C F Foulon, K L Alston, M R Zalutsky
Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA. cfoulon@duke.edu
Nuclear medicine and biology 1998 FebWe report herein the preparation and biological evaluation of two radioastatinated biotin conjugates, (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide. Both conjugates were stable in the presence of human serum and cerebrospinal fluid as well as murine serum, indicating a resistance to degradation to biotinidase. The normal tissue clearance of (3-[211At]astatobenzoyl)norbiotinamide and ((5-[211At]astato-3-pyridinyl)carbonyl)norbiotinamide was rapid, as observed previously with their iodo analogues. Also reported are the first syntheses of N-succinimidyl 5-[211At]astato-3-pyridinecarboxylate and 3-[211At]astatoaniline, two reagents of potential utility for labeling proteins and peptides with 211At.
C F Foulon, K L Alston, M R Zalutsky. Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy. Nuclear medicine and biology. 1998 Feb;25(2):81-8
PMID: 9468020
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