Kinetic modelling of [123I]CNS 1261--a potential SPET tracer for the NMDA receptor.
N-(1-napthyl)-N'-(3-[(123)I]-iodophenyl)-N-methylguanidine ([(123)I]CNS 1261) is a novel SPET ligand developed for imaging the NMDA receptor intra-channel MK 801/PCP/ketamine site. Data was acquired in 7 healthy volunteers after bolus injection of [(123)I]CNS 1261. Kinetic modeling showed reversible tracer binding. Arterial and venous time-activity curves overlapped after 90 min. The rank order of binding was: Thalamus > striatum > cortical regions > white matter. This distribution concurs with [(11)C]-ketamine and [(18)F]-memantine PET studies. These data provide a methodological basis for further direct in vivo challenge studies.
Erlandsson
Kjell
K
Institute of Nuclear Medicine, Royal Free and University College Medical School, Middlesex Hospital, Mortimer Street, London W1T 3AA, UK. k.erlandsson@nucmed.ucl.ac.uk
Bressan
Rodrigo A
RA
Mulligan
Rachel S
RS
Gunn
Roger N
RN
Cunningham
Vincent J
VJ
Owens
Jonathan
J
Wyper
David
D
Ell
Peter J
PJ
Pilowsky
Lyn S
LS
D000328:Adult; D001921:Brain / Q000378:metabolism*; D005260:Female; D006146:Guanidines / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D008954:Models, Biological; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
C417904:CNS 1261; D006146:Guanidines; D016194:Receptors, N-Methyl-D-Aspartate