Biological Activity
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.
References
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)
