Y. Zhao, E. Robins, D. Turton
Feb 1, 2006
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0
Influential Citations
18
Citations
Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
N-methyl-D-aspartate (NMDA) receptors play a key role in excitatory neurotransmission and are linked to a variety of acute and chronic neurodegenerative diseases including epilepsy, schizophrenia, Parkinson's disease and drug abuse. N-(2-chloro-5-methylthiophenyl)-N′-(3-methylthiophenyl)-N′-methylguanidine (CNS 5161) is a high affinity ligand (Ki=1.87±0.25 nM) for the NMDA PCP site, which potentially can be used for functional imaging of this receptor. Herein we report the synthesis of the corresponding positron emission tomography (PET) tracer [11C]CNS 5161 by means of [11C]methylation of the desmethyl guanidine precursor. [11C]CNS 5161 was synthesized with a decay corrected radiochemical yield of 10% within 45 min after end of bombardment (EOB). The final product was prepared in a sterile saline solution suitable for clinical studies with a radiochemical purity of >96% and a specific activity of 41 GBq/mmol at time of injection. Copyright © 2005 John Wiley & Sons, Ltd.