Characterization of [¹¹C]Lu AE92686 as a PET radioligand for phosphodiesterase 10A in the nonhuman primate brain.

ABSTRACT:

Purpose

[¹¹C]Lu AE92686 is a positron emission tomography (PET) radioligand that has recently been validated for examining phosphodiesterase 10A (PDE10A) in the human striatum. [¹¹C]Lu AE92686 has high affinity for PDE10A (IC ₅₀ = 0.39 nM) and may also be suitable for examination of the substantia nigra, a region with low density of PDE10A. Here, we report characterization of regional [¹¹C]Lu AE92686 binding to PDE10A in the nonhuman primate (NHP) brain.

Methods

A total of 11 PET measurements, seven baseline and four following pretreatment with unlabeled Lu AE92686 or the structurally unrelated PDE10A inhibitor MP-10, were performed in five NHPs using a high resolution research tomograph (HRRT). [¹¹C]Lu AE92686 binding w

SUBMITTER: Yang KC 

PROVIDER: S-EPMC5215309 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature