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Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent.

Abstract
Meta-[211At]astatobenzylguanidine ([211At]MABG) is an astatinated analogue of meta-iodobenzylguanidine (MIBG) that could be of value for therapeutic applications. The initial goal of this study was to determine whether [211At]MABG is taken up, like MIBG, by a specific uptake-I mechanism. Norepinephrine and desipramine (DMI) decreased [211At]MABG uptake in SK-N-SH human neuroblastoma cells. This uptake was found to be energy-dependent: In mice, pre-treatment with DMI reduced uptake of [211At]MABG at 1 hr post-injection in the adrenal and in the heart. Tetrabenazine at a dose of 40 mg/kg reduced uptake of [211At]MABG in the mouse heart in vivo (69% of control) whereas up to 100 microM of tetrabenazine did not affect the in vitro uptake of [211At]MABG in SK-N-SH cells. In SK-N-SH cells, 53% and 38%, respectively, of the initial uptake of [211At]MABG was retained at 4 hr and 6 hr. For no-carrier-added (n.c.a.) [131I]MIBG these values were similar, 60% and 48%. The ability of SK-N-SH cells to incorporate [3H]thymidine was reduced to less than 50% of control values when treated with as little as 3.2 nCi of [211At]MABG. In contrast, no significant reduction in the thymidine uptake was observed, even with 80 nCi of n.c.a. MIBG.
AuthorsG Vaidyanathan, D K Strickland, M R Zalutsky
JournalInternational journal of cancer (Int J Cancer) Vol. 57 Issue 6 Pg. 908-13 (Jun 15 1994) ISSN: 0020-7136 [Print] United States
PMID8206683 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)
Chemical References
  • Antineoplastic Agents
  • Guanidines
  • Iodobenzenes
  • 1-(3-astatobenzyl)guanidine
  • 3-Iodobenzylguanidine
  • Reserpine
  • Astatine
  • Tetrabenazine
Topics
  • 3-Iodobenzylguanidine
  • Animals
  • Antineoplastic Agents (metabolism)
  • Astatine (administration & dosage)
  • Biological Transport
  • Guanidines (metabolism)
  • Humans
  • In Vitro Techniques
  • Iodobenzenes (metabolism)
  • Mice
  • Mice, Inbred BALB C
  • Reserpine (pharmacology)
  • Tetrabenazine (pharmacology)
  • Tissue Distribution
  • Tumor Cells, Cultured

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