11C-DPA-713: A Novel Peripheral Benzodiazepine Receptor PET Ligand for In Vivo Imaging of Neuroinflammation

11C-AC-5216: A Novel PET Ligand for Peripheral Benzodiazepine Receptors in the Primate Brain

“…Therefore, AC-5216 might be closer to PK11195 as a pure PBR ligand than DAA1106 and its analogs. More recently, 11 C-DPA-27, with a structure different from that of 11 C-DAA1106 analogs, was developed to visualize PBR in a rat model of neuroinflammation (16). However, to our knowledge, no data about its distribution in the primate brain have been published to date.…”

“…The increase in PBR density has thus been used as an indicator of neuronal damage and neurodenerative disorders, such as Alzheimer's disease (6)(7)(8)(9)(10)(11)(12). These findings have prompted the development of an imaging agent labeled with a radioisotope, which has made it possible to visualize the distribution of PBR in the animal brain, including the human brain (13)(14)(15)(16).…”

Translocator Protein (18 kDa) Polymorphism (rs6971) Explains in-vivo Brain Binding Affinity of the PET Radioligand [18F]-FEPPA

“…The deficiencies of [ 11 C]-PK11195 coupled with the recognized importance of TSPO imaging have fueled considerable efforts to develop radiotracers with greater sensitivity to detect TSPO binding (James et al, 2006;Okubo et al, 2004). While [ 11 C]-PBR28 (Fujita et al, 2008) and [ 11 C]-DPA713 (Boutin et al, 2007) circumvent many of the deficiencies of [ 11 C]-PK11195, both are radiolabeled with the short-lived carbon-11, rendering unsuitable for wide-spread dissemination. The advantages of fluorine-18-labeled radiotracer are several; improved targetry means that [ 18 F]-fluoride can now be produced by low/medium energy cyclotrons in large quantities, the imaging quality of this radionuclide are superior to carbon-11, and most importantly the longer half-life (t 1/2 E 109 minutes), allows shipment to imaging sites distant from the site of production, which is particularly useful for clinical applications.…”

Assessment of Neuroinflammation in Transferred EAE Via a Translocator Protein Ligand

“…Although [ 11 C]-(R)-PK11195 is widely used for imaging of microglia, its considerable high plasma protein binding, high levels of nonspecific binding, relatively poor blood-brain barrier permeability and short half-life, limits its use in brain imaging (Chauveau et al, 2008). Recently, alternative PET radioligands for TSPO including the phenoxyarylacetamide derivative [ 11 C]-DAA1106 and its analogues (Gulyas et al, 2009;Takano et al, 2010;Venneti et al, 2008), the imidazopyridines (PBR111) and its analogues (Boutin et al, 2007a;Fookes et al, 2008) (Boutin et al, 2007b;James et al, 2008) have been investigated.…”