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

Publication ,  Journal Article
Vaidyanathan, G; Strickland, DK; Zalutsky, MR
Published in: Int J Cancer
June 15, 1994

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.

Duke Scholars

Published In

Int J Cancer

DOI

ISSN

0020-7136

Publication Date

June 15, 1994

Volume

57

Issue

6

Start / End Page

908 / 913

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Tetrabenazine
  • Reserpine
  • Oncology & Carcinogenesis
  • Mice, Inbred BALB C
  • Mice
  • Iodobenzenes
  • In Vitro Techniques
  • Humans
 

Citation

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Vaidyanathan, G., Strickland, D. K., & Zalutsky, M. R. (1994). Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent. Int J Cancer, 57(6), 908–913. https://doi.org/10.1002/ijc.2910570622
Vaidyanathan, G., D. K. Strickland, and M. R. Zalutsky. “Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent.Int J Cancer 57, no. 6 (June 15, 1994): 908–13. https://doi.org/10.1002/ijc.2910570622.
Vaidyanathan G, Strickland DK, Zalutsky MR. Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent. Int J Cancer. 1994 Jun 15;57(6):908–13.
Vaidyanathan, G., et al. “Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent.Int J Cancer, vol. 57, no. 6, June 1994, pp. 908–13. Pubmed, doi:10.1002/ijc.2910570622.
Vaidyanathan G, Strickland DK, Zalutsky MR. Meta-[211At]astatobenzylguanidine: further evaluation of a potential therapeutic agent. Int J Cancer. 1994 Jun 15;57(6):908–913.
Journal cover image

Published In

Int J Cancer

DOI

ISSN

0020-7136

Publication Date

June 15, 1994

Volume

57

Issue

6

Start / End Page

908 / 913

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Tetrabenazine
  • Reserpine
  • Oncology & Carcinogenesis
  • Mice, Inbred BALB C
  • Mice
  • Iodobenzenes
  • In Vitro Techniques
  • Humans