Preclinical pharmacology of mGlu2/3 receptor agonists: novel agents for schizophrenia?

Current Drug Targets. CNS and Neurological Disorders
Darryle D Schoepp DD, G J Marek

Abstract

Agonists for mGlu2/3 receptors decrease the evoked release of glutamate at certain (ie. forebrain / limbic) glutamatergic synapses, indicating that the functional role of mGlu2 and/or mGlu3 receptors is to suppress glutamate excitations. This offers a mechanism for dampening glutamate excitation under pathological states resulting from excessive glutamate release. Based, in part, on the psychotomimetic actions of phencyclidine (PCP)- like drugs, excessive or pathological glutamate release has been implicated in a number of clinical conditions including psychosis. With this in mind, the pharmacology of multiple mGlu2/3 receptor agonists have been investigated in PCP treated rats. Agonists for mGlu2/3 receptors such as LY354740 and LY379268 have been shown to block certain behavioral responses to PCP in rats. The effects of mGlu2/3 agonists on PCP-induced behaviors are blocked by a low doses of a selective mGlu2/3 receptor antagonist, indicating that these actions are mediated via mGlu2/3 receptors. In addition, mGlu2/3 agonists potently suppress glutamate release in rat prefrontal cortex, as reflected by excitatory post-synaptic potentials (EPSPs) induced by serotonin (5-HT) acting on 5HT(2A) receptors. These actions of LY354740...Continue Reading

Citations

Jul 8, 2005·Psychopharmacology·Charles H LargeDonald C Goff
Feb 26, 2005·Psychopharmacology·James N C Kew, John A Kemp
Mar 17, 2004·Current Opinion in Pharmacology·Gerard J Marek
Aug 21, 2003·Progress in Neurobiology·Mark J Millan
Dec 17, 2008·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·P Jeffrey Conn, Carrie K Jones
Nov 18, 2011·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Francesco MatriscianoAlessandro Guidotti
Jan 1, 2009·Nature Reviews. Drug Discovery·P Jeffrey ConnCraig W Lindsley
Oct 1, 2011·Science Translational Medicine·Daniel C JavittChi-Ming Lee
Jul 26, 2012·ISRN Pharmacology·Kyra-Verena SendtDerek K Tracy
Apr 21, 2011·Molecular Pharmacology·Francesco MatriscianoAlessandro Guidotti
Sep 14, 2012·Expert Opinion on Drug Discovery·Angelo Bifone, Alessandro Gozzi
Sep 25, 2012·Journal of Psychiatric Research·Fernando V GhedimAlexandra I Zugno
Nov 3, 2010·Neuropharmacology·F NicolettiJ P Pin
Nov 26, 2009·Bioorganic & Medicinal Chemistry Letters·Gary TresadernAndrés A Trabanco
Dec 9, 2008·Trends in Pharmacological Sciences·P Jeffrey ConnCarrie K Jones
Dec 8, 2007·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Amir KrivoyAbraham Weizman
Apr 17, 2007·Brain Research·Melanie J RobbinsPeter R Maycox
Jul 25, 2006·European Journal of Pharmacology·Gabor ImreGert J Ter Horst
Oct 1, 2013·Neurobiology of Disease·Hilary Highfield Nickols, P Jeffrey Conn
Nov 3, 2005·Expert Opinion on Emerging Drugs·Uriel Heresco-Levy
Aug 7, 2013·Bioorganic & Medicinal Chemistry Letters·Christopher L Cioffi
Feb 10, 2012·Bioorganic & Medicinal Chemistry Letters·Ji-Quan WangAnna-Liisa Brownell

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antipsychotic Drugs

Antipsychotic drugs are a class of medication primarily used to manage psychosis (including delusions, hallucinations, paranoia or disordered thought), principally in schizophrenia and bipolar disorder. Discover the latest research on antipsychotic drugs here