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Astatine-211-labeled biotin conjugates resistant to biotinidase for use in pretargeted radioimmunotherapy.

Abstract：

:We 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.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Foulon CF,Alston KL,Zalutsky MR

doi

10.1016/s0969-8051(97)00166-2

subject

Has Abstract

pub_date

1998-02-01 00:00:00

pages

81-8

issue

2

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(97)00166-2

journal_volume

25

pub_type

杂志文章

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