AMN082
Encyclopedia
AMN082 is a selective metabotropic glutamate receptor 7
(mGluR7) allosteric agonist
. It mimics the effect of glutamate. AMN082 is the first selective mGluR7 agonist
and has expanded the potential array of research opportunities on the effects of mGluR7 in the CNS.
, Kainate and NMDA
. Metabotropic receptors are G-protein coupled receptors that mediate slower, longer lasting effects through second messenger systems and are responsible for other neuronal functions that are not typically controlled by iGluRs. mGluRs are split into 3 separate groups (Group I, Group II, Group III) based on pharmacological profile, sequence homology, and preferred signal transduction pathway. mGlur7 is a member of Group III, the least studied of the groups. The discovery of AMN082 will serve as a useful pharmacological tool to expand research on Group III mGluRs.
Metabotropic glutamate receptor 7
Metabotropic glutamate receptor 7 is a protein that in humans is encoded by the GRM7 gene.-Agonists:*AMN082: allosteric agonist; induces rapid internalization; non-glutamatergic binding component-Interactions:...
(mGluR7) allosteric agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
. It mimics the effect of glutamate. AMN082 is the first selective mGluR7 agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
and has expanded the potential array of research opportunities on the effects of mGluR7 in the CNS.
Significance
The two main types of glutamate receptors are ionotropic receptors and metabotropic receptors. Ionotropic receptors (iGluRs) are fast-acting ligand-gated ion channels and include AMPAAMPA
AMPA is a compound that is a specific agonist for the AMPA receptor, where it mimics the effects of the neurotransmitter glutamate....
, Kainate and NMDA
NMDA
N-Methyl-D-aspartic acid or N-Methyl-D-aspartate is an amino acid derivative which acts as a specific agonist at the NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor...
. Metabotropic receptors are G-protein coupled receptors that mediate slower, longer lasting effects through second messenger systems and are responsible for other neuronal functions that are not typically controlled by iGluRs. mGluRs are split into 3 separate groups (Group I, Group II, Group III) based on pharmacological profile, sequence homology, and preferred signal transduction pathway. mGlur7 is a member of Group III, the least studied of the groups. The discovery of AMN082 will serve as a useful pharmacological tool to expand research on Group III mGluRs.