VU 0361737 (VU0361737)是mGlu4受体(mGluR4)选择性正变构调节剂,作用于人mGlu4受体的EC50为0.24 µM,可渗入中枢神经系统,具有神经保护作用,对mGluR1/2/3/6/7无明显作用,对mGluR5和mGluR8显现出较弱的活性。
参考文献
[1] Engers DW, et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.
[2] Engers DW, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Chem. 2011 Feb 24;54(4):1106-10.
[3] Jantas D, et al. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124-37.
冰袋运输。粉末直接保存于-25~-15℃,有效期3年。建议分装后-25~-15℃干燥保存,避免反复冻融。





