Open AccessMetabotropic Glutamate Receptor Subtype 5 Antagonists MPEP and MTEP
Author(s) -
Lea Paul M.,
Faden Alan I.
Publication year - 2006
Publication title -
cns drug reviews
Language(s) - English
Resource type - Journals
eISSN - 1527-3458
pISSN - 1080-563X
DOI - 10.1111/j.1527-3458.2006.00149.x
Subject(s) - metabotropic glutamate receptor 5 , metabotropic glutamate receptor 1 , metabotropic glutamate receptor , metabotropic glutamate receptor 2 , metabotropic glutamate receptor 7 , neuroscience , metabotropic receptor , metabotropic glutamate receptor 6 , pharmacology , metabotropic glutamate receptor 8 , metabotropic glutamate receptor 3 , glutamate receptor , metabotropic glutamate receptor 4 , nmda receptor , chemistry , medicine , receptor , psychology , biochemistry
ABSTRACT Glutamate regulates the function of central nervous system (CNS), in part, through the cAMP and/or IP3/DAG second messenger‐associated metabotropic glutamate receptors (mGluRs). The mGluR5 antagonist 2‐methyl‐6‐(phenylethynyl)‐pyridine (MPEP) has been extensively used to elucidate potential physiological and pathophysiological functions of mGluR5. Unfortunately, recent evidence indicates significant non‐specific actions of MPEP, including inhibition of NMDA receptors. In contrast, in vivo and in vitro characterization of the newer mGluR5 antagonist 3‐[(2‐methyl‐1,3‐thiazol‐4‐yl)ethynyl]pyridine (MTEP) indicates that it is more highly selective for mGluR5 over mGluR1, has no effect on other mGluR subtypes, and has fewer off‐target effects than MPEP. This article reviews literature on both of these mGluR5 antagonists, which suggests their possible utility in neurodegeneration, addiction, anxiety and pain management.