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Synthesis of [11C] N-(2-chloro-5-thiomethylphenyl)-N′-(3-methoxyphenyl)-N′-methylguanidine ([11C]GMOM): a candidate PET tracer for imaging the PCP site of the NMDA ion channel

✍ Scribed by Rikki N. Waterhouse; Filip Dumont; Abida Sultana; Norman Simpson; Marc Laruelle

Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
109 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

The N‐methyl‐D‐aspartate (NMDA) ion channel plays an important role in a number of neurodegenerative disorders including stroke, Parkinson's disease, Huntington's Chorea, Alzheimer's disease, schizophrenia and epilepsy. To provide effective radioligands for imaging the PCP binding site of the NMDA ion channel, we synthesized and characterized in vitro the candidate PCP site ligand N‐(2‐chloro‐5‐thiomethylphenyl)‐N′‐(3‐methoxyphenyl)‐N′‐methylguanidine (GMOM: K~i~ = 5.2 ± 0.3 nM, log P = 2.34). The corresponding PET radiotracer [^11^C]GMOM was synthesized with a radiochemical yield of 8.4 ± 3.2% EOS and with a specific activity of 1.23 ± 0.25 Ci/μmol EOS (n = 5). The average time required for synthesis, purification and formulation was 52 ± 5 min. The final product was prepared in a sterile saline solution suitable for in vivo use. Copyright © 2002 John Wiley & Sons, Ltd.

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