LSN2814617 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5).1 It potentiates glutamate-induced calcium mobilization in MCB3901 cells expressing human mGluR5 (EC50 = 52 nM). LSN2814617 increases rat hippocampal mGluR5 receptor occupancy (ED50 = 13 mg/kg). It increases wakefulness and decreases non-rapid eye movement (NREM) and REM sleep in rats when administered at doses of 0.3, 1, and 3 mg/kg.
1.Gilmour, G., Broad, L.M., Wafford, K.A., et al.In vitro characterisation of the novel positive allosteric modulators of the mGlu5 receptor, LSN2463359 and LSN2814617, and their effects on sleep architecture and operant responding in the ratNeuropharmacology64224-239(2013)
