PET studies of [18F]methyl-MK-801, a potential NMDA receptor complex radioligand.
Using positron emission tomography (PET), the potential of 18F-labelled fluoro-methyl-MK-801([18F]FMM) as a radioligand for in vivo studies of the NMDA receptor complex was investigated in baboons. In baseline conditions, there was a slight differential retention of [18F]FMM in cerebral cortex and striatum relative to cerebellum, compatible with specific binding. However, neither pretreatment with pharmacological doses of MK-801 or phencyclidine, nor severe, transient brain hypoxia, were able to clearly alter [18]FMM brain regional kinetics, indicating limited usefulness of this radioligand for in vivo PET investigations of the NMDA receptor.
Blin
J
J
Service Hospitalier Frederic Joliot, CEA, Departement de biologie, Orsay, France.
Denis
A
A
Yamaguchi
T
T
Crouzel
C
C
MacKenzie
E T
ET
Baron
J C
JC
D000818:Animals; D001921:Brain / Q000033:anatomy & histology; D001923:Brain Chemistry; D016291:Dizocilpine Maleate / Q000031:analogs & derivatives*; D000860:Hypoxia / Q000378:metabolism; D008297:Male; D010215:Papio / Q000378:metabolism*; D010622:Phencyclidine / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000187:drug effects / Q000378:metabolism*; D014055:Tomography, Emission-Computed
D016194:Receptors, N-Methyl-D-Aspartate; C068594:5-fluoromethyl MK 801; D016291:Dizocilpine Maleate; D010622:Phencyclidine