TY - JOUR
T1 - 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
AU - Klein, P.J.
AU - Christiaans, J.A.M.
AU - Metaxas, A.
AU - Schuit, R.C.
AU - Lammertsma, A.A.
AU - van Berckel, B.N.M.
AU - Windhorst, A.D.
PY - 2015
Y1 - 2015
N2 - 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 [
AB - 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 [
UR - https://www.scopus.com/pages/publications/84923088280
UR - https://www.scopus.com/inward/citedby.url?scp=84923088280&partnerID=8YFLogxK
U2 - 10.1016/j.bmc.2014.12.029
DO - 10.1016/j.bmc.2014.12.029
M3 - Article
SN - 0968-0896
VL - 23
SP - 1189
EP - 1206
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 5
ER -