AMN082 explained

AMN082 (N,-dibenzhydrylethane-1,2-diamine) 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 central nervous system.

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 receptors, kainate receptors, and NMDA receptors. 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. AMN082 is pharmacological tool used to expand research on Group III mGluRs.

Notes and References

  1. Li X, Gardner EL, Xi ZX . The metabotropic glutamate receptor 7 (mGluR7) allosteric agonist AMN082 modulates nucleus accumbens GABA and glutamate, but not dopamine, in rats . Neuropharmacology . 54 . 3 . 542–51 . March 2008 . 18155073 . 2410088 . 10.1016/j.neuropharm.2007.11.005 .
  2. Palucha A, Klak K, Branski P, van der Putten H, Flor PJ, Pilc A . Activation of the mGlu7 receptor elicits antidepressant-like effects in mice . Psychopharmacology . 194 . 4 . 555–62 . November 2007 . 17622518 . 10.1007/s00213-007-0856-2 . 22011436 .