BMT-145027

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC 50 of 47 nM. In Vitro BMT-145027 is a compound with high MsLM stability (85% remaining), acceptable potency (EC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:mGluR5 47 nM (EC 50 )

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