LSN2814617 是一种具有口服活性、强效、脑渗透性和选择性 mGlu5（代谢型谷氨酸 5）正变构调节剂 (PAM)，EC50 值为 52 nM（人 mGlu5）和 42 nM（大鼠 mGlu5）。
货号:ajcx28250
CAS:1313498-08-6
分子式:C18H20FN5O
分子量：341.4
溶解度:DMF: Slightly soluble,DMSO: Slightly soluble,Ethanol: Slightly soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

LSN2814617 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5).¹It 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)