PET imaging of brain macrophages using the peripheral benzodiazepine receptor in a macaque model of neuroAIDS

Targeted Imaging of Colonic Tumors in Smad3−/− Mice Discriminates Cancer and Inflammation

“…The role of inflammation in cancer development is an area of intense investigation (2,3). Previous studies have shown a high level of PBR expression in activated macrophages associated with inflammation (13,25), so it was important for us to rule out nonspecific retention of the targeted agent related to tumorassociated inflammatory processes. We found that retention profiles of NIR-conPK11195 discriminated between mice treated with DSS and tumor-bearing mice at times between 8 and 13 h postadministration (Fig.…”

“…PBR is primarily associated with mitochondrial steroidogenesis and has been shown to be up-regulated in the epithelial component of cancers of the colon, breast, and prostate (10), as well as in activated macrophages in the brain (11,12). The PBR synthetic ligand, PK11195, has been used clinically to image inflammation associated with several neurologic diseases (13)(14)(15). Con-PK11195, an analogue of the widely used PBR ligand PK11195, was recently prepared (16) and shown to be useful as a targeting agent for fluorescent probes as well as bimodal lanthanide chelate-imaging agents (17).…”

The high affinity peripheral benzodiazepine receptor ligand DAA1106 binds to activated and infected brain macrophages in areas of synaptic degeneration: Implications for PET imaging of neuroinflammation in lentiviral encephalitis

“…We and others have shown that activated brain macrophages can be labeled with [ 3 H](R)-PK11195 in SIVE (Mankowski et al, 2003, Venneti et al, 2004 and that [ 11 C](R)-PK11195 can be used to image activated brain macrophages in vivo using PET in macaques that develop encephalitis (Venneti et al, 2004). However, translation of these studies to human subjects has been less promising.…”

Evaluation of Reference Tissue Models for the Analysis of [11C](R)-PK11195 Studies

“…Both [ 11 C](R)-PK11195 and [ 11 C]PK11195 have been used as positron emmision tomography (PET) tracers to study activated microglia in various neurologic disorders. It has been used to study stroke (Ramsay et al, 1992;Pappata et al, 2000;Gerhard et al, 2000Gerhard et al, , 2005a), Alzheimer's disease (Groom et al, 1995; Cagnin et al, 2001a;Versijpt et al, 2003), multiple sclerosis (Banati et al, 2000;Debruyne et al, 2002Debruyne et al, , 2003Versijpt et al, 2005) and various other diseases (Pappata et al, 1991; Banati et al, 1999Banati et al, , 2001Goerres et al, 2001;Cagnin et al, 2001bCagnin et al, , 2004Cicchetti et al, 2002;Gerhard et al, 2003Gerhard et al, , 2004Gerhard et al, , 2005bTurner et al, 2004Turner et al, , 2005Venneti et al, 2004;Henkel et al, 2004;Ouchi et al, 2005). Most studies have used a reference tissue approach to quantify binding, either by applying the simplified reference tissue model (SRTM) (Lammertsma and Hume, 1996) or by using uptake normalized to a reference region.…”