BMT-145027

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC₅₀ of 47 nM. IC50 & Target: IC50: 47 nM (mGluR5)^[1] In Vitro: BMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC₅₀=47 nM), and a modest decrease in planarity (Fsp3 = 0.17). Importantly, BMT-145027 lacks inherent mGluR5 agonist activity when tested at concentrations up to 16 μM^[1]. In Vivo: Drug-treated and control mice are shown two identical objects. After a 24-h natural forgetting period, the mice are reintroduced to a familiar object while simultaneously presented with a novel object. Since mice spend more time exploring unfamiliar objects, improved memory is measured as time spent exploring the novel object. BMT-145027 leads to a significant increase in time spent with the novel object when dosed at 30 mg/kg, with an apparent trend in novel object preference at 10 mg/kg. Satellite animals indicates a total plasma concentration of 2800 nM at 30 mg/kg^[1].