[ 3H]-Methoxymethyl-MTEP and [ 3H]-Methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor

[ 3H]-Methoxymethyl-MTEP and [ 3H]-Methoxy-PEPy: potent and selective radioligands for the metabotropic glutamate subtype 5 (mGlu5) receptor

The design, synthesis, and characterization of two potent, non-competitive radioligands, [ 3H]-methoxymethyl-MTEP and [ 3H]-methoxy-PEPy, that are selective for the mGlu5 receptor are described. Graphic

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2003-02, Vol.13 (3), p.351-354
Hauptverfasser: Cosford, Nicholas D.P, Roppe, Jeffrey, Tehrani, Lida, Schweiger, Edwin J, Seiders, T.Jon, Chaudary, Ashok, Rao, Sara, Varney, Mark A
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Binding Sites
Biological and medical sciences
Brain - drug effects
Brain - metabolism
Chemical Phenomena
Chemistry, Physical
Glutamatergic system (aspartate and other excitatory aminoacids)
Humans
In Vitro Techniques
Ligands
Male
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Pyridines - pharmacokinetics
Pyridines - pharmacology
Radiopharmaceuticals - pharmacokinetics
Radiopharmaceuticals - pharmacology
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate - drug effects
Thiazoles - pharmacokinetics
Thiazoles - pharmacology
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Beschreibung
Zusammenfassung:The design, synthesis, and characterization of two potent, non-competitive radioligands, [ 3H]-methoxymethyl-MTEP and [ 3H]-methoxy-PEPy, that are selective for the mGlu5 receptor are described. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00997-6