First in human evaluation of [¹⁸F]PK-209, a PET ligand for the ion channel binding site of NMDA receptors.

ABSTRACT:

Background

Efforts to develop suitable positron emission tomography (PET) tracers for the ion channel site of human N-methyl-D-aspartate (NMDA) receptors have had limited success. [¹⁸F]PK-209 is a GMOM derivative that binds to the intrachannel phencyclidine site with high affinity and selectivity. Primate PET studies have shown that the volume of distribution in the brain was reduced by administration of the NMDA receptor antagonist MK-801, consistent with substantial specific binding. The purpose of the present study was to evaluate [¹⁸F]PK-209 in 10 healthy humans by assessing test-retest reproducibility and binding specificity following intravenous S-ketamine administration (0.5 mg ∙ kg^-1). Five healthy subjects underwent a test-retest protocol,

SUBMITTER: van der Aart J 

PROVIDER: S-EPMC6063804 | biostudies-literature | 2018 Jul

REPOSITORIES: biostudies-literature