Preparation and biological evaluation of an astatine-211 labeled biotin conjugate: biotinyl-3-[211 At]astatoanilide.
Biotinyl-3-[211 At]astatoanilide ([211 At]AtBA) was prepared in more than 80% yield by destannylation. In vitro, [211 At]AtBA exhibited a high affinity for streptavidin, and was stable after incubation in human serum, cerebrospinal fluid and distilled water, whereas it was rapidly degraded in mouse serum. HPLC analysis showed that the main degradation pathway in mouse serum was the cleavage of [211 At]astatoaniline. In mice, [211 At]AtBA and its 125I-labeled analogue cleared rapidly from most tissues; however, there was some evidence for dehalogenation of both tracers.
Foulon
C F
CF
Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA. cfoulon@acpub.duke.edu
Schoultz
B W
BW
Zalutsky
M R
MR
D000818:Animals; D001246:Astatine / Q000097:blood / Q000134:cerebrospinal fluid / Q000493:pharmacokinetics*; D001710:Biotin / Q000031:analogs & derivatives* / Q000097:blood / Q000138:chemical synthesis / Q000493:pharmacokinetics; D001711:Biotransformation; D004355:Drug Stability; D006801:Humans; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics; D007700:Kinetics; D051379:Mice; D013997:Time Factors; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; C106108:biotinyl-3-astatoanilide; D001710:Biotin; D001246:Astatine