AMN082 is an orally bioavailable allosteric agonist of metabotropic glutamate receptor 7 (mGluR7). It inhibits cAMP accumulation induced by forskolin in CHO cells expressing human mGluR7b (EC50 = 64 nM). AMN082 (10 μM) is selective for mGluR7a and mGluR7b over mGluR1b, mGluR4, and mGluR8a with 140, 90, 15, 18, and 20% activation, respectively, as well as over mGluR2, mGluR3, mGluR5a, mGluR6, GluR3, and NMDA receptors containing NR1a, NR2A, or NR2B subunits. AMN082 also binds to the norepinephrine transporter (NET) and α1-adrenergic receptor (α1-AR). It increases the proliferation of neural progenitor cells (NPCs) and induces their differentiation into neurons when used at a concentration of 1 μM. AMN082 (2.5 mg/kg) inhibits apomorphine-induced circling in a rat model of Parkinson''s disease induced by 6-hydroxy dopamine (6-OHDA; ).
