Synthesis and binding characteristics of N-(1-naphthyl)-N'-(3-[(125)I]-iodophenyl)-N'-methylguanidine ([(125)I]-CNS 1261): a potential SPECT agent for imaging NMDA receptor activation.
N-(1-Naphthyl)-N'-(3-[(125)I]-iodophenyl)-N'-methylguanidine ([(125)I]-CNS 1261) was synthesized as a potential radioligand to image N-methyl-D-aspartate (NMDA) receptor activation. [(125)I]-CNS 1261 was prepared by radioiodination of N-(1-naphthyl)-N'-(3-tributylstannylphenyl)-N'-methylguanidine using Na(125)I and peracetic acid. [(125)I]-CNS 1261 uptake in vivo reflected NMDA receptor distribution in normal rat brain, whereas in ischemic rat brain, uptake was markedly increased in areas of NMDA receptor activation. Radiolabeled CNS 1261 appears to be a good candidate for further development as a single photon emission computed tomography tracer in the investigation of NMDA receptor activation in cerebral ischemia.
Owens
J
J
Department of Clinical Physics, University of Glasgow, Glasgow, UK. j.owens@clinmed.gla.ac.uk
Tebbutt
A A
AA
McGregor
A L
AL
Kodama
K
K
Magar
S S
SS
Perlman
M E
ME
Robins
D J
DJ
Durant
G J
GJ
McCulloch
J
J
D000818:Animals; D001345:Autoradiography; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D001923:Brain Chemistry; D002545:Brain Ischemia / Q000000981:diagnostic imaging / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid; D016291:Dizocilpine Maleate / Q000493:pharmacokinetics; D006146:Guanidines / Q000097:blood / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D007457:Iodine Radioisotopes / Q000737:chemistry; D008024:Ligands; D008297:Male; D015394:Molecular Structure; D011869:Radioligand Assay; D051381:Rats; D017207:Rats, Sprague-Dawley; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
C417904:CNS 1261; D006146:Guanidines; D007457:Iodine Radioisotopes; D008024:Ligands; D016194:Receptors, N-Methyl-D-Aspartate; D016291:Dizocilpine Maleate