Agonist- and Reflex-Evoked Internalization of Metabotropic Glutamate Receptor 5 in Enteric Neurons

Agonist- and reflex-evoked internalization of metabotropic glutamate receptor 5 in enteric neurons.

We demonstrate that metabotropic glutamate receptor 5 (mGluR5) is present in the guinea pig ileum. A punctate ring-like distribution of immunoreactivity is found on the soma of a subset of neurons, consistent with an association of mGluR5 with the plasma membrane. mGluR5-containing cells in the submucosal plexus are predominantly noncholinergic and contain vasoactive intestinal peptide, a marke...

Phosphorylation-independent regulation of metabotropic glutamate receptor 5 desensitization and internalization by G protein-coupled receptor kinase 2 in neurons.

The uncoupling of metabotropic glutamate receptors (mGluRs) from heterotrimeric G proteins represents an essential feedback mechanism that protects neurons against receptor overstimulation that may ultimately result in damage. The desensitization of mGluR signaling is mediated by both second messenger-dependent protein kinases and G protein-coupled receptor kinases (GRKs). Unlike mGluR1, the at...

Group II Metabotropic Glutamate Receptor Agonist LY379268 Regulates AMPA Receptor Trafficking in Prefrontal Cortical Neurons

Group II metabotropic glutamate receptor (mGluR) agonists have emerged as potential treatment drugs for schizophrenia and other neurological disorders, whereas the mechanisms involved remain elusive. Here we examined the effects of LY379268 (LY37) on the expression and trafficking of the α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor subunits GluA1 and GluA2 in prefrontal neu...

Title : Metabotropic glutamate receptor 5 : a candidate

Background: Pharmacological modulation of metabotropic glutamate receptor 5 (mGluR5) is of marked interest as a novel therapeutic mechanism to treat schizophrenia and major depression. However, the status of mGluR5 in the pathophysiology of these disorders remains unknown. Discussion: The majority of studies in the schizophrenia post-mortem brain indicate that total mGluR5 expression is unalter...

A novel metabotropic glutamate receptor 5