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

Nicholas D P Cosford; Jeffrey Roppe; Lida Tehrani; Edwin J Schweiger; T Jon Seiders; Ashok Chaudary; Sara Rao; Mark A Varney

doi:10.1016/s0960-894x(02)00997-6

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

Bioorg Med Chem Lett. 2003 Feb 10;13(3):351-4. doi: 10.1016/s0960-894x(02)00997-6.

Authors

Nicholas D P Cosford¹, Jeffrey Roppe, Lida Tehrani, Edwin J Schweiger, T Jon Seiders, Ashok Chaudary, Sara Rao, Mark A Varney

Affiliation

¹ Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535, General Atomics Court, San Diego, CA 92121, USA. nicholas_cosford@merck.com

PMID: 12565928
DOI: 10.1016/s0960-894x(02)00997-6

Abstract

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.

MeSH terms

Animals
Binding Sites
Brain / drug effects
Brain / metabolism
Chemical Phenomena
Chemistry, Physical
Humans
In Vitro Techniques
Ligands
Male
Pyridines / pharmacokinetics
Pyridines / pharmacology*
Radiopharmaceuticals / pharmacokinetics
Radiopharmaceuticals / pharmacology*
Rats
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate / drug effects*
Thiazoles / pharmacokinetics
Thiazoles / pharmacology*

Substances

Ligands
Pyridines
Radiopharmaceuticals
Receptor, Metabotropic Glutamate 5
Receptors, Metabotropic Glutamate
Thiazoles
methoxymethyl-3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine