biostudies-literaturevan der Aart JCenter for Translational Molecular Medicine69https://www.ebi.ac.uk/biostudies/studies/S-EPMC6063804biostudies-literatureUnknown8(1)<h4>Background</h4>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, EJNMMI researchFirst in human evaluation of [¹⁸F]PK-209, a PET ligand for the ion channel binding site of NMDA receptors.PMC6063804LeARN 02N-101van der Pluijm Mvan Berckel BNMLammertsma AAvan der Aart JSchuit RCWindhorst ADMetaxas ABoellaard RKlein PJGolla SSVSchwarte LAfalseFirst in human evaluation of [¹⁸F]PK-209, a PET ligand for the ion channel binding site of NMDA receptors.<h4>Background</h4>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, 2018-01-01T00:00:00Z2018 Jul2025-04-19T06:30:42.758Z2019-03-26T23:50:42ZS-EPMC60638043005484610.1186/s13550-018-0424-2