LY2979165

LY2979165 is an alanine prodrug of 2812223, a selective and potent orthosteric mGlu2 (metabotropic glutamate receptor 2) receptor agonist. It was developed by Eli Lilly & Co. for potential treatment of psychiatric conditions. The drug was studied in clinical trials for bipolar disorder (Phase 1), and aggression/agitation in Alzheimer's disease (Phase 2). However, its development has been discontinued. Pharmacologically, LY2979165 is extensively converted to its active moiety 2812223 in the body. It showed activity in animal models of psychosis sensitive to mGlu2 activation and demonstrated the ability to attenuate ketamine-induced BOLD signals in healthy volunteers. Single oral doses up to 60 mg were well tolerated, with common adverse events including nausea, vomiting, dizziness, somnolence, and headache. Dose titration allowed higher doses to be tested.

Other names

2,4-Dinitrophenol (for Mitochon Pharmaceuticals' drug)LY-2979165 (for Mediti Pharma's drug)dimiracetam R:S 3:1 non-racemic mixture (for neuropathic pain candidate)