Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors

Heptahelical domain of metabotropic glutamate receptor 5 behaves like rhodopsin-like receptors.

Although agonists bind directly in the heptahelical domain (HD) of most class-I rhodopsin-like G protein coupled receptors (GPCRs), class-III agonists bind in the extracellular domain of their receptors. Indeed, the latter possess a large extracellular domain composed of a cysteine-rich domain and a Venus flytrap module. Both the low sequence homology and the structural organization of class-II...

Activation of metabotropic glutamate receptor 5 in the amygdala modulates pain-like behavior.

The central nucleus of the amygdala (CeA) has been identified as a site of nociceptive processing important for sensitization induced by peripheral injury. However, the cellular signaling components underlying this function remain unknown. Here, we identify metabotropic glutamate receptor 5 (mGluR5) as an integral component of nociceptive processing in the CeA. Pharmacological activation of mGl...

Metabotropic glutamate 5 receptor antagonism is associated with antidepressant-like effects in mice.

Antidepressant-like effects of metabotropic glutamate (mGlu)5 receptor antagonists have been reported previously. We now provide definitive identification of mGlu5 receptors as a target for these effects through the combined use of selective antagonists and mice with targeted deletion of the mGlu5 protein. In these experiments, the mGlu5 receptor antagonists 2-methyl-6-(phenylethynyl)-pyridine ...

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