Preparation and preliminary evaluation of 4-[211At]astato-N-piperidinoethyl benzamide.

Journal Article (Journal Article)

The potential therapeutic agent, 4-[211At]astato-N-piperidinoethyl benzamide (4-APAB) was synthesized via a halodestannylation reaction. Radiochemical yields were 69% for a 5 min reaction and reached 74% by 25 min, whereas 82% radiochemical yields were obtained under similar reaction conditions for radioiodination. A simplified procedure was adopted for the purification of the target compound. In vitro binding of 4-APAB to SK-MEL 28 melanoma and D247 glioma cell lines was 20.7 +/- 1.3% and 12.2 +/- 1.3%, respectively. In comparison, binding of 4-[131I]iodo-N-piperidinoethyl benzamide (4-IPAB) to SK-Mel 28 cells was 13.9 +/- 1.9%. Paired label biodistribution studies were performed in normal Balb/c mice using 4-IPAB and 4-APAB. Thyroid uptake at 1, 2, and 6 h was significantly higher for 4-APAB. Differences in liver accumulation between the two compounds were small but statistically significant at most time points. A higher accumulation of 211At compared with 131I was observed in lungs and spleen at all time points studied. These results indicate that 4-APAB is not stable in vivo, suggesting the need for a better sigma receptor ligand for use in 211At.

Full Text

Duke Authors

Cited Authors

  • Garg, PK; John, CS; Zalutsky, MR

Published Date

  • May 1995

Published In

Volume / Issue

  • 22 / 4

Start / End Page

  • 467 - 473

PubMed ID

  • 7550023

International Standard Serial Number (ISSN)

  • 0969-8051

Digital Object Identifier (DOI)

  • 10.1016/0969-8051(94)00134-6


  • eng

Conference Location

  • United States