Toward molecular imaging of the free fatty acid receptor 1.

ABSTRACT:

Aims

Molecular imaging of the free fatty acid receptor 1 (FFAR1) would be a valuable tool for drug development by enabling in vivo target engagement studies in human. It has also been suggested as a putative target for beta cell imaging, but the inherent lipophilicity of most FFAR1 binders produces high off-target binding, which has hampered progress in this area. The aim of this study was to generate a suitable lead compound for further PET labeling.

Methods

In order to identify a lead compound for future PET labeling for quantitative imaging of FFAR1 in human, we evaluated tritiated small molecule FFAR1 binding probes ([³H]AZ1, [³H]AZ2 and [³H]TAK-875) for their off-target binding, receptor density and affinity in human pancreatic tissue (i

SUBMITTER: Hellstrom-Lindahl E 

PROVIDER: S-EPMC5486603 | biostudies-literature | 2017 Jul

REPOSITORIES: biostudies-literature