BMT-145027是mGluR5的正变构调节物且没有固有的激动剂活性，EC50值为47nM。
CAS：2018282-44-3
分子式：C23H14ClF3N4
分子量：438.83
纯度：98%
存储：Store at -20°C

Background:

BMT-145027 is an mGluR5 positive allosteric modulator without inherent agonist activity, exhibits an EC50 of 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].

[1]. Hill MD, et al. Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators. ACS Med Chem Lett. 2016 Oct 3;7(12):1082-1086.