"目錄號: HY-14418

GPCR/G Protein-

VU 0361737是一種選擇性mGlu4受體正變構(gòu)調(diào)節(jié)劑 (PAM), 作用于人類和大鼠受體, EC50分別為240 nM和110 nM, 對mGlu5和mGlu8受體具有微弱的作用活性, 對 mGlu1, mGlu2, mGlu3,? mGlu6, 和mGlu7受體沒有抑制活性。

mGluR

相關(guān)產(chǎn)品

CTEP-LY341495-LY354740-LY404039-RG7090-Mavoglurant-MPEP Hydrochloride-Dipraglurant-Topiramate-JNJ-40411813-L-Glutamine-FITM-JNJ16259685-MTEP hydrochloride-(S)-MCPG-

生物活性

Description

VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.IC50 value: 110 nM (EC50, for rat ), 240 nM (EC50, for human)Target: mGlu4in vitro: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [3]in vivo: VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [3]

References

[1].Jantas D, et al.? Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: the impact of cell differentiation state. Neuropharmacology. 2014 Aug;83:36-53

[2].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

[3].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.

[4].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 Ch