BMT-145027 is anmGluR5positive allosteric modulator without inherent agonist activity, exhibits anEC₅₀of 47 nM.

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].

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].

438.83

Solid

C₂₃H₁₄ClF₃N₄

2018282-44-3

Room temperature in continental US; may vary elsewhere.

DMSO : 2.4 mg/mL(5.47 mM;Need ultrasonic and warming)

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