Synthesis and binding characteristics of N-(1-naphthyl)-N '-(3-[I-125]-iodophenyl)-N '-methylguanidine ([I-125]-CNS 1261): A potential SPECT agent for imaging NMDA receptor activation

N-(2 Naphthyl)-N'-(3-[I-125]-iodophenyl)-N'-methylguanidine ([I-125]-CNS 12 61) was syn thesized as a potential radioligand to image N-methyl-D-asparta te (NMDA) receptor activation. [I-125]-CNS 1261 was prepared by radioiodina tion of N-(1 naphthyl)-N'-(3-tributylstannyphenyl)-N'-methylguanidine using (NaI)-I-125 and peracetic acid. [I-125]-CNS 1261 uptake in vivo reflected NMDA receptor distribution in normal rat brain, whereas in ischemic rat bra in, uptake was markedly increased in areas of NMDA receptor activation. Rad iolabeled CNS 1261 appears to be a good candidate for further development a s a single photon emission computed tomography tracer in the investigation of NMDA receptor activation in cerebral ischemia. NUCL MED BIOL 27;6:557-56 4, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.