Mixed-Affinity Binding in Humans with 18-kDa Translocator Protein Ligands

• Published in: Journal of Nuclear Medicine Vol. 52; no. 1; pp. 24 - 32
• Main Authors: Owen, David R.J., Gunn, Roger N., Rabiner, Eugenii A., Bennacef, Idriss, Fujita, Masahiro, Kreisl, William C., Innis, Robert B., Pike, Victor W., Reynolds, Richard, Matthews, Paul M., Parker, Christine A.
• Format: Journal Article
• Language: English
• Published: United States Society of Nuclear Medicine 01.01.2011
• Subjects: Acetamides - metabolism; Binding sites; Binding, Competitive; Brain - metabolism; Carbon Radioisotopes; Human subjects; Humans; Independent sample; Isoquinolines - metabolism; Molecular Weight; Multiple sclerosis; Positron-Emission Tomography; Pyridines - metabolism; Radioligand Assay - methods; Receptors, GABA - analysis

11C-PBR28 PET can detect the 18-kDa translocator protein (TSPO) expressed within macrophages. However, quantitative evaluation of the signal in brain tissue from donors with multiple sclerosis (MS) shows that PBR28 binds the TSPO with high affinity (binding affinity [Ki], ∼4 nM), low affinity (Ki, ∼...