BMS-984923

BMS-984923 (BMS-984923) is a potent silent allosteric modulator (SAM) of mGluR5 with competitive antagonism of MPEPy binding with Ki of 0.6 nM, but has no detectable agonist and antagonist activity at mGluR5 signaling; does not affect glutamate/DHPG ((S)-3,5-Dihydroxyphenylglycine)-induced Ca2+ signaling in mGluR5-overexpressing HEK293T cells and cultured nureons; reduces the interaction of PrPC with mGluR5 in membrane fractions, prevents Aβo-induced signal transduction in brain slices, and rescues memory deficits and synaptic depletion in the APPswe/PS1ΔE9 transgenic mouse brain.

References 1. Huang H, et al. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9. 2. Haas LT, et al. Cell Rep. 2017 Jul 5;20(1):76-88. View Related Products by Target mGluR