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

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 sit...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2002-10, Vol.45 (11), p.955-964
Main Authors: Waterhouse, Rikki N., Dumont, Filip, Sultana, Abida, Simpson, Norman, Laruelle, Marc
Format: Article
Language:English
Subjects:
Biological and medical sciences
Contrast media. Radiopharmaceuticals
glutamate
Medical sciences
NMDA
PET
Pharmacology. Drug treatments
phencyclidine
radiotracer
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Summary: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: Ki = 5.2 ± 0.3 nM, log P = 2.34). The corresponding PET radiotracer [11C]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.
ISSN:0362-4803
1099-1344
DOI:10.1002/jlcr.622