Synthesis, structure activity relationship, radiolabeling and preclinical evaluation of high affinity ligands for the ion channel of the N-methyl-D-aspartate receptor as potential imaging probes for positron emission tomography

P.J. Klein, J.A.M. Christiaans, A. Metaxas, R.C. Schuit, A.A. Lammertsma, B.N.M. van Berckel, A.D. Windhorst

Research output: Contribution to journalArticleAcademicpeer-review

16 Citations (Scopus)


The N-methyl-d-aspartate receptor (NMDAr) is involved in many neurological and psychiatric disorders including Alzheimer's disease and schizophrenia. Currently, it is not possible to assess NMDAr availability in vivo. The purpose of this study was to develop a positron emission tomography (PET) ligand for the NMDAr ion channel. A series of di- and tri-N-substituted diarylguanidines was synthesized. In addition, in vitro binding affinity for the NMDAr ion channel in rat forebrain membrane fractions was assessed. Compounds 10, 11 and 32 were radiolabeled with either carbon-11 or fluorine-18. Ligands [
Original languageEnglish
Pages (from-to)1189-1206
JournalBioorganic and Medicinal Chemistry
Issue number5
Publication statusPublished - 2015

Cite this