Synthesis and characterization ofN-(2-chloro-5-methylthiophenyl)-N′-(3-methylthiophenyl)-N′-[11C]methylguanidine [11C]CNS 5161, a candidate PET tracer for functional imaging of NMDA receptors

Autor:	David R. Turton, Sajinder K. Luthra, Yongjun Zhao, Erik Årstad, Frank Brady, Edward G. Robins
Rok vydání:	2006
Předmět:	Stereochemistry Organic Chemistry Glutamate receptor Neurotransmission Desmethyl Ligand (biochemistry) Biochemistry Chemical synthesis Analytical Chemistry chemistry.chemical_compound chemistry Drug Discovery NMDA receptor Radiology Nuclear Medicine and imaging Guanidine Receptor Spectroscopy
Zdroj:	Journal of Labelled Compounds and Radiopharmaceuticals. 49:163-170
ISSN:	1099-1344 0362-4803
DOI:	10.1002/jlcr.1033
Popis:	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.
Databáze:	OpenAIRE
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