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1-(m-[211At]astatobenzyl)guanidine: synthesis via astato demetalation and preliminary in vitro and in vivo evaluation.

Publication ,  Journal Article
Vaidyanathan, G; Zalutsky, MR
Published in: Bioconjug Chem
1992

No-carrier-added 1-(m-[211At]astatobenzyl)guanidine ([211At]MABG) was synthesized by astato demetalation using two different routes. The overall yield for the two-step approach from 3-(tri-n-butylstannyl)benzylamine was 13%. N-Chlorosuccinimide-mediated astato desilylation of 1-[3-(trimethylsilyl)benzyl]guanidine in acetic acid gave poor yields. In trifluoroacetic acid, the reaction worked well. The radiochemical yield was independent of reaction time and the amount of precursor used; however, the temperature of the reaction had a marked effect. Yields of 85% were obtained in 5 min at 70 degrees C using 0.5 mumol of the precursor. The percentage specific binding in vitro of [211At]MABG was nearly constant over a 2-log activity range and was comparable to that of no-carrier-added [131]MIBG. The accumulation of [211At]MABG in the heart and adrenals of normal mice was similar to that observed for no-carrier-added [131]MIBG.

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Published In

Bioconjug Chem

DOI

ISSN

1043-1802

Publication Date

1992

Volume

3

Issue

6

Start / End Page

499 / 503

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Organic Chemistry
  • Neuroblastoma
  • Neoplasms
  • Mice, Inbred BALB C
  • Mice
  • Iodobenzenes
  • Iodine Radioisotopes
  • Guanidines
 

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Vaidyanathan, G., & Zalutsky, M. R. (1992). 1-(m-[211At]astatobenzyl)guanidine: synthesis via astato demetalation and preliminary in vitro and in vivo evaluation. Bioconjug Chem, 3(6), 499–503. https://doi.org/10.1021/bc00018a006
Vaidyanathan, G., and M. R. Zalutsky. “1-(m-[211At]astatobenzyl)guanidine: synthesis via astato demetalation and preliminary in vitro and in vivo evaluation.Bioconjug Chem 3, no. 6 (1992): 499–503. https://doi.org/10.1021/bc00018a006.
Vaidyanathan, G., and M. R. Zalutsky. “1-(m-[211At]astatobenzyl)guanidine: synthesis via astato demetalation and preliminary in vitro and in vivo evaluation.Bioconjug Chem, vol. 3, no. 6, 1992, pp. 499–503. Pubmed, doi:10.1021/bc00018a006.
Journal cover image

Published In

Bioconjug Chem

DOI

ISSN

1043-1802

Publication Date

1992

Volume

3

Issue

6

Start / End Page

499 / 503

Location

United States

Related Subject Headings

  • Tumor Cells, Cultured
  • Tissue Distribution
  • Organic Chemistry
  • Neuroblastoma
  • Neoplasms
  • Mice, Inbred BALB C
  • Mice
  • Iodobenzenes
  • Iodine Radioisotopes
  • Guanidines