The administration of radiolabeled compounds with gamma-emitting radionucli
des allows real time pursuit of in vivo behavior of the compounds by extern
al counting of the radioactivity. If the compounds possess a specific local
ization mechanism to target tissue, the image reflects the specific functio
n of the target. This technique has widely been applied in diagnostic nucle
ar medicine combined with appropriate radionuclides for clinical use. Two s
trategies have been developed to design radiolabeled compounds for targeted
imaging. One constitutes tethering radiolabeled compounds to carrier molec
ules that possess specific localization mechanisms to target tissue. Anothe
r approach constitutes chemical design of radiolabeled compounds, especiall
y metallic compounds, that possess specific localization characteristics to
the target per se. In this manuscript, progress of chemical design of radi
olabeled compounds for targeted imaging is briefly reviewed. Emphasis is la
id on chemical design of radiolabeled antibodies for targeted imaging. (C)
1999 Elsevier Science B.V. All rights reserved.