AMN082

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AMN082 (N,N'-dibenzhydrylethane-1,2-diamine dihydrochloride) is a selective metabotropic glutamate receptor 7 (mGluR7) allosteric agonist.[1][2] 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.

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 AMPA, 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.

References

 

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