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Synthesis of [ 11 C] N ‐(2‐chloro‐5‐thiomethylphenyl)‐ N ′‐(3‐methoxyphenyl)‐ N ′‐methylguanidine ([ 11 C]GMOM): a candidate PET tracer for imaging the PCP site of the NMDA ion channel
Author(s) -
Waterhouse Rikki N.,
Dumont Filip,
Sultana Abida,
Simpson Norman,
Laruelle Marc
Publication year - 2002
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.622
Subject(s) - chemistry , nmda receptor , in vivo , ligand (biochemistry) , saline , stereochemistry , receptor , biochemistry , medicine , microbiology and biotechnology , biology
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.