[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.
Cosford
Nicholas D P
ND
Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535, General Atomics Court, San Diego, CA 92121, USA. nicholas_cosford@merck.com
Roppe
Jeffrey
J
Tehrani
Lida
L
Schweiger
Edwin J
EJ
Seiders
T Jon
TJ
Chaudary
Ashok
A
Rao
Sara
S
Varney
Mark A
MA
D000818:Animals; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D011725:Pyridines / Q000493:pharmacokinetics / Q000494:pharmacology*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate / Q000187:drug effects*; D013844:Thiazoles / Q000493:pharmacokinetics / Q000494:pharmacology*
D008024:Ligands; D011725:Pyridines; D019275:Radiopharmaceuticals; D064529:Receptor, Metabotropic Glutamate 5; D018094:Receptors, Metabotropic Glutamate; D013844:Thiazoles; C469680:methoxymethyl-3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine