic mouse human neuroblastoma xenograft model.

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.
AuthorsG Vaidyanathan, H S Friedman, S T Keir, M R Zalutsky
JournalNuclear medicine and biology (Nucl Med Biol) Vol. 23 Issue 6 Pg. 851-6 (Aug 1996) ISSN: 0969-8051 [Print] United States
PMID8940730 (Publication Type: Comparative Study, Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Antineoplastic Agents
  • Guanidines
  • Iodine Radioisotopes
  • Iodobenzenes
  • 1-(3-astatobenzyl)guanidine
  • 3-Iodobenzylguanidine
  • Astatine
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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