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[111In]5-[(3aR,6S,6aS)-2-Oxo-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-6-yl]pentanoic acid.


Chopra A.


Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2008 May 01 [updated 2008 May 28].


White blood cells (WBCs) labeled with radioactive gallium (67Ga), indium (111In), or technetium (99mTc) are often used for the detection of infections, but this application of WBCs is laborious and requires the use of autologous WBCs, which increases the probability of introducing an infection (1). In addition, this technique may not detect all types of infections. Although computed tomography (CT) and magnetic resonance imaging (MRI) are often used to characterize an infection or inflammation, these techniques also have limitations. CT cannot be used at frequent intervals because it requires the use of high radiation doses, and MRI has a low sensitivity to detect infections during early stages until major pathological changes occur (2). Polyclonal immunoglobulins and albumin labeled with 67Ga, or 111In, or 99mTc have also been used for the detection of infections and inflammation, but these proteins clear very slowly from circulation, tend to accumulate in the liver, and are not suitable for the early detection of infection or inflammation (3). The technique of pretargeting with a bifunctional antibody followed by the administration of an appropriate radiolabeled ligand was used successfully to image tumors in mice (4). Rusckowski et al. used a similar approach for the detection of infection and administered 111In-labeled biotin to animals a few hours after pretreatment with unlabeled streptavidin, a 65-kDa protein (5). Streptavidin is assumed to accumulate at the site of infection/inflammation because of increased vascularity and vascular permeability. Subsequent administration of 111In-biotin leads to the accumulation of radioactivity at the site of infection or inflammation because biotin has a very strong affinity (dissociation constant = 10-15) for streptavidin (6). Free 111In-biotin is secreted through the kidneys, whereas a complex of 111In-biotin and streptavidin not bound at the site of infection or inflammation is secreted through the hepatobiliary system (6). This technique was used successfully for the detection of infections after prosthetic vascular graft (3, 7) and osteomyelitis (8), including that of the vertebra (9). Although the components used to prepare 111In-biotin and perform this work in humans are available commercially, Lazzeri et al. have stated that the technique is not approved for this indication by the United States Food and Drug Administration (9). It is pertinent to mention streptavidin and avidin are both targets of biotin. Streptavidin is produced by Streptomyces avidinii whereas avidin is found in avian eggs, but both have been used for the detection of infections (see sections below).

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