Preparation and preliminary evaluation of 4-[211At]astato-N-piperidinoethyl benzamide.
Nucl Med Biol
; 22(4): 467-73, 1995 May.
Article
in En
| MEDLINE
| ID: mdl-7550023
ABSTRACT
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Piperidines
/
Benzamides
/
Astatine
/
Antineoplastic Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Nucl Med Biol
Journal subject:
BIOLOGIA
/
MEDICINA NUCLEAR
Year:
1995
Document type:
Article
Affiliation country: