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Society of Nuclear Medicine, Journal of Nuclear Medicine, 1(52), p. 24-32, 2010

DOI: 10.2967/jnumed.110.079459

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

Journal article published in 2010 by Drj R. J. Owen, Roger N. Gunn, Ea A. Rabiner, Idriss Bennacef, Masahiro Fujita, Wc C. Kreisl, Rb B. Innis, Vw W. Pike, Richard Reynolds ORCID, Pm M. Matthews ORCID, Ca A. Parker
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

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, ~200 nM), or mixed affinity (2 sites with Ki, ~4 nM and ~300 nM). Our study tested whether similar binding behavior could be detected in brain tissue from donors with no history of neurologic disease, with TSPO-binding PET ligands other than 11C-PBR28, for TSPO present in peripheral blood, and with human brain PET data acquired in vivo with 11C-PBR28.